Catalog No.: PC-43414Not For Human Use, Lab Use Only.
I-BET151 (GSK1210151A) is a potent, selective BET bromodomain inhibitor with IC50 of 0.5, 0.25 and 0.79 uM for BRD2, BRD3 and BRD4 in FP assays, shows no effect on the 23 other bromodomain proteins including MLL.
I-BET151 (GSK1210151A) is a potent, selective BET bromodomain inhibitor with IC50 of 0.5, 0.25 and 0.79 uM for BRD2, BRD3 and BRD4 in FP assays, shows no effect on the 23 other bromodomain proteins including MLL.
I-BET151 (GSK1210151A) demonstrates potent efficacy against cell lines harbouring different MLL-fusions (MOLM13 cell IC50=120 nM, MV4:11 cell IC50=26 nM).
I-BET151 (GSK1210151A) induces early cell cycle arrest and apoptosis, selectively abrogates BRD3/4 recruitment to chromatin。
I-BET151 (GSK1210151A) shows significant therapeutic value and survival benefit in mouse models of murine MLL-AF9 and human MLL-AF4 leukaemia.
