Catalog No.
Product Name
Application
Product Information
Product Citation
- Monomethyl auristatin E (MMAE) is an antimitotic agent which inhibits cell division by blocking the polymerisation of tubulin, and also shows inhibition of antibody-drug conjugates (ADCs) activity.
- Sochaj-Gregorczyk AM, .et al. , J Immunother, 2016, Jul-Aug;39(6):223-32 PMID: 27227324
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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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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. - Albendazole is a member of the benzimidazole compounds used as a drug indicated for the treatment of a variety of worm infestations.
- Chloroxine is an antibacterial drug useful for dandruff and seborrheic dermatitis.
- Colchicine is an inhibitor of microtubules by specific binding to tubulin.
- Yao-Yu Hsieh, .et al. , Mol Oncol, 2023, Oct 16 PMID: 37842807
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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. -
ERRα and ERRγ inverse agonist
Kaempferol is found to inhibit bovine aorta myosin light chain kinase with a Ki of 0.3-0.5 microM and also is found to inhibit VEGF expression and in vitro angiogenesis through a novel ERK-NFκB-cMyc-p21 pathway.- Asmaa R. Abdel-Hamed, .et al. , J Med Chem Sci, 2023, 6: 250-268
- A O Hamouda, .et al. , Eur Rev Med Pharmacol Sci, 2022, Dec;26(23):8644-8659 PMID: 36524484
- Podophyllotoxin is a potent inhibitor of microtubule assembly that binds at the colchicine site of tubulin.
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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. - Vinorelbine is the first 5??NOR semi-synthetic vinca alkaloid. It is obtained by semi-synthesis from alkaloids extracted from the rosy periwinkle, Catharanthus roseus.
- Rotem Ben-Hamo, .et al. , Nat Commun, 2020, 11: 3296
- Roma Kaul, .et al. , Br J Cancer, 2019, 121, pages611-621 PMID: 31481735
- Nicholas F. Dybdal-Hargreaves, .et al. , Oncotarget, 2018, Jan 19; 9(5): 5545-5561 PMID: 29464017
- APRIL L. RISINGER, .et al. , Anticancer Res, 2015, Nov; 35(11): 5845-5850 PMID: 26504006
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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.
- Junna Tanaka, .et al. , Cell Signal, 2024, Jul:119:111172 PMID: 38604342
- Ryuzaburo Yuki, .et al. , Eur J Pharmacol, 2024, Jan 15:963:176229 PMID: 38072041
- 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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Myosin activator
CK-1827452 is a selective cardiac specific myosin activator.- Oleg Lookin, .et al. , Clin Exp Pharmacol Physiol, 2021, Aug 29 PMID: 34459025
- Gabor A. Fulop, .et al. , Basic Res Cardiol, 2021, 116(1): 24 PMID: 33844095
- Wanjian Tang, .et al. , J Biol Chem, 2019, October 2 PMID: 31578282
- Thinh T. Kieu, .et al. , Biophysical Journal, 2019, 2019 PMID: 31103235
- Alexandre J. S. Ribeiro, .et al. , Circ Res, 2017, May 12; 120(10): 1572-1583 PMID: 28400398
- Anja M. Swenson, .et al. , J Biol Chem, 2017, Mar 3; 292(9): 3768-3778 PMID: 28082673
- Nánási P Jr, .et al. , Eur J Pharmacol, 2017, Aug 15;809:73-79 PMID: 28506910
- Horváth B, .et al. , Naunyn Schmiedebergs Arch Pharmacol, 2017, Dec;390(12):1239-1246 PMID: 28940010
- Szentandrassy N, .et al. , J Physiol Pharmacol, 2016, Aug;67(4):483-489 PMID: 27779469
- L Nagy, .et al. , Br J Pharmacol, 2015, Sep; 172(18): 4506-4518 PMID: 26140433
- Larissa Butler, .et al. , Toxicol Sci, 2015, Jun;145(2):396-406 PMID: 25820236
- Epothilone D improves microtubule density, axonal integrity, and cognition in a transgenic mouse model of tauopathy.
- Baihong Guo, .et al. , Neurobiol Aging, 2020, Sep 12;96:223-232 PMID: 33039900
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CENP-E inhibitor
GSK-923295, is a small-molecule inhibitor of the mitotic kinesin centromere-associated protein E, (CENP-E).- Amber S Zhou, .et al. , PLoS Biol, 2023, Oct 26;21(10):e3002339 PMID: 37883329
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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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gap-junction modulator
Tonabersat is a novel benzopyran derivative that blocks the cortical spreading depression proposed to be associated with migraine attacks. -
VCAM-1 antagonist
CDP323 is a small-molecule prodrug antagonist of the vascular cell adhesion molecule 1 binding to ??4-integrins- Mustafa Ahmadzai, .et al. , Front Immunol, 2015, 6: 525 PMID: 26539194
- Vincristine is an inhibitor of polymerization of microtubules by binding to tubulin with IC50 of 32 μM.
- Li-Li Li, .et al. , Nat Commun, 2020, Oct 9;11(1):5107 PMID: 33037199
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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). - Cevipabulin (TTI-237), an antimicrotubule agent, is a small synthetic molecule of triazolopyrimidine derivative with potential antitumor activity. With a novel mechanism of action distinct from the action of other vinca alkaloid compounds, TTI-237 specifically binds to tubulin at the vinca site, and promotes the polymerization of tubulin into microtubules.
- Yao-Yu Hsieh, .et al. , Mol Oncol, 2023, Oct 16 PMID: 37842807
- Combretastatin A4 is an antitumor, antiangiogenic and antimetastatic agent, in vitro and in vivo. Combretastatin A4 is a microtubule-targeting agent that binds β-tubulin with Kd of 0.4 μM.
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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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α4β1/α4β7 integrin antagonist
Firategrast is an orally bioavailable alpha4 beta1/alpha4 beta7 integrin antagonist designed to reduce trafficking of lymphocytes into the central nervous system (CNS).- Higuchi S, .et al. , Dev Growth Differ, 2016, Sep;58(7):586-99 PMID: 27633818
- Eribulin mesylate is the mesylate salt of a synthetic analogue of halichondrin B, a substance derived from a marine sponge (Lissodendoryx sp.) with antineoplastic activity.
- Tomohiro Nabekura, .et al. , Biochem Biophys Rep, 2020, Mar; 21: 100727 PMID: 31993509
- Snyder C, .et al. , Toxicol In Vitro, 2018, Aug;50:109-123 PMID: 29427706
- Pyrintegrin is a cell-permeable small molecule that promotes human embryonic stem cell (hESC) survival by > 30-fold.
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microtubule-targeting agent
Fosbretabulin disodium is the disodium salt of a water-soluble phosphate derivative of a natural stilbenoid phenol derived from the African bush willow (Combretum caffrum) with potential vascular disrupting and antineoplastic activities. -
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.- Chiao-Ping Chen, .et al. , Biomed Pharmacother, 2023, Oct:166:115389 PMID: 37659202
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microtubule depolymerizing agent
Ansamitocin P-3 is a maytansine analog which displays potent cytotoxicity against the human solid tumor cell lines A-549 and HT-29.
