Cytoskeleton - MedchemExpress.com...Inhibitors, Agonists, Screening Libraries Cytoskeleton The...
Transcript of Cytoskeleton - MedchemExpress.com...Inhibitors, Agonists, Screening Libraries Cytoskeleton The...
Inhibitors, Agonists, Screening Librarieswww.MedChemExpress.com
Cytoskeleton
The cytoskeleton is a filamentous network of F-actin, microtubules, and intermediate filaments (IFs) composed of one of threechemically distinct subunits, actin, tubulin, or one of several classes of IF protein. Cytoskeleton not only helps cells maintain theirshape and internal organization, but also provides mechanical support that enables cells to carry out essential functions likedivision and movement.
The cytoskeleton is involved in intracellular signal transduction at least two ways. First, individual proteins of the cytoskeleton mightparticipate directly in signal transduction by linking two or more signaling proteins. Second, the cytoskeleton might provide amacromolecular scaffold, which spatially organizes components of a signal transduction cascade. Cell migration is a complex andmultistep process involved in homeostasis maintenance, morphogenesis, and disease development, such as cancer metastasis, andrequires coordination of cytoskeletal dynamics and reorganization, cell adhesion, and signal transduction, and takes a variety offorms. Many signaling pathways including Rho-family GTPases, Paxillin/FAK signaling and PI3K signaling is involved in the processby regulating cytoskeletal activity.
Since the cytoskeleton is involved in virtually all cellular processes, abnormalities in this essential cellular component frequentlyresult in disease. Drugs that modulate microtubule stability, inhibitors of posttranslational modifications of cytoskeletalcomponents, specifically compounds affecting the levels of tubulin acetylation, and compounds targeting signaling moleculeswhich regulate cytoskeleton dynamics, constitute the mostly addressed therapeutic interventions for the diseases including cancerand neurodegenerative disorders.
References:[1] Janmey PA. Physiol Rev. 1998 Jul;78(3):763-81.[2] Forgacs G, et al. J Cell Sci. 2004 Jun 1;117(Pt 13):2769-75.[3] Eira J, et al. . Prog Neurobiol. 2016 Jun;141:61-82.
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• Arp2/3 Complex 3
• Dynamin 5
• Gap Junction Protein 7
• Integrin 10
• Kinesin 17
• Microtubule/Tubulin 20
• Mps1 34
• Myosin 37
• PAK 40
Inhibitors, Agonists, Screening Librarieswww.MedChemExpress.com
Target List in Cytoskeleton
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Arp2/3 ComplexActin-related protein 2/3 complex
The intact ARP2/3 complex is first purified from based on its affinity for the actin-binding protein profilin,Acanthamoeba castellaniiand is shown to consist of a stable assembly of seven polypeptides. Two of the subunits are actin-related proteins of the ARP2 andARP3 subfamilies, giving the complex its name.
The ARP2/3 complex possesses little biochemical activity on its own. However, when engaged by nucleation-promoting factor (NPF)proteins, it is activated to initiate the formation of a new (daughter) filament that emerges from an existing (mother) filament in ay-branch configuration with a regular 70° branch angle. This coupling of nucleation and branching by the ARP2/3 complex isreferred to as autocatalytic branching or dendritic nucleation, and is central to its functions in vivo.
Polymerization of actin filaments directed by the Arp2/3 complex supports many types of cellular movements.
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Arp2/3 Complex Inhibitors
CK-636 (CK-0944636) Cat. No.: HY-15892
CK-636 is a cell permeable inhibitor of Arp2/3, that could inhibit actincomplex
polymerization, with values of 4 μM, 24 μMIC50
and 32 μM for human, fission yeast and bovine,respectively.
Purity: 98.10%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg
CK-666Cat. No.: HY-16926
CK-666 is a cell-permeable inhibitor ofactin-related protein , andArp2/3 complexbinds to Arp2/3 complex, stabilizes the inactivestate of the complex, blocking movement of theArp2 and Arp3 subunits into the activatedfilament-like (short pitch) conformation.
Purity: 99.63%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg
CK-869Cat. No.: HY-16927
CK-869 is an Actin-Related Protein 2/3 (ARP2/3)complex inhibitor, with an of 7 μM.IC50
Purity: 99.76%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg
Cytochalasin B (Phomin) Cat. No.: HY-16928
Cytochalasin B is a cell-permeable mycotoxinbinding to the barbed end of filaments,actindisrupting the formation of actin polymers, with
value of 1.4-2.2 nM for F-actin.Kd
Purity: >99.0%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg
Cytochalasin D (Zygosporin A; NSC 209835) Cat. No.: HY-N6682
Cytochalasin D (Zygosporin A; NSC 209835) is apotent and cell-permeable inhibitor of actinpolymerization derived from fungus, inhibits theG-actin–cofilin interaction by binding to G-actin.
Purity: >99.0%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 1 mg
Dihydrocytochalasin BCat. No.: HY-N6701
Dihydrocytochalasin B (H2CB) is a Cytokinesisinhibitor and changes the morphology of the cells,similar to that of cytochalasin B; does notinhibit glucose transport.
Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg
Latrunculin A (LAT-A) Cat. No.: HY-16929
Latrunculin A (LAT-A) is a toxin isolated from thered sea sponge , binds toLatrunculia magnificaactin monomers, inhibits polymerization of actin,with s of 0.1, 0.4, 4.7 μM and 0.19 μM forKd
ATP-actin, ADP-Pi-actin, ADP-actin and G-actin,respectively.
Purity: >95.0%Clinical Data: No Development ReportedSize: 100 μg (0.2 mM * 1 mL in Ethanol),
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Dynamin
Dynamins are large superfamily GTPase proteins that are involved in various cellular processes including budding of transportvesicles, division of organelles, cytokinesis, and pathogen resistance. Dynamins are involved in scission (cleavage of the vesicle fromthe parent membrane) of nascent vesicles from parent membranes in eukaryotic cells. Dynamins interact directly with the lipidbilayer at the necks of clathrin-coated pits to sever and release coated vesicles. Dynamins contain five domains, including GTPasedomain, middle domain, PH domain, GTPase effector domain (GED), and proline rich domain (PRD), while the dynamin-relatedproteins (DRPs) lack one or more of these domains or have additional domains. Dynamins and DRPs participate in a wide variety ofcellular processes, including budding mitochondrial fission (mammalian Dlp1 and Dnm1) and fusionSaccharomyces cerevisiae(mammalian OPA1, Mgm1 and Msp1), vacuolar fission ( Vps1),S.cerevisiae Schizosaccharomycespombe S. cerevisiaeinterferon-induced anti-viral protection (fish Mx proteins), plant cell cytokinesis and membrane fission ( DRPArabidopsis thalianaproteins), as well as pathogen resistance.
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Dynamin Inhibitors
DynasoreCat. No.: HY-15304
Dynasore is a cell-permeable inhibitordynaminwith an of 15 μM.IC50
Purity: 99.61%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 10 mg, 50 mg
Mdivi-1 (Mitochondrial division inhibitor 1) Cat. No.: HY-15886
Mdivi-1 is a selective dynamin-related protein 1( ) inhibitor. Mdivi-1 is a mitochondrialDrp1division/ inhibitor.mitophagy
Purity: 98.75%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg
SchaftosideCat. No.: HY-N0703
Schaftoside is a flavonoid found in a variety ofChinese herbal medicines, such as .Eleusine indicaSchaftoside inhibits the expression of TLR4 andMyd88. Schaftoside also decreases Drp1 expressionand phosphorylation, and reduces mitochondrialfission.
Purity: >99.0%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 20 mg
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Gap Junction Protein
Gap junction channels are essential in normal heart function and they assist in the mediated spread of electrical impulses thatstimulate synchronized contraction (via an electrical syncytium) of cardiac tissues.
Gap junction (GJ) proteins play an important role in direct communication between cells of many tissue types. GJs are specialisedintercellular membrane-spanning domains that allow the passage of small molecules including second messenger (e.g. c-AMP,inositol triphosphate) or ionic signals from one cell to another. GJ proteins and their long evolutionary history have permittedadaptation of gap junction intercellular communication (GJIC) with several important functions and multiple regulatory processes.Formation of GJIC is an essential mechanism in coordinating growth and development and tissue compartmentalization duringembryonic development.
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Gap Junction Protein Inhibitors & Modulators
AT-1002Cat. No.: HY-114426
AT-1002, a 6-mer synthetic peptide, is a tight regulator and absorption enhancer.junction
Purity: >98%Clinical Data: No Development ReportedSize: 250 mg, 500 mg
AT-1002 TFACat. No.: HY-114426A
AT-1002 TFA, a 6-mer synthetic peptide, is a tight regulator and absorption enhancer.junction
Purity: 99.84%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg
Danegaptide (GAP-134; ZP 1609) Cat. No.: HY-10913
Danegaptide (GAP-134), a small modified dipeptide,has been identified as a potent and selectivesecond generation gap junction modifier with oralbioavailability.
Purity: >98%Clinical Data: Phase 2Size: 1 mg, 5 mg
Danegaptide Hydrochloride (GAP-134 (Hydrochloride); ZP 1609 Hydrochloride) Cat. No.: HY-10913A
Danegaptide Hydrochloride (GAP-134 Hydrochloride)is a selective modifier of the gap junctionprotein.
Purity: 99.75%Clinical Data: Phase 2Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg
Gap 26Cat. No.: HY-P1082
Gap 26 is a connexin mimetic peptide correspondingto the residues 63-75 of connexin 43, which is a
blocker.gap junction
Purity: 99.30%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg
Gap 27Cat. No.: HY-P0139
Gap 27, connexin43 mimetic peptide, is a gap inhibitor.junction
Purity: 98.34%Clinical Data: No Development ReportedSize: 1 mg, 5 mg
Gap19Cat. No.: HY-P1136
Gap19, a peptide derived from nine amino acids ofthe Cx43 cytoplasmic loop (CL), is a potent andselective connexin 43 (Cx43) hemichannelblocker. Gap19 inhibits hemichannels caused bypreventing intramolecular interactions of theC-terminus (CT) with the CL.
Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg
Gap19 TFACat. No.: HY-P1136A
Gap19 TFA, a peptide derived from nine amino acidsof the Cx43 cytoplasmic loop (CL), is a potent andselective connexin 43 (Cx43) hemichannelblocker. Gap19 TFA inhibits hemichannels caused bypreventing intramolecular interactions of theC-terminus (CT) with the CL.
Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg
Larazotide acetateCat. No.: HY-106268A
Larazotide acetate is a synthetic peptide thatfunctions as a tight junction regulator andreverses leaky junctions to their normally closedstate.
Purity: 99.68%Clinical Data: Phase 2Size: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg, 25 mg
Meclofenamate sodium (Meclofenamic acid sodium) Cat. No.: HY-B1320
Meclofenamic acid sodium is a nonsteroidalanti-inflammatory drug (NSAID) approved for use inarthritis (osteo and rheumatoid), analgesia (mildto moderate pain), dysmenorrhea, and heavymenstrual blood loss (menorrhagia).
