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microtubule assembly inhibitor
4-Demethylepipodophyllotoxin is a potent inhibitor of microtubule assembly. -
Microtubule Associated inhibitor
ABT-751 is an antimitotic agent, inhibits microtubule polymerization, binds to β-tubulin on the colchine site; blocks cell cycle at G2M phase and induces apoptosis. -
Microtubule Inhibitor
CYT997 is a novel anti-cancer vascular disrupting agent (VDA). In vitro, CYT997 is shown to potently inhibit the proliferation of vascular endothelial growth factor-stimulated human umbilical vein endothelial cells (IC(50) 3.7 ?? 1.8 nM) and cause significant morphological changes at 100 nM, including membrane blebbing. -
Microtubule Associated inhibitor
Docetaxel (Taxotere) is an antineoplastic agent that acts by disrupting the microtubular network in cells that is essential for mitotic and interphase cellular functions.- Adi Jacob Berger, .et al. , Nat Cancer, 2021, 2, 1055-1070 PMID: 35121883
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Microtubule Associated inhibitor
Epothilone A acts by stabilising microtubule formation at the taxol binding site and causes cell cycle arrest at the G2/M transition, leading to cytotoxicity. -
Microtubule Associated inhibitor
Epothilone B is a macrolide that causes the formation of bundles of intracellular microtubules in non-mitotic cells, induces the formation of hyperstable tubulin polymers, and arrests cell cycling in mitosis.- Yicheng Zhu, .et al. , Neurosci Res, 2021, Apr 17 PMID: 33864880
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KSP Inhibitor
Ispinesib (SB-715992) is a potent inhibitor of kinesin spindle protein, a kinesin motor protein essential for the formation of a bipolar mitotic spindle and cell cycle progression through mitosis. -
Microtubule Associated inhibitor
Paclitaxel (Taxol) is a mitotic inhibitor that stabilizes microtubules and as a result, interferes with the normal breakdown of microtubules during cell division.- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
- Yu Pan, .et al. , Nucleic Acids Res, 2021, Jan 11;49(1):38-52 PMID: 33290562
- Li-Li Li, .et al. , Nat Commun, 2020, Oct 9;11(1):5107 PMID: 33037199
- Baglo Y, .et al. , Photochem Photobiol, 2019, Dec 19 PMID: 31856423
- Owiti AO, .et al. , AAPS PharmSciTech, 2018, Nov;19(8):3534-3549 PMID: 30151731
- Owiti AO, .et al. , AAPS PharmSciTech, 2018, Oct;19(7):3110-3122 PMID: 30112614
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Tubulin inhibitor
Vincristine is a mitotic inhibitor, and is used in cancer chemotherapy. -
Microtubule Associated inhibitor
Vinflunine Tartrate is a tartrate salt of vinflunine that destabilizes microtubules with an IC50 of 18.8 nM and interferes with the dynamics of microtubules during cell division. -
KSP inhibitor
KSP inhibitor ARRY-520 specifically inhibits KSP (kinesin-5 or Eg5) with potential antineoplastic activity. -
Mps1 inhibitor
AZ 3146 is a potent and selective monopolar spindle 1 (Mps1) kinase inhibitor (IC50 = 35 nM). It interferes with chromosome alignment and overrides spindle assembly checkpoint and also Inhibits the recruitment of Mad1, Mad2 and centromere protein E (CENP-E) to kinetochores.
