Biological Activity
i-bet 151 dihydrochloride is a bet bromodomain inhibitor that prevents bet from recruiting to chromatin. i-bet 151 induces mll-fusion leukemia cell line apoptosis and g0 / g1 cell cycle arrest in vitro, and reduces bcl2 expression in nomo1 cells. i-bet 151 improves the survival rate of two kinds of mll fusion leukemia mice, and enhances the differentiation of human ipscs into megakaryocytes.[1]. malherbe p, masciadri r, norcross r d, et al. characterization of (r,s)-5,7-di-tert-butyl-3-hydroxy-3-trifluoromethyl-3h-benzofuran-2-one as a positive allosteric modulator of gabab receptors. british journal of pharmacology, 2008, 154(4): 797.