Purity: 98.62%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 50 mg, 100 mg, 200 mg
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Meclofenamic acidCat. No.: HY-117275
Meclofenamic acid is a nonsteroidalanti-inflammatory drug (NSAID) approved for use inarthritis (osteo and rheumatoid), analgesia (mildto moderate pain), dysmenorrhea, and heavymenstrual blood loss (menorrhagia).
Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg
Tonabersat (SB-220453) Cat. No.: HY-15204
Tonabersat is a modulator.gap-junction
Purity: 99.68%Clinical Data: Phase 2Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg
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Integrin
Integrins, a family of heterodimeric adhesion receptors for diverse extracellular matrices, have consistently been implicated ascrucial drivers of ovarian cancer development and progression. A number of the RGD-based members of the integrin family,including α5β1, and αvβ3 or αvβ5 integrins, are markedly elevated in aggressive ovarian tumors. These adhesion receptors appearto promote cell adhesion, survival, motility and invasion during ovarian tumor growth or metastatic progression. Importantly, thefunctions of these integrins are strongly dependent on the activation of focal adhesion kinase (FAK) and its downstream signaling,including the PI3K/Akt- and Ras/MAPK-dependent pathways.
Integrins are transmembrane proteins and are major receptors for cell-extracellular matrix (ECM) and cell-cell adhesion. Modulationof these molecules, particularly αv integrin family, has exhibited profound effects on fibrosis in multiple organ and disease state.Based on the several studies, the integrins αvβ3, αvβ5, αvβ6, and αvβ8 have been known to modulate the fibrotic process viaactivation of latent transforming growth factor (TGF)-β in pre-clinical models of fibrosis.
Each integrin is typically formed by the non-covalent pairing of one α subunit, of which, 18 types are known to exist, and one βsubunit, of which 8 types are known to exist. Together, 24 distinct heterodimers have been identified to date. The αv subunit canform heterodimers with the β1, β3, β5, β6 or β8 subunits and β1 can associate with many different α subunits from α1 to α11, andαv, indicating that not all theoretically possible α and subunit pairs form. Interestingly, the activation of TGF-β appears to be acommon function of multiple αv integrins.
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Integrin Inhibitors, Antagonists & Modulators
Arg-Gly-Asp-Ser (RGDS peptide; Fibronectin tetrapeptide) Cat. No.: HY-12290
Arg-Gly-Asp-Ser is an integrin binding sequencethat inhibits function,integrin receptordecreases systemic inflammation via inhibition ofcollagen-triggered activation of leukocytes andattenuates expression of inflammatory cytokines,iNOS and MMP-9.
Purity: >98.0%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg
Arg-Gly-Asp-Ser (TFA) (RGDS peptide (TFA); Fibronectin tetrapeptide (TFA)) Cat. No.: HY-12290A
Arg-Gly-Asp-Ser (TFA) is an integrin bindingsequence that inhibits function.integrin receptorArg-Gly-Asp-Ser (TFA) directly and specificallybind pro-caspase-8, pro-caspase-9 andpro-caspase-3, while it does not bindpro-caspase-1.
Purity: >98%Clinical Data:Size: 1 mg, 5 mg
ATN-161Cat. No.: HY-13535
ATN-161 is a novel antagonist, whichintegrin α5β1inhibits angiogenesis and growth of livermetastases in a murine model.
Purity: >98%Clinical Data: Phase 2Size: 5 mg, 10 mg, 50 mg, 100 mg
ATN-161 trifluoroacetate salt (ATN-161 TFA salt) Cat. No.: HY-13535A
ATN-161 trifluoroacetate salt is a novel integrin antagonist, which inhibits angiogenesis andα5β1
growth of liver metastases in a murine model.
Purity: >95.0%Clinical Data: Phase 2Size: 5 mg, 10 mg, 50 mg, 100 mg
BI-1950Cat. No.: HY-124040
BI-1950 is a highly potent lymphocyte function inhibitor. LFA-1 isassociated antigen-1 (LFA-1)
an essential component in normal immune systemfunction and a target for drug discovery.
Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg
BMS-688521Cat. No.: HY-10596
BMS-688521 is a highly potent, orally activeinhibitor of the interaction, withLFA-1/ICAMan of 2.5 nM in the adhesion assay and anIC50
of 60 nM in the MLR assay. BMS-688521 isIC50
efficacious in a mouse allergic eosinophilic lunginflammation model.
Purity: >98%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg
c(phg-isoDGR-(NMe)k)Cat. No.: HY-111413
c(phg-isoDGR-(NMe)k) is a selective and potent ligand with an of 2.9 nM.α5β1-integrin IC50
Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg
c(phg-isoDGR-(NMe)k) TFACat. No.: HY-111413A
c(phg-isoDGR-(NMe)k) TFA is a selective and potent ligand with an of 2.9 nM.α5β1-integrin IC50
Purity: >98%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg
CarotegrastCat. No.: HY-14857
Carotegrast is an orally available α4 integrin inhibitor with anti-inflammatoriesreceptor
activities.
Purity: >98%Clinical Data: No Development ReportedSize: 100 mg, 250 mg, 500 mg
Cilengitide (EMD 121974) Cat. No.: HY-16141
Cilengitide is a potent and selective integrininhibitor for α β and α β receptor, withv 3 v 5
s of 4 and 79 nM, respectively.IC50
Purity: 99.06%Clinical Data: Phase 3Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg
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Cucurbitacin BCat. No.: HY-N0416
Cucurbitacin B belongs to a class of highlyoxidized tetracyclic triterpenoids; could represscancer cell progression.
Purity: 99.92%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg
CWHM-12Cat. No.: HY-18644
CWHM-12 is a potent inhibitor of withαV integrinss of 0.2, 0.8, 1.5, and 1.8 nM for ,IC50 αvβ8
, , and .αvβ3 αvβ6 αvβ1
Purity: 99.65%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg
Cyclo(-RGDfK)Cat. No.: HY-P0023
Cyclo(-RGDfK) is a potent and selective inhibitorof the integrin, with an of 0.94 nM.α βv 3 IC50
Purity: >98.0%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg
Cyclo(Arg-Gly-Asp-D-Phe-Val) TFACat. No.: HY-P1613A
Cyclo(Arg-Gly-Asp-D-Phe-Val) (TFA) is an inhibitorof , with antitumor activity.integrin αvβ3
Purity: 99.40%Clinical Data: No Development ReportedSize: 1 mg, 5 mg
Cyclo(RADfK)Cat. No.: HY-P0031
Cyclo(RADfK) is a selective α(v)β(3) integrinligand that has been extensively used forresearch, therapy, and diagnosis ofneoangiogenesis.
Purity: 98.03%Clinical Data: No Development ReportedSize: 1 mg
Cyclo(RGDyK)Cat. No.: HY-100563A
Cyclo(RGDyK) is a potent and selective α βV 3
inhibitor with an of 20 nM.integrin IC50
Purity: >98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg
Cyclo(RGDyK) trifluoroacetateCat. No.: HY-100563
Cyclo(RGDyK) trifluoroacetate is a potent andselective inhibitor with an α β integrinV 3 IC50
of 20 nM.
Purity: 99.13%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg
E7820 (ER68203-00) Cat. No.: HY-14571
E7820 is an angiogenesis inhibitor by suppressing, a cell adhesion molecule expressed onintegrin a2
endothelial cells.
Purity: 99.36%Clinical Data: Phase 2Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg
EptifibatideCat. No.: HY-B0686
Eptifibatide is a cyclic heptapeptide, acts as acompetitive antagonist for the activated platelet
, with anti-plateletglycoprotein IIb/IIIa receptoractivity.
Purity: 96.49%Clinical Data: LaunchedSize: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg
Firategrast (SB 683699) Cat. No.: HY-14951
Firategrast is an orally bioavailable /α4β1 α4β7 antagonist.integrin
Purity: 99.66%Clinical Data: Phase 2Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg
12 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]
Fradafiban (BIBU-52) Cat. No.: HY-101720
Fradafiban is a nonpeptide platelet glycoproteinIIb/IIIa antagonist, which binds to the humanplatelet GP IIb/IIIa complex with a K value ofd
148 nM.
Purity: >98%Clinical Data: Phase 1Size: 1 mg, 5 mg, 10 mg, 20 mg
GLPG0187Cat. No.: HY-100506
GLPG0187 is a broad spectrum receptorintegrinantagonist with antitumor activity; inhibitsα β -integrin with an of 1.3 nM.v 1 IC50
Purity: 98.97%Clinical Data: Phase 1Size: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg
Gly-Arg-Gly-Asp-SerCat. No.: HY-P0295
Gly-Arg-Gly-Asp-Ser is a pentapeptide that formsthe cell-binding domain of a glycoprotein,osteopontin. Gly-Arg-Gly-Asp-Ser binds to integrinreceptors αvβ3 and αvβ5 with estimated of 5IC50
and 6.5 μM.
Purity: 98.12%Clinical Data: No Development ReportedSize: 2 mg, 5 mg, 10 mg, 25 mg
Gly-Arg-Gly-Asp-Ser (TFA)Cat. No.: HY-P0295A
Gly-Arg-Gly-Asp-Ser (TFA) is a pentapeptide thatforms the cell-binding domain of a glycoprotein,osteopontin. Gly-Arg-Gly-Asp-Ser binds to integrin
αvβ3 and αvβ5 with estimated of 5receptors IC50
and 6.5 μM.
Purity: >98%Clinical Data:Size: 1 mg, 5 mg
GRGDSPCat. No.: HY-P0290
GRGDSP, a synthetic linear RGD peptide, is an inhibitor.integrin
Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg
GRGDSP TFACat. No.: HY-P0290A
GRGDSP (TFA) is an inhibitor.integrin
Purity: 98.53%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg
ILK-IN-2 (OSU-T315 analog) Cat. No.: HY-18676B
ILK-IN-2 (OSU-T315 analog) is a ILK inhibitor.
Purity: >98.0%Clinical Data: No Development ReportedSize: 2 mg, 5 mg, 10 mg
Integrin Antagonists 27Cat. No.: HY-18668
Integrin Antagonists 27 is a small moleculeintegrin αvβ3 antagonist with binding affinity of18 nM, as s novel anticancer agent.
Purity: >98.0%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg
Integrin-IN-2Cat. No.: HY-130119
Integrin-IN-2 (compound 39) is an orallybioavailable pan inhibitor.αv integrinIntegrin-IN-2 can increases the , ,αvβ6 αvβ3
and binding affinities with αvβ5 αvβ8 pIC50
values of 7.8, 8.4, 8.4 and 7.4, respectively.
Purity: >98%Clinical Data: No Development ReportedSize: 100 mg, 250 mg, 500 mg
iRGD peptide (c(CRGDKGPDC)) Cat. No.: HY-P0122
iRGD peptide is a 9-amino acid cyclic peptide,triggers tissue penetration of drugs by firstbinding to , then proteolyticallyav integrinscleaved in the tumor to produce CRGDK/R tointeract with neuropilin-1, and hastumor-targeting and tumor-penetrating properties.
Purity: 98.62%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg
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IrigeninCat. No.: HY-N2587
Irigenin is a is a lead compound, and mediates itsanti-metastatic effect by specifically andselectively blocking and integrinsα9β1 α4β1binding sites on C-C loop of Extra Domain A (EDA).Irigenin shows anti-cancer properties.
