|Description||ELR510444 is a potent microtube disruptor with potential anticancer activity. ELR510444 has potent microtubule-disrupting activity, causing a loss of cellular microtubules and the formation of aberrant mitotic spindles and leading to mitotic arrest and apoptosis of cancer cells. ELR510444 potently inhibited cell proliferation with an IC(50) value of 30.9 nM in MDA-MB-231 cells, inhibited the rate and extent of purified tubulin assembly, and displaced colchicine from tubulin, indicating that the drug directly interacts with tubulin at the colchicine-binding site. ELR510444 is not a substrate for the P-glycoprotein drug transporter and retains activity in βIII-tubulin-overexpressing cell lines, suggesting that it circumvents both clinically relevant mechanisms of drug resistance to this class of agents. ELR510444 also shows potent antitumor activity in the MDA-MB-231 xenograft model with at least a 2-fold therapeutic window.|
Vinblastine sulfate, also called cellblastin, derived from C. roseus, as a microtubule disrupter and antineoplastic agent, it binds tubulin and disrupts microtu...
Eribulinmesilate can inhibit experimental metastasis of breast cancer cells by reversing phenotype from epithelial-mesenchymal transition (EMT) to mesenchymal-e...
7-xylosyltaxol is a taxol (Paclitaxel) derivative, which binds to tubulin and inhibits the disassembly of microtubules.
Flutax 1, the more soluble difluoro-fluorescein derivative with improved photostability Flutax-2, binds to the taxol microtubule binding site with high affinity...
XRP44X, under the IUPAC name [4-(3-chlorophenyl)piperazin-1-yl]-(5-methyl-2-phenylpyrazol-3-yl)methanone, as an inhibitor of Tubulin it indirectly inhibits Net ...
ELR510444 is a potent microtube disruptor with potential anticancer activity. ELR510444 has potent microtubule-disrupting activity, causing a loss of cellular m...
Harmine induces apoptosis and inhibits proliferation, migration and invasion of human gastric cancer cells, which may be mediated by down-regulation of COX-2 ex...
This active molecular is DM1 with a linker SMCC that can react with antibody to make antibody drug conjugate. DM1 is an antibody-conjugatable maytansinoid that ...
CMPD-1, also called MK2a Inhibitor, inhibits tubulin polymerisation. It inhibit p38α-mediated MK2a phosphorylation (apparent Ki = 330 nM).
Methylene Blue, whose brand name is Calbiochem, inhibits tau filament formation (IC50 = 1.9 μM) and soluble guanylyl cyclase.
Colchicine, a toxic plant-derived alkaloid extracted from plants of the genus Colchicum, inhibits microtubule polymerization (IC50 = 3.2 μM).
Docetaxel, also called Taxoltere metro, a semisynthetic side-chain analogue of taxol differing at two positions in its chemical structure, is an inhibitior of m...
ABT 751, also called E7010, is a a novel bioavailable tubulin-binding and antimitotic agent (in neuroblastoma: IC50= 0.6–2.6 μM; in non-neuroblastoma cell line...
Docetaxel is a cytotoxic agent, which is related to its ability to promote the formation of microtubule bundles and induce sustained mitotic arrest, followed by...
Dolastatin 10 is an inhibitior of microtubule disassembly (IC50= 1.2μM) and potently inhibits vincristine binding to tubulin in a noncompetitive manner ( Ki= 1....
Plinabulin is a vascular disrupting agent (VDA) against tubulin-depolymerizing with IC50 value of 9.8~18 nM in tumor cells under the development of Nereus Pharm...
MPC 6827 hydrochloride
MPC 6827 hydrochloride, the hydrochloride salt form of verubulin, inhibits of microtubule formation (IC50 = 1.5 - 3.4 nM). in vitro: inhibits polymerization of...
Dolastatin 10 trifluoroacetate inhibits tubulin polymerization and induces tubulin aggregation in vitro.
Podophyllotoxin, a kind of non-alkaloid toxin lignan extracted from the roots and rhizomes of Podophyllum plant, has been shown to inhibit the growth of various...
Vinblastine is inhibitor of nAChR and can inhibit the formation of microtubule. It is a natural alkaloid isolated from the plant Vinca rosea Linn. It binds to t...