Tubulin inhibitor 33, a tubulin polymerization inhibitor, inhibits tubulin polymerization in a dose-dependent manner with an IC50 of 9.05 μM. Tubulin inhibitor 33 has antitumor effects and induces cell apoptosis that can be used for antitumor research[1].
Tubulin polymerization-IN-31 (Compound 4c) is a tubulin polymerization inhibitor with an IC50 of 3.64 μM. Tubulin polymerization-IN-31 induces cancer cell apoptosis and shows antitumor activity[1].
Paclitaxel D5 is a deuterium-labeled Paclitaxel. Paclitaxel is a naturally occurring antineoplastic agent and stabilizes tubulin polymerization[1].
Fmoc-MMAE is a protective group-conjugated monomethyl auristatin E (MMAE), which is a potent tubulin inhibitor. Fmoc-MMAE can be used in the synthesis of ADC[1].
A potent, specific, allosteric and cell-active inhibitor of KSP with IC50 of 11 nM; has no ihibitory activity toward other kinesins, includin CENP-E, MKLP-1, KIF-3A, and uKHC (IC50>50 uM); induces the formation of monoastral spindles, causes mitotic arrest in a dose-dependent manner (EC50=30 nM) in A2780 ovarian carcinoma cells; sustained KSP inhibition activates the proapoptotic protein, Bax, and both activation of the spindle checkpoint and subsequent mitotic slippage are required for Bax activation.
KIF18A-IN-3 is a potent KIF18A inhibitor (IC50=61 nM). KIF18A-IN-3 causes significant mitotic arrest and increases the number of mitotic cells in tumor tissues. KIF18A-IN-3 can be used for researching cancer[1].
RGDSPASSKP is a RGDS-containing fibronectin decapeptide[1].
Mivobulin (NSC 613862) is a tubulin inhibitor, binds to tubulin in the region that overlaps the colchicine site, and inhibits tubulin polymerization. Mivobulin (NSC 613862) promotes the formation of abnormal polymers and a GTPase activity in the tubulin dimer. Anti-cancer activity[1].
Taxinine B is a taxoid that can be isolated from Japanese Yew Taxus Cuspid. Taxinine B inhibits CaCl2-induced depolymerization of microtubule. Taxinine B is useful for overcoming multidrug resistance in tumor cells[1].
Galacto-RGD is an RGD analogue that can be coupled with the radioactive isotope 18F and used as an integrin α₅β₃ selective tracer[1].
S-Trityl-L-cysteine (NSC 83265) is a selective and allosteric kinesin Eg5 inhibitor with an IC50 of 1 μM for the inhibition of basal ATPase activity and 140 nM for the microtubule-activated ATPase activity. S-Trityl-L-cysteine has antitumor activities[1][2].
Monastrol is a potent and cell-permeable inhibitor of the mitotic kinesin Eg5 with an IC50 value of 14 μM.
Clathrin-IN-4 (compound 8b), a Wiskostatin (HY-12534) analogue, is a potent inhibitor of clathrin mediated endocytosis with an IC50 of 2.1 μM. Clathrin-IN-4 is a dynamin I GTPase activity inhibitor with an IC50 of 9.1 μM[1].
BMS-688521 is a highly potent, orally active inhibitor of the LFA-1/ICAM interaction, with an IC50 of 2.5 nM in the adhesion assay and an IC50 of 60 nM in the MLR assay. BMS-688521 is efficacious in a mouse allergic eosinophilic lung inflammation model[1].
Vincristine-d3-ester (Leurocristine-d3-ester) sulfate is the deuterium labeled Vincristine sulfate. Vincristine sulfate is an antitumor vinca alkaloid which inhibits microtubule formation in mitotic spindle, resulting in an arrest of dividing cells at the metaphase stage. It binds to microtubule with a Ki of 85 nM[1].
ML-9 is a selective and potent inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity[3]. ML-9 inhibits inhibits MLCK, PKA and PKC activity with Ki values of 4, 32 and 54 μM, respectively[1]. ML-9 induces autophagy by stimulating autophagosome formation and inhibiting their degradation[3].
RGD peptide acts as an inhibitor of integrin-ligand interactions and plays an important role in cell adhesion, migration, growth, and differentiation[1]. RGD peptides promote apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing[2][3].
Tubulysin IM-2 is an ADC Cytotoxin and tubulin binder used as anti-microtubule toxins.
AZ13705339 is a potent, selective PAK1 inhibitor with IC50 of 0.33 nM, displays 14-, 470-, 4100- and 2600-fold selectivity over Src, FGFR1, KDR and PAK4; inhibits cellular pPAK1 inhibition in MCF10A cell line with IC50 of 59 nM.
Cytochalasin D (Zygosporin A; NSC 209835) is a potent and cell-permeable inhibitor of actin polymerization derived from fungus, inhibits the G-actin–cofilin interaction by binding to G-actin. Cytochalasin D (Zygosporin A; NSC 209835) also inhibits the binding of cofilin to F-actin and decreases the rate of both actin polymerization and depolymerization in living cells[1][2][3].
Tadocizumab (C4G1; YM-337) is a humanized monoclonal antibody tageting integrin αIIbβ3. Tadocizumab has antiplatelet and antithrombotic effects, and can be used for cardiovascular disease research[1][2].
Tubulin inhibitor 12 (Hit 9) is a novel tubulin inhibitor (IC50=25.3 μM). Tubulin inhibitor 12 shows anti-tumor activity and anti-proliferative activity[1].
Wiskostatin is a potent and selective inhibitor of neuronal Wiskott-Aldrich syndrome protein (N-WASP)-mediated actin polymerization. Wiskostatin causes a rapid, profound, and irreversible decrease in cellular ATP levels[1].
Violanone, an isoflavanone compound, can inhibit tubulin polymerization. Violanone also exhibits larvicidal activity against A. aegypti[1][2].
MK-0429 is a potent integrin antagonist with IC50s of 12.2 nM (α5β1 integrin) and 2.8 nM (αvβ3 integrin), respectively.
Anticancer agent 98 (compound 12k) is a microtubule/tubulin-polymerization inhibitor (Kd=16.9 μM). Anticancer agent 98 exerts antiproliferative potency against tumor cells, exhibits anti-angiogenesis effect in vitro. Anticancer agent 98 exhibits good human and mouse liver microsomes stability with both t1/2>300 min[1].
Tubulin inhibitor 18 (compound 5j) is a potent inhibitor of tubulin. Tubulin inhibitor 18 is a chalcone compound. Tubulin inhibitor 18 has the potential for the research of cancer diseases[1].
Vinblastine is a cytotoxic alkaloid used against various cancer types. Vinblastine inhibits the formation of microtubule and suppresses nAChR with an IC50 of 8.9 μM.
Tirofiban(L700462;MK383) is a potent non-peptide, glycoprotein IIb/IIIa (integrins alphaIIbbetaIII) antagonistTarget: integrin IIb/IIIa Tirofiban hydrochloride monohydrate blocks platelet aggregation and thrombus formation. Tirofiban is an antithrombotic used in the treatment of unstable angina.Tirofiban, in a concentration-dependent manner reduced platelet aggregation evoked by ADP (IC50 approximately 70 ng/ml), collagen (IC50 approximately 200 ng/ml), and thrombin (IC50 approximately 5,000 ng/ml).
JNJ-26076713 is a potent and orally active alpha V integrin antagonist with IC50 values of 2.3 nM and 6.3 nM for alpha(V)beta(3) and alpha(V)beta(5), respectively. JNJ-26076713 inhibits retinal neovascularization[1].