Purity: >98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 20 mg
Lifitegrast (SAR 1118; SHP-606) Cat. No.: HY-19344
Lifitegrast (SAR 1118) is an integrin lymphocytefunction-associated antigen-1 ( ) antagonist;LFA-1inhibits Jurkat T cell attachment to ICAM-1with an of 2.98 nM.IC50
Purity: 99.58%Clinical Data: LaunchedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg
LXW7Cat. No.: HY-P0178
LXW7 is an octamer disulfide cyclic peptide, alsoa ligand, acts as a potent andαvβ3 integrinspecific endothelial progenitor cells (EPCs) andendothelial cells (ECs) targeting ligand. LXW7increases phosphorylation of VEGFR-2 andactivation of ERK1/2.
Purity: >98%Clinical Data: No Development ReportedSize: 100 mg, 250 mg, 500 mg
MK-0429 (L-000845704) Cat. No.: HY-15102
MK-0429 (L-000845704) is an orally active, potent,selective and nonpeptide antagonistαvβ3 integrinwith an of 80 nM.IC50
Purity: 99.73%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg
NatalizumabCat. No.: HY-108831
Natalizumab is a recombinant, humanized monoclonalantibody, binds to α4β1- and blocks itsintegrininteraction with vascular cell adhesion molecule-1(VCAM-1). Natalizumab can be used for thetreatment of relapsing remitting multiplesclerosis and Crohn's disease.
Purity: >98%Clinical Data: No Development ReportedSize: 100 mg, 250 mg, 500 mg
OSU-T315Cat. No.: HY-18676
OSU-T315 (ILK-IN-1) is a small Integrin-linkedkinase inhibitor with an IC of 0.6 μM,(ILK) 50
inhibiting PI3K/AKT signaling by dephosphorylationof AKT-Ser473 and other ILK targets (GSK-3β andmyosin light chain).
Purity: 99.88%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 2 mg, 5 mg, 10 mg, 50 mg
RGDCat. No.: HY-P0278
RGD is a tripeptide that effectively triggers celladhesion, addresses certain cell lines and elicitsspecific cell responses; binds to .integrins
Purity: >98%Clinical Data: Phase 2Size: 5 mg, 10 mg
RGD peptide (GRGDNP) (TFA)Cat. No.: HY-P1740A
RGD peptide (GRGDNP) (TFA) acts as an inhibitor ofintegrin-ligand interactions and plays animportant role in cell adhesion, migration,growth, and differentiation.
Purity: 98.80%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 1 mg, 5 mg
RGD peptide GRGDNPCat. No.: HY-P1740
RGD peptide (GRGDNP) acts as an inhibitor ofintegrin-ligand interactions and plays animportant role in cell adhesion, migration,growth, and differentiation.
Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg
RGD TrifluoroacetateCat. No.: HY-P0278A
RGD Trifluoroacetate is a tripeptide thateffectively triggers cell adhesion, addressescertain cell lines and elicits specific cellresponses; RGD Trifluoroacetate binds to .integrins
Purity: >98.0%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg
14 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]
RisuteganibCat. No.: HY-P1930
Risuteganib is an anti-integrin that downregulatesoxidative stress and restores homeostasis, andtargets three integrin receptors that areimplicated in dry age-related macular degeneration(AMD) in order to restore homeostasis in theretina .
Purity: >98%Clinical Data: No Development ReportedSize: 100 mg
RWJ 50271Cat. No.: HY-110086
RWJ 50271 is an selective inhibitor oflymphocyte function-associatedantigen-1/intercellular adhesion
interaction with anmolecule-1(LFA-1/ICAM-1) of 5.0 μM (HL60 cells).IC50
Purity: >99.0%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg
SR121566ACat. No.: HY-U00235
SR121566A is a novel non-peptide Glycoprotein ( ) antagonist, which canIIb/IIIa GP IIb-IIIa
inhibit ADP-, arachidonic acid- andcollagen-induced human platelet aggregation with
s of 46±7.5, 56±6 and 42±3 nM, respectively.IC50
Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg, 20 mg
TCS 2314Cat. No.: HY-12308
TCS 2314 (compound 3) is orally active andselective very late antigen-4 (VLA-4, α4β1,
antagonist with an of 4.4 nM.CD49d/CD29) IC50
Purity: >99.0%Clinical Data: No Development ReportedSize: 5 mg
Tirofiban (L700462; MK383) Cat. No.: HY-17369B
Tirofiban(L700462;MK383) is a potent non-peptide,glycoprotein IIb/IIIa (integrins alphaIIbbetaIII)antagonist Target: integrin IIb/IIIa Tirofibanhydrochloride monohydrate blocks plateletaggregation and thrombus formation.
Purity: >98%Clinical Data: LaunchedSize: 5 mg, 10 mg
Tirofiban hydrochloride monohydrateCat. No.: HY-17369
Tirofiban hydrochloride monohydrate is a potentnon-peptide, glycoprotein IIb/IIIa (integrinsalphaIIbbetaIII) antagonist IC50 value: Target:integrin IIb/IIIa Tirofiban hydrochloridemonohydrate blocks platelet aggregation andthrombus formation.
Purity: 99.99%Clinical Data: LaunchedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg
TR-14035Cat. No.: HY-15770
TR-14035 is a a dual alpha4beta7(IC50=7nM)/alpha4beta1 (IC50=87 nM) integrin antagonist .
Purity: 95.14%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg
Vedolizumab (Anti-Human lymphocyte α4β7 integrin, Humanized Antibody) Cat. No.: HY-P9911
Vedolizumab is a humanized monoclonal antibodythat targets the α4β7 for the treatment ofintegrinulcerative colitis and Crohn's disease.
Purity: 99.64%Clinical Data: LaunchedSize: 1 mg, 5 mg
Zaurategrast (CT7758) Cat. No.: HY-70073
Zaurategrast (CT7758) is a potent andoral-effective inhibitor.α -integrin4
Purity: 98.81%Clinical Data: Phase 2Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg
Zaurategrast ethyl ester (CDP323; UCB1184197) Cat. No.: HY-75385
Zaurategrast ethyl ester (CDP323), the ethyl esterprodrug of CT7758, is a / integrinα4β1 α4β7antagonist used for the treatment of inflammatoryand autoimmune disorders.
Purity: 99.06%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg
www.MedChemExpress.com 15
Zaurategrast ethyl ester sulfate (CDP323 sulfate; UCB1184197 sulfate) Cat. No.: HY-75385A
Zaurategrast ethyl ester sulfate (CDP323 sulfate),the ethyl ester prodrug of CT7758, is a
/ integrin antagonist used for theα4β1 α4β7treatment of inflammatory and autoimmunedisorders.
Purity: >98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg
α2β1 Integrin Ligand PeptideCat. No.: HY-P1868
α2β1 Integrin Ligand Peptide interacts with theα2β1 integrin receptor on the cell membrane andmediates extracellular signals into cells. It is apotential antagonist of collagen receptors.
Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg
α2β1 Integrin Ligand Peptide (TFA)Cat. No.: HY-P1868A
α2β1 Integrin Ligand Peptide TFA interacts withthe α2β1 integrin receptor on the cell membraneand mediates extracellular signals into cells. Itis a potential antagonist of collagen receptors.
Purity: 99.33%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg
αvβ1 integrin-IN-1Cat. No.: HY-100445
αvβ1 integrin-IN-1 (Compound C8) is a potent andselective inhibitor with an ofαvβ1 integrin IC50
0.63 nM. Antifibrotic effects.
Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg
16 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]
Kinesin
Kinesin is a protein belonging to a class of motor proteins found in eukaryotic cells. Kinesins move along microtubule filaments,and are powered by the hydrolysis of ATP (thus kinesins are ATPases). The active movement of kinesins supports several cellularfunctions including mitosis, meiosis and transport of cellular cargo. Most kinesins walk towards the plus end of a microtubule,entails transporting cargo from the centre of the cell towards the periphery. Kinesins were discovered as microtubule (MT)-basedanterograde intracellular transport motors. The founding member of this superfamily, the genomes of mammals encode more than40 kinesin proteins, organized into at least 14 families named kinesin-1 through kinesin-14.
www.MedChemExpress.com 17
Kinesin Inhibitors
(R)-Filanesib ((R)-ARRY-520) Cat. No.: HY-15187A
(R)-Filanesib ((R)-ARRY-520) is the R-enantiomerof ARRY-520. (R)-Filanesib ((R)-ARRY-520) is asynthetic inhibitorkinesin spindle protein (KSP)with of 6 nM.IC50
Purity: 98.86%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg
AZ82Cat. No.: HY-12241
AZ82 is a selective kinesin-like protein KIFC1 inhibitor, with a of 43 nM and an(HSET/KIFC1) Ki
of 300 nM for KIFC1.IC50
Purity: 99.08%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg
CW-069Cat. No.: HY-15857
CW-069 is an allosteric inhibitor of with an ofmicrotubule motor protein HSET IC50
75 μM.
Purity: 99.75%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg
DimethylenastronCat. No.: HY-19944
Dimethylenastron is a potent kinesin Eg5inhibitor, with an of 200 nM.IC50
Purity: 98.24%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg
Eg5 Inhibitor V, trans-24Cat. No.: HY-112915
Eg5 Inhibitor V, trans-24 is a potent and specific inhibitor with an of 0.65 μM, andkinesin Eg5 IC50
can be used in the research of cancer.
Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg
EMD534085Cat. No.: HY-15000
EMD534085 is a potent and selective inhibitor ofthe mitotic with an of 8 nM.kinesin-5 IC50
Purity: 99.03%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg
Filanesib (ARRY-520) Cat. No.: HY-15187
Filanesib (ARRY-520) is a synthetic kinesin spindle inhibitor with of 6 nM.protein (KSP) IC50
Purity: 99.73%Clinical Data: Phase 2Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg
GSK-923295Cat. No.: HY-10299
GSK-923295 is a special, allosteric inhibitor ofcentromere-associated protein-E (CENP-E)kinesin motor ATPase activity, with of 3.2±0.2Ki
nM and 1.6± 0.1 nM for human and canine,respectively.
Purity: 99.56%Clinical Data: Phase 1Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg
Ispinesib (SB-715992) Cat. No.: HY-50759
Ispinesib is a specific inhibitor of kinesin, with a of 1.7 nM.spindle protein (KSP) Ki app
Purity: 99.83%Clinical Data: Phase 2Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg
K858 (Racemic)Cat. No.: HY-19966
K858 Racemic is an ATP-uncompetitive inhibitor of with an of 1.3 μM.kinesin Eg5 IC50
Purity: 99.93%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg
18 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]
Kif15-IN-1Cat. No.: HY-15948
Kif15-IN-1 is an inhibitor of the mitotic Kinesin, and is used for thefamily member 15 (Kif15)
research of cellular proliferative diseases.
Purity: 99.53%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg
Kif15-IN-2Cat. No.: HY-15949
Kif15-IN-2 is an inhibitor of the mitotic kinesin, and is used for the research of cellularKif15
proliferative diseases.