- Ryoko Ota, .et al. , Cell Signal, 2023, Sep;109:110764 PMID: 37315749
- Ryuzaburo Yuki, .et al. , J Cell Mol Med, 2021, Feb;25(3):1677-1687 PMID: 33465289
- Yamagishi A, .et al. , Int J Mol Sci, 2020, Feb 5;21(3) PMID: 32033461
- Kakihana A, .et al. , FASEB J, 2018, Nov 29:fj201801369R PMID: 30496702
- Suzuki M, .et al. , Anticancer Res, 2016, Jun;36(6):2783-92 PMID: 27272789
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CENP-E inhibitor
GSK-923295, is a small-molecule inhibitor of the mitotic kinesin centromere-associated protein E, (CENP-E). -
microtubule inhibitor
Ixabepilone is an epothilone B analog- Dong-Sheng Cao, .et al. , Eur J Med Chem, 2020, Aug 1;199:112421 PMID: 32428794
- Hoque M, .et al. , Pharmacol Res, 2018, Aug;134:166-178 PMID: 29944980
- APRIL L. RISINGER, .et al. , Anticancer Res, 2015, Nov; 35(11): 5845-5850 PMID: 26504006
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Microtubule Associated inhibitor
Cabazitaxel is a semi-synthetic derivative of a natural taxoid. Cabazitaxel in combination with prednisone is a treatment option for hormone-refractory prostate cancer following docetaxel-based treatment- Satoshi Endo, .et al. , J Biochem, 2021, Mar 17 PMID: 33729485
- Tomohiro Nabekura, .et al. , Biochem Biophys Rep, 2020, Mar; 21: 100727 PMID: 31993509
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PAK4 inhibitor
PF-3758309 is a small-molecule p21-activated kinase inhibitor inhibiting oncogenic signaling and tumor growth. -
MLCK inhibitor
ML 7 hydrochloride is a selective inhibitor of myosin light chain kinase (MLCK).- Praneeth Siripurapu, .et al. , J Biol Chem, 2017, Oct 20; 292(42): 17482-17495 PMID: 28864771
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TTK inhibitor
CFI-402257, a pyrazolopyridin derivative, has been found to be a TTK inhibitor that could influence chromosome segregation and induce cell death so that is significant in anticancer studies.- Jian Yu, .et al. , BMC Cancer, 2022, Jul 18;22(1):786 PMID: 35850753
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Integrin inhibitor
Cilengitide is a cyclic Arg-Gly-Asp peptide with potential antineoplastic activity. Cilengitide binds to and inhibits the activities of the alpha(v)beta(3) and alpha(v)beta(5) integrins, thereby inhibiting endothelial cell-cell interactions, endothelial cell-matrix interactions, and angiogenesis.- Yi Han Tan, .et al. , Cell Microbiol, 2017, Aug;19(8) PMID: 28186697
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Integrin inhibitor
Cilengitide is a cyclic Arg-Gly-Asp peptide with potential antineoplastic activity. Cilengitide binds to and inhibits the activities of the alpha(v)beta(3) and alpha(v)beta(5) integrins, thereby inhibiting endothelial cell-cell interactions, endothelial cell-matrix interactions, and angiogenesis.- Marion Bouvet, .et al. , Sci Rep, 2020, 10: 11404 PMID: 32647159
- Rosalie Richards, .et al. , bioRxiv, 2018, 15 Oct 2018
- Hiroki Kanazawa, .et al. , PLoS One, 2017, 12(2): e0173051 PMID: 28235037
- Yasuda J, .et al. , Naunyn Schmiedebergs Arch Pharmacol, 2017, Nov;390(11):1135-1144 PMID: 28785775
- Yasuda J, .et al. , Eur J Pharmacol, 2017, Jul 15;807:64-70 PMID: 28457922
- Hsian-Yu Wang, .et al. , Onco Targets Ther, 2016, 9: 2961-2973 PMID: 27284246
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PAK inhibitor
FRAX597, a small-molecule pyridopyrimidinone, is a potent and ATP competitive inhibitor of the group I PAKs (PAK1 IC50= 8 nM, PAK2 IC50= 13 nM, PAK3 IC50= 19 nM). -
allosteric PAK1 inhibitor
