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An inhibitor of tubulin polymerization
Batabulin is an inhibitor of tubulin polymerization.1 It covalently binds to cysteine 239 (Cys239) of the β1, β2, and β4 tubulin isotypes and inhibits polymerization of bovine brain tubulin (IC50 = 2 ?M) in cell-free assays. Batabulin (30, 100, and 300 nM) induces cytoskeletal collapse and cell cycle arrest at the G2/M phase in MCF-7 breast cancer cells. It is cytotoxic against a panel of drug-sensitive and -resistant cancer cell lines (IC50s = 11-165 nM). Batabulin (40 mg/kg) reduces tumor volume in CCRF CEM lymphoblastic leukemia and CEM/VBL100 multidrug-resistant lymphoblastic leukemia mouse xenograft models.
1.Shan, B., Medina, J.C., Santha, E., et al.Selective, covalent modification of β-tubulin residue Cys-239 by T138067, an antitumor agent with in vivo efficacy against multidrug-resistant tumorsProc. Natl. Acad. Sci. USA96(10)5686-5691(1999)
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