Purity: 98.18%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg
Litronesib (LY-2523355; KF-89617) Cat. No.: HY-14846
Litronesib is a selective mitosis-specific kinesin inhibitor, with antitumor activity.Eg5
Purity: 99.59%Clinical Data: Phase 2Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg
Litronesib Racemate (LY-2523355 Racemate; KF-89617 Racemate) Cat. No.: HY-14846A
Litronesib (Racemate) is the racemate oflitronesib. Litronesib is a selective, allostericinhibitor of .kinesin Eg5
Purity: 99.20%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 2 mg, 5 mg
Monastrol ((±)-Monastrol) Cat. No.: HY-101071A
Monastrol is a potent and cell-permeable inhibitorof the mitotic with an value ofkinesin Eg5 IC50
14 μM.
Purity: 99.95%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg
PaprotrainCat. No.: HY-101298
Paprotrain is a cell-permeable inhibitor of the, inhibits the ATPase activity ofkinesin MKLP-2
MKLP-2 with an of 1.35 μM and a of 3.36 μMIC50 Ki
and shows a moderate inhibition activity on with an of 5.5 μM.DYRK1A IC50
Purity: 97.05%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg
PF-2771Cat. No.: HY-19530
PF-2771 is a potent and selective centromere inhibitor, inhibiting CENP-Eprotein E (CENP-E)
motor activity with an of 16.1 nM; PF-2771 isIC50
used as an anticancer agent.
Purity: 99.56%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg
SB-743921Cat. No.: HY-12069
SB-743921 is a potent inhibitor of the mitotic, with a of 0.1 nM.kinesin KSP (Eg5) Ki
Purity: 97.31%Clinical Data: Phase 2Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg
www.MedChemExpress.com 19
Microtubule/Tubulin
Microtubules are a component of the cytoskeleton, found throughout the cytoplasm. These tubular polymers of tubulin can growas long as 50 micrometres, with an average length of 25 µm, and are highly dynamic. The outer diameter of a microtubule is about24 nm while the inner diameter is about 12 nm. Microtubules are found in eukaryotic cells and are formed by the polymerization ofa dimer of two globular proteins, alpha and beta tubulin. Tubulin is one of several members of a small family of globular proteins.The tubulin superfamily includes five distinct families, the alpha-, beta-, gamma-, delta-, and epsilon-tubulins and a sixth familywhich is present only in kinetoplastid protozoa. The most common members of the tubulin family are α-tubulin and β-tubulin, theproteins that make up microtubules. Microtubules are very important in a number of cellular processes. They are involved inmaintaining the structure of the cell.
20 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]
Microtubule/Tubulin Inhibitors & Modulators
10-Deacetyl-7-xylosyl paclitaxel (10-Deacetyl-7-xylosyltaxol;
10-Deacetylpaclitaxel 7-Xyloside; …) Cat. No.: HY-20584
10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel(a microtubule stabilizing agent; enhances tubulinpolymerization) derivative with improvedpharmacological features.
Purity: >98%Clinical Data: No Development ReportedSize: 10 mg, 50 mg
10-Deacetyltaxol (10-Deacetylpaclitaxel) Cat. No.: HY-N1391
10-Deacetyltaxol (10-Deacetylpaclitaxel) is ataxane derivative isolated from Taxus
Zucc.wallichiana
Purity: >98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 20 mg
10-Oxo Docetaxel (Docetaxel Impurity 1) Cat. No.: HY-16674
10-Oxo Docetaxel (Docetaxel Impurity 1) is a noveltaxoid having remarkable anti-tumor properties anda Docetaxel intermediate.
Purity: 93.89%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg
2-Methoxyestradiol (2-ME2; NSC-659853) Cat. No.: HY-12033
2-Methoxyestradiol (2-ME2), an orally activeendogenous metabolite of 17β-estradiol (E2), is an
inducer and an inhibitor withapoptosis angiogenesispotent antineoplastic activity. 2-Methoxyestradiolalso destablize .microtubules
Purity: 99.82%Clinical Data: Phase 2Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg
4'-Demethylepipodophyllotoxin (4'-O-demethylepipodophyllotoxin; 4'-DMEP) Cat. No.: HY-17435
4'-Demethylepipodophyllotoxin(4'-DMEP) is a keyintermediate compound for the preparation ofpodophyllotoxin-type anti-cancer drugs; a potentinhibitor of microtubule assembly.
Purity: 99.20%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 50 mg, 100 mg
7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) Cat. No.: HY-16675
7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) is aimpurity of docetaxel detected by high performanceliquid chromatography (HPLC).
Purity: >98.0%Clinical Data: No Development ReportedSize: 1 mg, 5 mg
7-Epi-docetaxel (4-epi-Docetaxel; 7-Epidocetaxel; 7-Epitaxotere) Cat. No.: HY-16676
7-Epi-10-oxo-docetaxel (Docetaxel Impurity C;7-Epitaxotere) is a impurity of docetaxel.
Purity: 99.22%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 1 mg, 10 mg
7-epi-Taxol (7-epi-Paclitaxel) Cat. No.: HY-N0227
7-epi-Taxol is an active metabolite of taxol, withactivity comparable to that of taxol against cellreplication, promoting bundlemicrotubuleformation and against microtubuledepolymerization.
Purity: 99.75%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg
7-xylosyltaxol (7-Xylosylpaclitaxel; Taxol-7-xyloside) Cat. No.: HY-77574
7-xylosyltaxol(Taxol-7-xyloside) is a taxol(Paclitaxel) derivative; Paclitaxel binds totubulin and inhibits the disassembly ofmicrotubules.
Purity: >98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg
ABT-751 (E7010) Cat. No.: HY-13270
ABT-751(E 7010) is a novel bioavailabletubulin-binding and antimitotic sulfonamide agentwith IC50 of about 1.5 and 3.4 μM in neuroblastomaand non-neuroblastoma cell lines, respectively.
Purity: 99.87%Clinical Data: Phase 2Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg
www.MedChemExpress.com 21
AcLys-PABC-VC-Aur0101Cat. No.: HY-111554
AcLys-PABC-VC-Aur0101 is a drug-linker conjugate (anti-CXCR4 ADC) with potent antitumorfor ADC
activity by using Aur0101 (an auristatinmicrotubule inhibitor), linked via the cleavablelinker AcLys-PABC-VC.
Purity: >98%Clinical Data: No Development ReportedSize: 100 mg, 250 mg, 500 mg
AmPEG6C2-Aur0131Cat. No.: HY-111555
AmPEG6C2-Aur0131 is a drug-linker conjugate for (anti-CXCR4 ADC) with potent antitumorADC
activity by using Aur0131 (an auristatinmicrotubule inhibitor), linked via thenon-cleavable linker AmPEG6C2.
Purity: >98%Clinical Data: No Development ReportedSize: 100 mg, 250 mg, 500 mg
Amphethinile (Amphetinile; CRC 82-07) Cat. No.: HY-100190
Amphethinile is an agent. The affinityanti-tubulinconstant for the association ( ) ofKa
Amphethinile with tubulin is 1.3 μM.
Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg
Ansamitocin P 3' (Antibiotic C 15003P3'; Maytansinol butyrate) Cat. No.: HY-19839
Ansamitocin P 3' exhibits antitumour activity, isan antibody drug conjugate cytotoxin. The moreinformation please refer to Ansamitocin P-3(HY-15739, a tubulin inhibitor).
Purity: 87.63%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 2 mg, 5 mg, 10 mg, 25 mg, 50 mg
Ansamitocin P-3 (Antibiotic C 15003P3; Maytansinol isobutyrate) Cat. No.: HY-15739
Ansamitocin P-3 (Antibiotic C 15003P3) is a inhibitor. Ansamitocin P-3 is amicrotubule
macrocyclic antitumor antibiotic.
Purity: >98.0%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg
Auristatin ECat. No.: HY-15582
Auristatin E is a cytotoxic tubulin modifier withpotent and selective antitumor activity; MMAEanalog and cytotoxin in Antibody-drug conjugates.Auristatin E inhibits cell division by blockingthe polymerisation of tubulin.
Purity: 99.36%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg
Auristatin FCat. No.: HY-15583
Auristatin F is a cytotoxic tubulin modifier withpotent and selective antitumor activity; MMAFanalog and cytotoxin in Antibody-drug conjugates.Auristatin F inhibits cell division by blockingthe polymerisation of tubulin.
Purity: 97.51%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg
BNC105Cat. No.: HY-16114
BNC105 is a tubulin polymerization inhibitor withpotent antiproliferative and tumor vasculardisrupting properties.
Purity: 99.49%Clinical Data: Phase 2Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg
BTB-1Cat. No.: HY-101770
BTB-1 is a potent, selective and reversiblemitotic motor protein inhibitor with an Kif18A IC50
of 1.69 μM.
Purity: 99.62%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg
Cabazitaxel (XRP6258; RPR-116258A; taxoid XRP6258) Cat. No.: HY-15459
Cabazitaxel is a semi-synthetic derivative of thenatural taxoid 10-deacetylbaccatin III withpotential antineoplastic activity.
Purity: 99.96%Clinical Data: LaunchedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg
22 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]
CCB02Cat. No.: HY-114302
CCB02 is a selective CPAP-tubulin interactioninhibitor, binding to tubulin and competing forthe CPAP binding site of β-tubulin, with an IC50
of 689 nM, and shows potent anti-tumor activity.
Purity: 99.77%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg
CephalomannineCat. No.: HY-77554
Cephalomannine is a taxol derivative withantitumor, antiproliferative properties.
Purity: 99.29%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg
Ceratamine ACat. No.: HY-N6997
Ceratamine A is an antimitotic heterocyclicalkaloid isolated from the marine sponge
, acts as aPseudoceratina sp.microtubule-stabilizing agent. Ceratamine Aexhibits cytotoxicity against human cancer celllines.
Purity: >98%Clinical Data: No Development ReportedSize: 100 mg, 250 mg, 500 mg
Cevipabulin (TTI-237) Cat. No.: HY-14949
Cevipabulin (TTI-237) is an oral,microtubule-active antitumor compound and inhibitsthe binding of [ H] vinblastine to tubulin, with3
an of 18-40 nM for cytotoxicity in humanIC50
tumor cell line.
Purity: 99.03%Clinical Data: Phase 1Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg
Cevipabulin fumarate (TTI-237 fumarate) Cat. No.: HY-14949C
Cevipabulin fumarate (TTI-237 fumarate) is anoral, microtubule-active, antitumor compound andinhibits the binding of [ H]NSC 49842 to tubulin,3
with an of 18-40 nM for cytotoxicity in humanIC50
tumor cell line.
Purity: 99.08%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg
ColchicineCat. No.: HY-16569
Colchicine is a inhibitor and atubulin disrupting agent. Colchicinemicrotubule
inhibits microtubule polymerization with an IC50
of 3 nM.
Purity: 99.98%Clinical Data: LaunchedSize: 10 mM × 1 mL, 200 mg, 500 mg
Combretastatin A4 (CRC 87-09) Cat. No.: HY-N2146
Combretastatin A4 is a -targetingmicrotubuleagent that binds with of 0.4 μM.β-tubulin Kd
Purity: 99.41%Clinical Data: Phase 1Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg
Crolibulin (EPC2407) Cat. No.: HY-13603
Crolibulin is a small molecule tubulin inhibitor.polymerization
Purity: 98.04%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg
Cys-mcMMADCat. No.: HY-15750
Cys-mcMMAD is a drug-linker conjugate for ADC.MMAD is a potent tubulin inhibitor.