NVS-PAK1-1 is a potent and selective allosteric PAK1 inhibitor with an IC50 of 5 nM. -
Dynamin inhibitor
Dynasore is a non-competitive inhibitor of dynamin 1, dynamin 2 and mitochondrial dynamin (Drp1) GTPase activity- Umut Kerem Kolac, .et al. , Mol Biol Rep, 2023, Jan;50(1):493-506 PMID: 36352179
- KOLAC UK, .et al. , Research Square, 2022, 03 Jun
- Tsukamoto H, .et al. , J Biol Chem, 2018, Jun 29;293(26):10186-10201 PMID: 29760187
- Shigetoshi Yokoyama, .et al. , eLife, 2018, 7: e37854 PMID: 30526845
- Naoko Fujii, .et al. , J Biol Chem, 2016, Nov 18; 291(47): 24787-24799 PMID: 27733684
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PKC inhibitor
GF 109203X is a potent and selective inhibitor of protein kinase C, selective for the α and β1 isoforms (IC50 values are 0.0084, 0.0180, 0.210, 0.132, and 5.8 μM for α, β1, δ, ε and ζ isoforms respectively). Selective over MLCK, PKG and PKA (IC50 values are 0.6, 4.6, and 33 μM respectively). Potent antagonist at the 5-HT3 receptor (Ki = 29.5 nM). -
microtubule inhibitor
Nocodazole is a microtubule inhibitor; inhibits mitosis. Also inhibits autophagosome-lysosome fusion. -
PKA, PKG, Casein Kinase I and II inhibitor
A-3 Hydrochloride is an inhibitor of PKA (cAMP-dependent protein kinase, Ki=4.3μM) and cGMP-dependent protein kinase, Ki=3.8μM, PKC (protein kinase C, Ki=47μM), casein kinase I and II, and MLCK (myosin light chain kinase) ( Ki=7.4μM). -
myosin II inhibitor
Blebbistatin, a myosin II inhibitor, is photoinactivated by blue light. -
microtubule dynamics inhibitor
Vinblastine sulfate inhibits microtubule formation and suppresses nAChR activity with IC50 of 8.9 μM in a cell-free assay, used to treat certain kinds of cancer. -
PAK inhibitor
FRAX486 is a small-molecule PAK inhibitor.- Natalia Barraza-Núñez, .et al. , Neurotox Res, 2023, Mar 3 PMID: 36867391
- Yukie Yamahashi, .et al. , Mol Psychiatry, 2022, 03 June
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CaMKII inhibitor
KN-93 Phosphate is a potent and specific inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMKII) with Ki of 0.37 μM, no remarkable inhibitory effects on APK, PKC, MLCK or Ca2+-PDE activities.- Kazuki Yuasa, .et al. , Sci Rep, 2018, 8: 9037 PMID: 29899565
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Mps1 inhibitor
MPI-0479605 is an ATP competitive and selective inhibitor of mitotic kinase Mps1 -
DRP1 inhibitor
Mdivi-1 is a selective cell-permeable inhibitor of mitochondrial division DRP1 (dynamin-related GTPase) and mitochondrial division Dynamin I (Dnm1) with IC50 of 1-10 uM.- Umut Kerem Kolac, .et al. , Mol Biol Rep, 2023, Jan;50(1):493-506 PMID: 36352179
- KOLAC UK, .et al. , Research Square, 2022, 03 Jun
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Microtubule polymerization inhibitor
Cucurbitacin B, a natural triterpenoid is well-known for its strong anticancer activity, and recent studies showed that the compound inhibits JAK/STAT3 pathway. Also it is an potent Microtubule polymerization inhibitor -
Dynamin inhibitor
Dynamin Inhibitory Peptide is a peptide inhibitor of the GTPase dynamin. -
Panx-1 mimetic inhibitor
Scrambled 10Panx, Panx-1 mimetic inhibitory peptide, is a blocker of pannexin-1 gap junctions. -
αvβ3 integrin inhibitor
Cyclo (-RGDfK) is a potent and selective inhibitor of the αvβ3 integrin.- Julian Tu, .et al. , Synlett, 2020, 31, A-F
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KSP inhibitor
ARRY-520 R enantiomer is the R form of ARRY-520, which is a synthetic, small molecule kinesin spindle protein (KSP) inhibitor with IC50 of 6 nM.