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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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CENP-E inhibitor
GSK-923295, is a small-molecule inhibitor of the mitotic kinesin centromere-associated protein E, (CENP-E). -
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
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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.
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allosteric PAK1 inhibitor
NVS-PAK1-1 is a potent and selective allosteric PAK1 inhibitor with an IC50 of 5 nM. -
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
- Pyrintegrin is a cell-permeable small molecule that promotes human embryonic stem cell (hESC) survival by > 30-fold.
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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 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. -
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
- Monomethyl auristatin F (MMAF) is a synthetic antineoplastic agent. It is part of some experimental anti-cancer antibody-drug conjugates such as vorsetuzumab mafodotin and SGN-CD19A.
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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 -
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 -
Gap-junction modifier
GAP-134 Hydrochloride, a small modified dipeptide, has been identified as a potent and selective second generation gap junction modifier with oral bioavailability. -
PAK4/NAMPT Inhibitor
KPT 9274 ( ATG-019) is an orally bioavailable small molecule that is a non-competitive dual inhibitor of PAK4 and NAMPT. It shows an IC50 of ~120 nM for NAMPT in a cell-free enzymatic assay. -
Kinesin Eg5 inhibitor
Dimethylenastron is an inhibitor of mitotic motor kinesin Eg5 with IC50 value of 200 nM. -
Integrin inhibitor
Cyclo(RGDyK) trifluoroacetate is a potent and selective alphaVbeta3 integrin inhibitor with IC50 of 20 nM. -
αV integrins inhibitor
CWHM 12 can suppress all 5 alpha V integrins. CWHM12 not only worked the same way to prevent fibrosis as the genetic deletion method, it also prevent the progression of existing fibrosis in the liver and lungs and reversed some of the damage caused by fibrosis to those organs. -
tubulin polymerization inhibitor
Crolibulin, also known as EPC2407 and crinobulin, is a small molecule tubulin polymerization inhibitor with potential antineoplastic activity. -
α1β1 inhibitor
Highly potent integrin α1β1 inhibitor (IC50 = 0.8 nM for α1β1 binding to type IV collagen). Selective for α1β1 over α2β1, αIIbβ3, αvβ3, α4β1, α5β6, α9β1 and α4β7. Inhibits FGF2-stimulated angiogenesis in the chicken chorioallantoic model. Displays antitumor efficacy in a synergistic mouse model of Lewis lung carcinoma; blocks human melanoma growth in nude mice. -
α9β1/α4β1 integrin inhibitor
BOP sodium salt is a novel dual alpha9beta1/alpha4beta1 integrin inhibitor. -
MLCK inhibitor
ML-9 is a selective and potent inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity. ML-9 inhibits inhibits MLCK, PKA and PKC activity with Ki values of 4, 32 and 54 μM, respectively. ML-9 induces autophagy by stimulating autophagosome formation and inhibiting their degradation. -
MPS1 checkpoint inhibitor
BOS-172722 is an inhibitor of monopolar spindle 1 (MPS1) checkpoint with an IC50 of 2 nM. -
α4β1/α4β7 integrin antagonist
Zaurategrast ethyl ester (CDP323), the ethyl ester prodrug of CT7758, is a α4β1/α4β7 integrin antagonist used for the treatment of inflammatory and autoimmune disorders. - Ombrabulin hydrochloride is a derivative of CA-4 phosphate, which is known to exhibit antivascular effects through selective disruption of the tubulin cytoskeleton of endothelial cells.
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tubulin polymerization inhibitor
Soblidotin (Auristatin PE) is a novel synthetic Dolastatin 10 derivative and inhibitor of tubulin polymerization. -
cytotoxic tubulin modifier
Auristatin F is a cytotoxic tubulin modifier with potent and selective antitumor activity; MMAF analog and cytotoxin in Antibody-drug conjugates. Auristatin F inhibits cell division by blocking the polymerisation of tubulin. -
cytotoxic tubulin modifier
Auristatin E is a cytotoxic tubulin modifier with potent and selective antitumor activity; MMAE analog and cytotoxin in Antibody-drug conjugates. Auristatin E inhibits cell division by blocking the polymerisation of tubulin.