Purity: >98%Clinical Data: No Development ReportedSize: 1 mg
D-64131Cat. No.: HY-15482
D-64131 is a novel inhibitor of Tubulinpolymerization that competitively binds with[(3)H]colchicine to αβ-Tubulin.
Purity: 99.42%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 10 mg, 50 mg
www.MedChemExpress.com 23
D8-MMAD (Demethyldolastatin 10 D8; Monomethylauristatin D D8;
Monomethyl Dolastatin 10 D8) Cat. No.: HY-15581S
D8-MMAD is a deuterated form of MMAD, which is a disrupting agent.microtubule
Purity: >98.0%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg
D8-MMAE (D8-Monomethyl auristatin E) Cat. No.: HY-15162A
D8-MMAE is a deuterated labeled MMAE, a potent inhibitor and a tubulin inhibitor.mitotic
Purity: 99.29%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg
D8-MMAF (Monomethylauristatin F D8) Cat. No.: HY-15579S
D8-MMAF is a deuterated form of MMAF, which is a disrupting agent.microtubule
Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg
D8-MMAF hydrochlorideCat. No.: HY-15579AS
D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride, which is a microtubuledisrupting agent.
Purity: 99.56%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg
DeoxypodophyllotoxinCat. No.: HY-N2500
Deoxypodophyllotoxin (DPT), a derivative ofpodophyllotoxin, is a lignan with potentantimitotic, anti-inflammatory and antiviralproperties isolated from rhizomes of
(Berberidaceae).Sinopodophullumhexandrum
Purity: >98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg
DM3 (Maytansinoid DM3) Cat. No.: HY-130080
DM3 (Maytansinoid DM3) is a maytansine analogbearing disulfide or thiol groups and a tubulininhibitor, and is a cytotoxic moiety of
.antibody-drug conjugates (ADCs)
Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg
DM3-SMeCat. No.: HY-130081
DM3-SMe is a maytansine derivative and a tubulininhibitor, and is a cytotoxic moiety of
, which can beantibody-drug conjugates (ADCs)linked to antibody through disulfide bond orstable thioether bond.
Purity: >98%Clinical Data: No Development ReportedSize: 100 mg
DM4Cat. No.: HY-12454
DM4 is is an agent that inhibit cellantitubulindivision. DM4 can be used in the preparation ofantibody drug conjugate.
Purity: 98.28%Clinical Data: Phase 2Size: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg
DM4-SMeCat. No.: HY-130082
DM4-SMe is a metabolite of antibody-maytansin and a inhibitor, andconjugates (AMCs) tubulin
also a cytotoxic moiety of antibody-drug conjugates, which can be linked to antibody through(ADCs)
disulfide bond or stable thioether bond. DM4-SMeinhibits KB cells with an of 0.026 nM.IC50
Purity: >98%Clinical Data: No Development ReportedSize: 45 mg, 100 mg
DM4-SPDPCat. No.: HY-126493
DM4-SPDP is a drug-linker conjugate composed of apotent antitubulin agent DM4 and a linker SMCC tomake antibody drug conjugate.
Purity: >98%Clinical Data: No Development ReportedSize: 10 mg, 25 mg, 50 mg
24 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]
Docetaxel (RP-56976) Cat. No.: HY-B0011
Docetaxel is an antineoplastic drug by inhibiting depolymerization, and attenuatingmicrotubule
of the effects of and gene expression.bcl-2 bcl-xL
Purity: 99.96%Clinical Data: LaunchedSize: 10 mM × 1 mL, 100 mg, 200 mg
Docetaxel Trihydrate (RP-56976 (Trihydrate)) Cat. No.: HY-B0011A
Docetaxel Trihydrate is a semi-synthetic taxaneanalogue, acts as a stabilizer.microtubule
Purity: 99.86%Clinical Data: LaunchedSize: 10 mM × 1 mL, 100 mg, 200 mg
Dolastatin 10 (DLS 10; NSC 376128) Cat. No.: HY-15580
Dolastatin 10 (DLS 10) is a potent antimitoticpeptide, isolated from the marine mollusk Dolabela
, that inhibits polymerization.auricularia tubulin
Purity: 98.52%Clinical Data: Phase 2Size: 1 mg, 5 mg
ELR510444Cat. No.: HY-16191
ELR510444 is a novel microtubule disruptor;inhibits MDA-MB-231 cell proliferation with IC50of 30.9 nM; not a substrate for the P-glycoproteindrug transporter and retains activity inβIII-tubulin-overexpressing cell lines.
Purity: 95.55%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg
EntasobulinCat. No.: HY-16777
Entasobulin is a polymerization inhibitorβ-tubulinwith potential anticancer activity.
Purity: 98.04%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg, 20 mg
Epothilone A (Epo A) Cat. No.: HY-13503
Epothilone A is a competitive inhibitor of thebinding of [ H] paclitaxel to polymers,3 tubulinwith a of 0.6-1.4 μM.Ki
Purity: 99.75%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg, 25 mg
Epothilone B (EPO 906; Patupilone) Cat. No.: HY-17029
Epothilone B is a stabilizer with amicrotubule of 0.71μM. It acts by binding to the αβ-tubulinKi
heterodimer subunit which causes decreasing ofαβ-tubulin dissociation.
Purity: 99.88%Clinical Data: Phase 3Size: 10 mM × 1 mL, 2 mg, 5 mg, 10 mg, 50 mg
Epothilone D (KOS 862) Cat. No.: HY-15278
Epothilone D (KOS 862) is a potent microtubulestabilizer.
Purity: 99.93%Clinical Data: Phase 2Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg
Eribulin (B1939; E7389; ER-086526) Cat. No.: HY-13442
Eribulin (E7389) is a targetingmicrotubuleagent that is used in the treatment of metastaticbreast cancer. Eribulin (E7389) inhibits theproliferation of cancer cells by bindingmicrotubule proteins and microtubules.
Purity: >98%Clinical Data: LaunchedSize: 1 mg
Eribulin mesylate (B1939 mesylate; E7389 mesylate; ER-086526 mesylate) Cat. No.: HY-13442A
Eribulin mesylate (E7389 mesylate) is a targeting agent that is used in themicrotubule
treatment of metastatic breast cancer. Eribulinmesylate (E7389 mesylate) inhibits theproliferation of cancer cells by bindingmicrotubule proteins and microtubules.
Purity: 99.52%Clinical Data: LaunchedSize: 500 μg, 1 mg
www.MedChemExpress.com 25
Estramustine phosphate sodiumCat. No.: HY-13627
Estramustine phosphate sodium is anantimicrotubule chemotherapy agent; arrestsprostate cancer cells in the G2/M phase of thecell cycle.
Purity: 99.84%Clinical Data: LaunchedSize: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg
FlubendazoleCat. No.: HY-B0294
Flubendazole is a safe and efficaciousanthelmintic drug, which is widely used foranthelmintic to human, rodents and ruminants.Flubendazole exerts anticancer activities bymechanisms including inhibition of microtubulefunction.
Purity: 99.09%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 100 mg, 500 mg
Fosbretabulin disodium (CA 4DP; CA 4P; Combretastatin A4 disodium phosphate) Cat. No.: HY-17449
Fosbretabulin disodium(CA 4DP; CA 4P) is amicrotubule destabilizing drug, a type ofvascular-targeting agent, a drug designed todamage the vasculature (blood vessels) of cancertumors causing central necrosis.
Purity: 99.47%Clinical Data: Phase 3Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg
Indibulin (ZIO 301; D 24851) Cat. No.: HY-13649
Indibulin (ZIO 301), an orally applicableinhibitor of assembly, shows potenttubulinanticancer activity with a minimal neurotoxicity.
Purity: >98%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg
Ixabepilone (Azaepothilone B; BMS 247550; BMS 247550-1) Cat. No.: HY-10222
Ixabepilone is an orallybioavailable inhibitor,microtubulewhich binds to tubulin and promotes tubulinpolymerization and microtubule stabilization,thereby arrests cells in the G2-M phase of thecell cycle and induces tumor cell apoptosis.
Purity: 99.93%Clinical Data: LaunchedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg
Lexibulin (CYT-997) Cat. No.: HY-10498
Lexibulin(CYT-997) is a potent tubulinpolymerisation inhibitor with IC50 of 10-100 nM incancer cell lines; with potent cytotoxic andvascular disrupting activity in vitro and in vivo.
Purity: 99.46%Clinical Data: Phase 2Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg
Lexibulin dihydrochloride (CYT-997 dihydrochloride) Cat. No.: HY-10498A
Lexibulin 2Hcl (CYT-997 2Hcl) is a potent tubulinpolymerisation inhibitor with IC50 of 10-100 nM incancer cell lines; with potent cytotoxic andvascular disrupting activity in vitro and in vivo.
Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg
Maytansinol (Ansamitocin P-0) Cat. No.: HY-19474
Maytansinol inhibits microtubule assembly andinduces microtubule disassembly in vitro. Target:Microtubule/Tubulin in vitro: Maytansinol disruptsthe mitotic spindle and prevents mitotic exit inDrosophila.
Purity: 99.04%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg
MC-Alkyl-Hydrazine Modified MMAFCat. No.: HY-128961
MC-Alkyl-Hydrazine Modified MMAF is a drug-linker with potent antitumor activityconjugate for ADC
by using the Modified MMAF (a tubulin inhibitor),linked via the noncleavable MC-Alkyl-Hydrazine.
Purity: >98%Clinical Data:Size: 100 mg, 250 mg, 500 mg
Mc-MMADCat. No.: HY-15740
Mc-MMAD is a protective group(maleimidocaproyl)-conjugated MMAD. MMAD is apotent tubulin inhibitor. Mc-MMAD is a drug-linkerconjugate for ADC.
Purity: 98.50%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg
26 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]
Mc-MMAE (Maleimidocaproyl-monomethylauristatin E) Cat. No.: HY-15741
Mc-MMAE is a protective group(maleimidocaproyl)-conjugated monomethylauristatin E (MMAE), which is a potent tubulininhibitor. Mc-MMAE is a drug-linker conjugate forADC.
Purity: 96.47%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg
MC-Val-Cit-PAB-MMAFCat. No.: HY-112786
MC-Val-Cit-PAB-MMAF is a drug-linker conjugate for with antitumor activity by using the tubulinADC
inhibitor, MMAF, linked via cathepsin cleavableMC-Val-Cit-PAB.
Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg
McMMAF (Maleimidocaproyl monomethylauristatin F) Cat. No.: HY-15578
McMMAF is a protective group-conjugated MMAF. MMAFis a potent tubulin polymerization inhibitor.
Purity: 99.94%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg
Mertansine (DM1; Maytansinoid DM1) Cat. No.: HY-19792
Mertansine (DM1) is a inhibitormicrotubulinand is an antibody-conjugatable maytansinoid thatis developed to overcome systemic toxicityassociated with maytansine and to enhancetumor-specific delivery.
Purity: 98.74%Clinical Data: Phase 2Size: 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg
Microtubule inhibitor 1Cat. No.: HY-114313
Microtubule inhibitor 1 is an antitumor agent with inhibitorymicrotubule polymerization
activity, with an value of 9-16 nM in cancerIC50
cells.
