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)