Purity: >98%Clinical Data: No Development ReportedSize: 100 mg, 250 mg, 500 mg
Mivobulin (NSC 613862; (S)-(-)-NSC 613862) Cat. No.: HY-106423
Mivobulin (NSC 613862) is a inhibitor,tubulinbinds to tubulin in the region that overlaps thecolchicine site, and inhibits tubulinpolymerization. Mivobulin (NSC 613862) promotesthe formation of abnormal polymers and a GTPaseactivity in the tubulin dimer.
Purity: >98%Clinical Data: No Development ReportedSize: 100 mg, 250 mg, 500 mg
MMAD (Demethyldolastatin 10; Monomethylauristatin D;
Monomethyl Dolastatin 10) Cat. No.: HY-15581
MMAD is a potent inhibitor, is a toxintubulinpayload in antibody drug conjugates ( ).ADCs
Purity: 99.92%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg
MMAF (Monomethylauristatin F) Cat. No.: HY-15579
MMAF (Monomethylauristatin F) is a potent tubulin inhibitor and is used as apolymerization
antitumor agent. MMAF (Monomethylauristatin F) iswidely used as a cytotoxic component ofantibody-drug conjugates ( s) such asADCvorsetuzumab mafodotin and SGN-CD19A.
Purity: >98%Clinical Data: No Development ReportedSize: 2 mg, 5 mg, 10 mg
MMAF Hydrochloride (Monomethylauristatin F Hydrochloride) Cat. No.: HY-15579A
MMAF Hydrochloride (Monomethylauristatin FHydrochloride) is a potent tubulin
inhibitor and is used as apolymerizationantitumor agent.
Purity: 99.89%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 2 mg, 5 mg, 10 mg
MMAF sodium (Monomethylauristatin F sodium) Cat. No.: HY-15579B
MMAF sodium (Monomethylauristatin F sodium) is apotent inhibitor and istubulin polymerizationused as a antitumor agent.
Purity: 99.73%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 2 mg, 5 mg, 10 mg
www.MedChemExpress.com 27
Monomethyl auristatin E (MMAE; SGD-1010) Cat. No.: HY-15162
Monomethyl auristatin E (MMAE; SGD-1010) is asynthetic derivative of dolastatin 10 andfunctions as a potent inhibitor bymitoticinhibiting tubulin polymerization.
Purity: 99.94%Clinical Data: Phase 4Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg
MPT0B392Cat. No.: HY-101287
MPT0B392, an orally active quinoline derivative,induces activation,c-Jun N-terminal kinase (JNK) leading to .apoptosis
Purity: >98%Clinical Data: No Development ReportedSize: 100 mg, 250 mg, 500 mg
Nocodazole (Oncodazole; R17934) Cat. No.: HY-13520
Nocodazole is a rapidly-reversible inhibitor of. Nocodazole binds to β-tubulin andmicrotubule
disrupts microtubule assembly/disassemblydynamics, which prevents mitosis and inducesapoptosis in tumor cells. Nocodazole inhibits
, and activates .Bcr-Abl CRISPR/Cas9
Purity: 98.68%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg
Ombrabulin (AVE8062; AC7700) Cat. No.: HY-14797
Ombrabulin (AVE8062) is a derivative of CA-4phosphate, which is known to exhibit antivasculareffects through selective disruption of the tubulincytoskeleton of endothelial cells.
Purity: >98%Clinical Data: Phase 3Size: 1 mg, 5 mg, 10 mg, 20 mg
Ombrabulin hydrochloride (AVE8062 (hydrochloride); AC7700 (hydrochloride)) Cat. No.: HY-18256
Ombrabulin hydrochloride is a derivative of CA-4phosphate, which is known to exhibit antivasculareffects through selective disruption of the tubulincytoskeleton of endothelial cells.
Purity: 99.84%Clinical Data: Phase 3Size: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg
OSIP-486823 (OSIP 486823; OSIP486823; CP248) Cat. No.: HY-U00004
OSIP-486823 is a novel -interferingmicrotubuleagent with distinct biological effects on bothprotein kinase G (PKG) and microtubules.
Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg, 20 mg
Paclitaxel (Taxol) Cat. No.: HY-B0015
Paclitaxel (Taxol), a naturally occurringantineoplastic agent, stabilizes tubulin
, resulting in arrest at the G2/Mpolymerizationphase of the cell cycle and apoptotic cell death.
Purity: 99.97%Clinical Data: LaunchedSize: 10 mM × 1 mL, 50 mg, 100 mg, 500 mg
Parbendazole (SKF 29044) Cat. No.: HY-115364
Parbendazole is a potent inhibitor of assembly, destabilizes tubulin,microtubule
with an of 8.79nM, and exhibits aEC50
broad-spectrum anthelmintic activity.
Purity: >98.0%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 10 mg, 25 mg, 50 mg, 100 mg
PBOX 6Cat. No.: HY-U00446
PBOX 6 is a pyrrolo-1,5-benzoxazepine (PBOX)compound, acts as a -depolymerizingmicrotubuleagent and an apoptotic agent.
Purity: >98.0%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg
PE859Cat. No.: HY-12662
PE859 is a potent inhibitor of both and tau Aβaggregation with values of 0.66 and 1.2 μM,IC50
respectively.
Purity: 98.01%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg
28 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]
PEG4-aminooxy-MMAFCat. No.: HY-128968
PEG4-aminooxy-MMAF is a drug-linker conjugate for with potent antitumor activity by using theADC
potent antitubulin agent MMAF, linked via thenoncleavable PEG4.
Purity: >98%Clinical Data:Size: 100 mg, 250 mg, 500 mg
PF-06380101 (Aur0101; Auristatin-0101) Cat. No.: HY-12522
PF-06380101 (Aur0101), an auristatin inhibitor, is a cytotoxicmicrotubule
Dolastatin 10 analogue.
Purity: 99.62%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg
PironetinCat. No.: HY-116446
Pironetin is an α/β unsaturated lactone isolatedfrom species. Pironetin binds toStreptomyces
and is a potent inhibitor ofα-tubulin polymerization, and has cell cyclemicrotubule
arrest and antitumor activity.
Purity: >98%Clinical Data: No Development ReportedSize: 1 mg
Plinabulin (NPI-2358) Cat. No.: HY-14444
Plinabulin (NPI-2358) is a vascular disruptingagen ( ) against withVDA tubulin-depolymerizingan of 9.8 nM against HT-29 cells. PlinabulinIC50
binds the colchicine binding site of β-tubulinpreventing polymerization and has potentinhibitory to tumor cells.
Purity: >98.0%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg
Podofilox (Podophyllotoxin) Cat. No.: HY-15552
Podofilox (Podophyllotoxin) is a potent inhibitorof microtubule assembly and DNA topoisomerase II.
Purity: 99.79%Clinical Data: LaunchedSize: 10 mM × 1 mL, 100 mg, 500 mg
Rosabulin (STA 5312) Cat. No.: HY-14934
Rosabulin is a potent inhibitor,microtubulewith anti-cancer activities.
Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg, 20 mg
S516Cat. No.: HY-130233
S516 (Compound 22) is an active metabolite ofCKD-516 and a potent tubulin polymerizationinhibitor with an of 4.29 μM. S516 has markedIC50
antitumor activity.
Purity: >98%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg
Soblidotin (Auristatin PE; TZT-1027) Cat. No.: HY-14672
Soblidotin (Auristatin PE) is a novel syntheticDolastatin 10 derivative and inhibitor of tubulinpolymerization.
Purity: 99.76%Clinical Data: Phase 2Size: 1 mg, 5 mg, 10 mg, 25 mg, 50 mg
SS28Cat. No.: HY-100761
SS28, a SRT501 analog with oral bioavailability,inhibits to cause celltubulin polymerizationcycle arrest at G2/M phase. SS28 results inapoptosis rather than necrosis tubulin.
Purity: >98%Clinical Data: No Development ReportedSize: 100 mg, 250 mg, 500 mg
SSE15206Cat. No.: HY-111425
SSE15206 is a polymerizationmicrotubuleinhibitor (GI = 197 nM in HCT116 cells) that50
overcomes multidrug resistance. Causes aberrantmitosis resulting in G2/M arrest due to incompletespindle formation in cancer cells.
Purity: 99.74%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg
www.MedChemExpress.com 29
Taccalonolide ACat. No.: HY-N2416
Taccalonolide A is a microtubule stabilizer, whichis a steroid isolated from , withTacca chantriericytotoxic and antimalarial activities.Taccalonolide A causes G -M accumulation, Bcl-22
phosphorylation and initiation of apoptosis.
Purity: >98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg
Taccalonolide AJCat. No.: HY-N4208
Taccalonolide AJ is a semi-synthesis compound withcellular stabilizing activity.microtubuleTaccalonolide AJ exhibits high potencyantiproliferative activity against cancer cells,with an IC of 4.2 nM for HeLa cells.50
Purity: 99.38%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg
Taccalonolide BCat. No.: HY-N3028
Taccalonolide B is microtubule stabilizer isolatedfrom , with antitumor activity.Tacca plantagineaTaccalonolide B is effective in vitro against celllines that overexpress P-glycoprotein (Pgp) andmultidrug-resistance protein (MRP7).
Purity: >98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg
Taltobulin (HTI-286; SPA-110) Cat. No.: HY-15584
Taltobulin (HTI-286; SPA-110) is an analogue ofHemiasterlin; potent tubulin inhibitor; ADCscytotoxin. IC50 value: Target: tubulin in vitro:HTI-286 significantly inhibited proliferation ofall three hepatic tumor cell lines (mean IC50 = 2nmol/L +/- 1 nmol/L) in vitro.
Purity: 99.90%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg
Taltobulin hydrochloride (HTI-286 hydrochloride; SPA-110 hydrochloride) Cat. No.: HY-15584B
Taltobulin hydrochloride is an analogue ofHemiasterlin; potent tubulin inhibitor; ADCscytotoxin. IC50 value: Target: tubulin in vitro:HTI-286 significantly inhibits proliferation ofall three hepatic tumor cell lines (mean IC50 = 2nmol/L +/- 1 nmol/L).
Purity: 99.05%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg
Taltobulin trifluoroacetate (HTI-286 trifluoroacetate; SPA-110 trifluoroacetate) Cat. No.: HY-15584A
Taltobulin trifluoroacetate (HTI-286; SPA-110) isan analogue of Hemiasterlin; potent tubulininhibitor; ADCs cytotoxin.
Purity: 99.96%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg
Tasidotin hydrochloride (ILX651) Cat. No.: HY-13760
Tasidotin hydrochloride is a peptide analog of theantimitotic depsipeptide dolastatin 15, as aninhibitor of microtubule assembly and microtubuledynamics.
Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg, 20 mg
Tirbanibulin (KX2-391; KX-01) Cat. No.: HY-10340
Tirbanibulin (KX2-391) is an inhibitor of Srcthat targets the peptide substrate site of Src,with of 9-60 nM in cancer cell lines.GI50
Purity: >98%Clinical Data: Phase 2Size: 5 mg, 10 mg, 50 mg, 100 mg
Tirbanibulin dihydrochloride (KX2-391 (dihydrochloride); KX-01 (dihydrochloride)) Cat. No.: HY-10340A
Tirbanibulin (dihydrochloride) (KX2-391(dihydrochloride)) is an inhibitor of thatSrctargets the peptide substrate site of Src, with
of 9-60 nM in cancer cell lines.GI50
Purity: 96.24%Clinical Data: Phase 2Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg
Tirbanibulin Mesylate (KX2-391 Mesylate; KX01 Mesylate) Cat. No.: HY-10340B
Tirbanibulin Mesylate (KX2-391 Mesylate) is aninhibitor of that targets the peptideSrcsubstrate site of Src, with of 9-60 nM inGI50
cancer cell lines.
Purity: 99.88%Clinical Data: Phase 2Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg
30 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]
Triclabendazole (CGA89317) Cat. No.: HY-B0621
Triclabendazole(CGA89317) is a benzimidazole, itbinds to tubulin impairing intracellular transportmechanisms and interferes with protein synthesis.
Purity: 98.38%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 100 mg, 500 mg
Tubulin inhibitor 1Cat. No.: HY-112607
Tubulin inhibitor 1 is a inhibitor,tubulininhibits tubulin polymerization. Tubulin inhibitor1 shows potent anti-tumor activity, casuescellular mitotic arrest in the G2/M phase, andinduces cellular .apoptosis
Purity: 99.91%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg
TubulysinCat. No.: HY-128914
Tubulysin family of secondary metabolites areoriginally isolated from the myxobacteria
and Archangium geophyra Angiococcus.disciformis
Purity: >98%Clinical Data:Size: 100 mg, 250 mg, 500 mg
Tubulysin A (TubA) Cat. No.: HY-15995
Tubulysin A(TubA) is a myxobacterial product thatcan function as an antiangiogenic agent in many invitro assays; anti-microtubule, anti-mitotic, anapoptosis inducer, anticancer, anti-angiogenic,and antiproliferative.
Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg
Tubulysin BCat. No.: HY-N1243
Tubulysin B is a highly cytotoxic peptide andpotent destabilizing agentsmicrotubuleisolated from the myxobacteria Archangium
and .geophyra Angiococcus disciformis
Purity: >98%Clinical Data: No Development ReportedSize: 100 mg, 250 mg, 500 mg
Tubulysin CCat. No.: HY-N2347
Tubulysin C is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and .geophyra Angiococcus disciformis
Purity: >98%Clinical Data: No Development ReportedSize: 100 mg, 250 mg, 500 mg
Tubulysin DCat. No.: HY-N2348
Tubulysin D is one of the most potent derivativesamong the tubulysins isolated from themyxobacterial species andArchangium geophyra
.Angiococcus disciformis
Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg
Tubulysin ECat. No.: HY-N2346
Tubulysin E is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and .geophyra Angiococcus disciformis
Purity: >98%Clinical Data: No Development ReportedSize: 100 mg, 250 mg, 500 mg
Tubulysin FCat. No.: HY-N7049
Tubulysin F is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and .geophyra Angiococcus disciformis
Purity: >98%Clinical Data:Size: 100 mg, 250 mg, 500 mg
Tubulysin GCat. No.: HY-N7050
Tubulysin G is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and .geophyra Angiococcus disciformis
Purity: >98%Clinical Data:Size: 100 mg, 250 mg, 500 mg
www.MedChemExpress.com 31
Tubulysin HCat. No.: HY-N7051
Tubulysin H is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and .geophyra Angiococcus disciformis
Purity: >98%Clinical Data:Size: 100 mg, 250 mg, 500 mg
Tubulysin ICat. No.: HY-N7052
Tubulysin I is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and .geophyra Angiococcus disciformis
Purity: >98%Clinical Data:Size: 100 mg, 500 mg
Tubulysin MCat. No.: HY-N7053
Tubulysin M is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and .geophyra Angiococcus disciformis
Purity: >98%Clinical Data:Size: 25 mg, 50 mg, 100 mg
Valecobulin (CKD-516) Cat. No.: HY-13598
Valecobulin (CKD516) is a valine prodrug of (S516)and a vascular disrupting agent (VDA). Valecobulinis a potent inhibitorβ-tubulin polymerizationwith marked antitumor activity against murine andhuman solid tumors.
Purity: >98%Clinical Data: No Development ReportedSize: 100 mg, 250 mg, 500 mg
Valecobulin hydrochloride (CKD-516 hydrochloride) Cat. No.: HY-13598A
Valecobulin hydrochloride (CKD-516 hydrochloride)is a valine prodrug of S516 (HY-130233) and avascular disrupting agent (VDA). Valecobulinhydrochloride is a potent β-tubulin
inhibitor with marked antitumorpolymerizationactivity against murine and human solid tumors.
Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg
Vat-Cit-PAB-Monomethyl Dolastatin 10Cat. No.: HY-126492
Vat-Cit-PAB-Monomethyl Dolastatin 10 is a with potentdrug-linker conjugate for ADC
antitumor activity by using Monomethyl Dolastatin10 (a potent tubulin inhibitor), linked via theADC linker Vat-Cit-PAB.
Purity: >98%Clinical Data: No Development ReportedSize: 10 mg, 25 mg, 50 mg
Vc-MMADCat. No.: HY-15742
Vc-MMAD consists the ADCs linker (Val-Cit) andpotent tubulin inhibitor (MMAD). Vc-MMAD is adrug-linker conjugate for ADC.
Purity: >98%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg
VcMMAE (mc-vc-PAB-MMAE) Cat. No.: HY-15575
VcMMAE (mc-vc-PAB-MMAE) is a drug-linker conjugate with potent antitumor activity by usingfor ADC
the anti-mitotic agent, monomethyl auristatin E(MMAE, a tubulin inhibitor), linked via thelysosomally cleavable dipeptide, valine-citrulline(vc).
Purity: 99.89%Clinical Data: Phase 2Size: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg
VERU-111 (ABI-231) Cat. No.: HY-120599
VERU-111 (ABI-231) is a potent and orallybioavailable inhibitor, whichα and β tubulindisplays strong antiproliferative activity, withan average IC of 5.2 nM against panels of50
melanoma and prostate cancer cell lines.
Purity: >98%Clinical Data: No Development ReportedSize: 100 mg, 250 mg, 500 mg
Verubulin (MPC 6827) Cat. No.: HY-14907
Verubulin (MPC-6827) is a-disrupting agent with potent andmicrotubule
broad-spectrum in vitro and in vivo cytotoxicactivities, and acts as a promising candidate forthe treatment of multiple cancer types.
Purity: >98%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg
32 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]
Verubulin hydrochloride (MPC-6827 hydrochloride) Cat. No.: HY-12098
Verubulin hydrochloride (MPC-6827 hydrochloride)is a blood brain barrier permeable
-disrupting agent, with potent andmicrotubulebroad-spectrum in vitro and in vivo cytotoxicactivities.
Purity: 98.27%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 1 mg, 5 mg
Vinblastine sulfate (Vincaleukoblastine sulfate salt) Cat. No.: HY-13780
Vinblastine sulfate is a cytotoxic alkaloid usedagainst various cancer types. Vinblastine sulfateinhibits the formation of microtubule andsuppresses nAChR with an of 8.9 μM.IC50
Purity: 99.85%Clinical Data: LaunchedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg
Vincristine (Leurocristine; NSC-67574; 22-Oxovincaleukoblastine) Cat. No.: HY-N0488A
Vincristine (Leurocristine) is amicrotubule-destabilizing agent (MDA). Vincristine(Leurocristine) binds to tubulin and inhibits theformation of microtubules, thereby inhibitingmitosis of the cancer cell.
Purity: >98%Clinical Data: LaunchedSize: 5 mg, 10 mg, 20 mg
Vincristine sulfate (Leurocristine sulfate; NSC-67574
sulfate; 22-Oxovincaleukoblastine sulfate) Cat. No.: HY-N0488
Vincristine sulfate is an antitumor vinca alkaloidwhich inhibits formation in mitoticmicrotubulespindle, resulting in an arrest of dividing cellsat the metaphase stage. It binds to microtubulewith a of 85 nM.Ki
Purity: 99.66%Clinical Data: LaunchedSize: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg, 200 mg
Vinorelbine (KW-2307 base) Cat. No.: HY-12053
Vinorelbine is an anti-mitotic agent whichinhibits the proliferation of Hela cells with IC50
of 1.25 nM.
Purity: >98%Clinical Data: LaunchedSize: 10 mg, 50 mg
Vinorelbine ditartrate (KW-2307; Nor-5'-anhydrovinblastine ditartrate) Cat. No.: HY-12053A
Vinorelbine (ditartrate) is an anti-mitotic agentwhich inhibits the proliferation of Hela cellswith IC of 1.25 nM.50
Purity: 99.58%Clinical Data: LaunchedSize: 10 mM × 1 mL, 10 mg, 50 mg
www.MedChemExpress.com 33
Mps1Monopolar spindle 1
Monopolar spindle 1 (Mps1), also known as TTK, is a serine threonine kinase, which ensures proper biorientation of sisterchromatids on the mitotic spindle by the activation of the spindle assembly checkpoint (SAC). Mps1 has been shown to function asthe key kinase that activates the spindle assembly checkpoint (SAC) to secure proper distribution of chromosomes to daughtercells.
Mps1 is a dual specificity protein kinase that is essential for the bipolar attachment of chromosomes to the mitotic spindle and formaintaining the spindle assembly checkpoint until all chromosomes are properly attached. Mps1 is expressed at high levels duringmitosis and is abundantly expressed in cancer cells. Disruption of Mps1 function induces aneuploidy and cell death.
34 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]
Mps1 Inhibitors
AZ3146Cat. No.: HY-14710
AZ3146 is a reasonably potent and selective inhibitor with of 35 nM forMps1 IC50
Mps1 .Cat
Purity: 99.92%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg
BAY1217389Cat. No.: HY-12859
BAY 1217389 is a potent, and selective inhibitorof the monopolar spindle 1 ( ) kinase withMPS1an value less than 10 nM.IC50
Purity: 99.94%Clinical Data: Phase 1Size: 10 mM × 1 mL, 2 mg, 5 mg, 10 mg, 25 mg, 50 mg
BOS-172722Cat. No.: HY-112162
BOS-172722 is an inhibitor of monopolar spindle 1 checkpoint with an of 2 nM.(MPS1) IC50
Purity: 99.41%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg
CCT251455Cat. No.: HY-12603
CCT251455 is a potent and selective mitotic kinasemonopolar spindle 1 ( ) inhibitor with anMPS1
of 3 nM.IC50
Purity: >98%Clinical Data: No Development ReportedSize: 100 mg, 250 mg, 500 mg
Empesertib (BAY 1161909) Cat. No.: HY-12858
Empesertib (BAY 1161909) is a potent Mps1inhibitor, with an of < 1 nM.IC50
Purity: >98.0%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg
MPI-0479605Cat. No.: HY-12660
MPI-0479605 is a potent and selectiveATP-competitive inhibitor of , with an Mps1 IC50
of 1.8 nM.
Purity: 99.85%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 2 mg, 5 mg, 10 mg, 50 mg
Mps1-IN-1Cat. No.: HY-13298
Mps1-IN-1 is a potent, selective andATP-competitive kinase inhibitor, with anMps1
and a of 367 nM and 27 nM.IC50 Kd
Purity: 99.66%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg
Mps1-IN-2Cat. No.: HY-13994
Mps1-IN-2 is a potent, selective andATP-competitive dual inhibitor, withMps1/Plk1an and a of 145 nM and 12 nM for Mps1IC50 Kd
and a of 61 nM for Plk1.Kd
Purity: 98.06%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg
Mps1-IN-3Cat. No.: HY-12401
Mps1-IN-3 is a potent and selective kinaseMPS1inhibitor, with an of 50 nM.IC50
Purity: >98.0%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg
NMS-P715Cat. No.: HY-12382
NMS-P715 is a selective, ATP-competitive inhibitorof , with an of 182 nM.MPS1 IC50
Purity: >99.0%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 50 mg, 100 mg
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TC-Mps1-12Cat. No.: HY-110115
TC-Mps1-12 is a potent and selective monopolar inhibitor, with an of 6.4spindle 1 (Mps1) IC50
nM.
Purity: >99.0%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg
36 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]
Myosin
Myosin light chain kinase (MLCK) is a ubiquitous Ca /calmodulin (CaM)-activated kinase found in smooth, cardiac, and skeletal2+
muscle as well as in mammalian nonmuscle cells.
Myosin light chain kinase (MLCK) is a regulatory protein forsmooth muscle contraction, which acts by phosphorylating20-kDamyosin light chain (MLC20) to activate the myosin ATPase activity.Myosin light chain kinase (MLCK) of smooth musclehasbeen puried as an enzyme that phosphorylates 20-kDa lightchain of smoothmuscle myosin (MLC20).
Analysis of the cross talk between Ras-ERK and PI3K-AKT signaling pathways reveals integrin β1, myosin light chain kinase (MLCK)and myosin IIA are required for the activation of PI3K-AKT following inhibition of the Ras-ERK pathway. Integrin β1, MLCK, andmyosin IIA are factors in the development of resistance to MEK inhibitors.
Myosin light chain kinase (MLCK) phosphorylates the regulatory light chain (RLC) of myosin producing increases in forcedevelopment during skeletal muscle contraction.
www.MedChemExpress.com 37
Myosin Inhibitors, Activators & Modulators
(-)-Blebbistatin ((S)-(-)-Blebbistatin) Cat. No.: HY-13441
(-)-Blebbistatin is an S enantiomer ofblebbistatin. Blebbistatin is a potent andselective inhibitor with s rangingmyosin II IC50
from 0.5 to 5 μM.
Purity: 99.42%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg
ATM-3507Cat. No.: HY-100948
ATM-3507 is a potent inhibitor withtropomyosins from 3.83-6.84 μM in human melanoma cellIC50
lines.
Purity: >98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 50 mg, 100 mg
ATM-3507 trihydrochlorideCat. No.: HY-100948B
ATM-3507 trihydrochloride is a potent inhibitor with s from 3.83-6.84tropomyosin IC50
μM in human melanoma cell lines.
Purity: 98.10%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg
BlebbistatinCat. No.: HY-13813
Blebbistatin is a selective non-muscle myosin inhibitor, promotes directionalII (NMII)
migration of corneal endothelial cells (CECs) andaccelerates wound healing, and better preservescell junctional integrity and barrier function.
Purity: >97.0%Clinical Data: No Development ReportedSize: 1 mg
BTS (N-Benzyl-p-toluenesulfonamide; N-Tosylbenzylamine) Cat. No.: HY-16690
BTS is a potent inhibitor of Ca2+-stimulatedmyosin S1 ATPase (IC50 ~ 5 μM) and reversiblyblocks the gliding motility.
Purity: 99.78%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 500 mg
HA-100Cat. No.: HY-100984
HA-100 is an inhibitor of cGMP-dependent proteinkinase ( ), cAMP-dependent protein kinasePKG( ), protein kinase C ( ) and PKA PKC MLC-kinasewith s of 4, 8, 12 and 240 μM, respectively.IC50
Purity: 99.76%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg
Mavacamten (MYK461; SAR439152) Cat. No.: HY-109037
Mavacamten is a modulator of ,cardiac myosinwith of 490, 711 nM for bovine cardiac andIC s50
human cardiac, respectively.
Purity: 99.94%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg
ML-7 hydrochlorideCat. No.: HY-15417
ML-7 hydrochloride is a naphthalene sulphonamidederivative, potently inhibits ( =300MLCK IC50
nM).
Purity: 99.49%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 10 mg, 50 mg
ML-9Cat. No.: HY-100932
ML-9 is a selective and potent inhibitor of Akt, inhibits myosin light-chain kinase (MLCK)kinase
and stromal interaction molecule 1 (STIM1)activity. ML-9 inhibits inhibits MLCK, PKA and PKCactivity with values of 4, 32 and 54 μM,Ki
respectively.
Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg
ML-9 Free BaseCat. No.: HY-100932A
ML-9 (Free Base) is a selective and potentinhibitor of , inhibits myosinAkt kinaselight-chain kinase (MLCK) and stromal interactionmolecule 1 (STIM1) activity.
Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg
38 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]
MLCK inhibitor peptide 18Cat. No.: HY-P1029
MLCK inhibitor peptide 18 is a myosin light chainkinase ( ) inhibitor with an of 50 nM,MLCK IC50
and inhibits only at 4000-foldCaM kinase IIhigher concentrations.
Purity: 98.71%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg, 25 mg
MS-444 (BE-34776) Cat. No.: HY-100685
MS-444 inhibits the activity of purified smoothmuscle myosin light chain kinase ( ) with anMLCK
value of 10 μM.IC50
Purity: >98%Clinical Data: No Development ReportedSize: 100 mg, 250 mg, 500 mg
Omecamtiv mecarbil (CK-1827452) Cat. No.: HY-14233
Omecamtiv mecarbil is a selective cardiac myosinactivator.
Purity: 99.28%Clinical Data: Phase 3Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg
para-NitroblebbistatinCat. No.: HY-120870
para-Nitroblebbistatin is a non-cytotoxic,photostable, fluorescent and specific Myosin IIinhibitor, usd in the study of the specific roleof myosin II in physiological, developmental, andcell biological studies.
Purity: >98%Clinical Data: No Development ReportedSize: 100 mg, 250 mg, 500 mg
www.MedChemExpress.com 39
PAKp21 activated kinases
PAKs (p21-activated kinases) are key regulators of actin dynamics, cell proliferation and cell survival. PAKs are Ser/Thr kinases thatare classified into two groups on the basis of their structural and functional features: group I (PAK1–3) and group II (PAK4–6). GroupI PAKs have an auto-inhibitory domain (also called an inhibitory switch domain) and a kinase domain (catalytic domain, CD) and areactivated by the binding of the active (that is, GTP-bound) forms of Rho GTPases, such as Cdc42 and Rac1. Group II PAKs have noauto-inhibitory domains and are not activated by active Rho GTPases. Because the deregulation of PAKs is closely associated withvarious human diseases,small-molecule inhibitors of these kinases have great potential as therapeutic agents. In addition, thesecompounds can also be used as powerful tools in studies aimed at understanding the PAK signaling pathway.
PAKs are considered prime regulators of the actin cytoskeleton and motility. Due to their central role in actin remodelling and theirability to activate Matrix metalloproteinases (MMPs), Rho GTPases play an important role in tumor cell invasion and metastasis. Thecurrent evidence suggests the involvement of PAKs in motility, cell survival, anchorage-independent growth, angiogenesis, invasion,migration and regulation of cell cycle and mitosis. Consequently, PAKs have also been implicated in a number of pathologicalconditions including cancer.
40 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]
PAK Inhibitors & Activators
5-Aminosalicylic Acid (Mesalamine; 5-ASA; Mesalazine) Cat. No.: HY-15027
5-Aminosalicylic acid (Mesalamine) acts as aspecific agonist and also inhibitsPPARγp21-activated kinase 1 ( ) and .PAK1 NF-κB
Purity: >98.0%Clinical Data: LaunchedSize: 10 mM × 1 mL, 500 mg, 10 g
Fingolimod (FTY720 free base) Cat. No.: HY-11063
Fingolimod is a ( )sphingosine 1-phosphate S1Pantagonist with of 0.033 nM in K562 and NKIC50
cells. Fingolimod also is a activator, apak1immunosuppressant.
Purity: 99.95%Clinical Data: LaunchedSize: 10 mM × 1 mL, 5 mg, 10 mg
Fingolimod hydrochloride (FTY720) Cat. No.: HY-12005
Fingolimod hydrochloride is a sphingosine ( ) antagonist with an of1-phosphate S1P IC50
0.033 nM in K562 and NK cells. Fingolimodhydrochloride also is a activator.pak1
Purity: 99.86%Clinical Data: LaunchedSize: 10 mM × 1 mL, 100 mg, 200 mg, 1 g, 5 g
FRAX1036Cat. No.: HY-19538
FRAX1036 is a inhibitor with s of 23.3 nM,PAK Ki
72.4 nM, and 2.4 μM for PAK1, PAK2 and PAK4,respectively.
Purity: 99.32%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg
FRAX486Cat. No.: HY-15542B
FRAX486 is a p21-activated kinase ( ) inhibitorPAKwith s of 14, 33 and 39 nM for PAK1, PAK2 andIC50
PAK3, respectively.
Purity: >98.0%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg
FRAX597Cat. No.: HY-15542A
FRAX597 is a potent group I p21-activated Kinases( s) inhibitor with of 8, 13 and 19 nM forPAK IC50
, and .PAK1 2 3
Purity: >99.0%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg
G-5555Cat. No.: HY-19635
G-5555 is a potent p21-activated kinase 1 ( )PAK1inhibitor with s of 3.7 nM and 11 nM for PAK1Ki
and PAK2, respectively.
Purity: 99.18%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg
G-5555 hydrochlorideCat. No.: HY-19635A
G-5555 hydrochloride is a potent and selectivep21-activated kinase 1 ( ) inhibitor with a PAK1 Ki
of 3.7 nM.
Purity: 98.19%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg
GNE 2861Cat. No.: HY-12632
GNE 2861 is a inhibitor that displays groupPAKII selectivity. GNE 2861 inhibits PAK4, PAK5 andPAK6 with s of 7.5, 36, 126 nM, respectively.IC50
Purity: 99.33%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg
IPA-3Cat. No.: HY-15663
IPA-3 is a selective non-ATP competitive PAK1inhibitor with of 2.5 μM, and shows noIC50
inhibition to group II PAKs (PAKs 4-6).
Purity: >98.0%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg
www.MedChemExpress.com 41
NVS-PAK1-1Cat. No.: HY-100519
NVS-PAK1-1 is a potent and selective allosteric inhibitor with an of 5 nM.PAK1 IC50
Purity: 99.82%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg
PF-3758309Cat. No.: HY-13007
PF-3758309 is a potent, orally available, andreversible ATP-competitive inhibitor of PAK4( = 2.7 nM; =18.7 nM).Kd Ki
Purity: 99.95%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg
42 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]