I-BET151

I-BET151 is an inhibitor of bromodomain and extra terminal (BET) family proteins. BET proteins recognize acetylated lysine residues via their 2 bromodomains (Gallenkamp et al.). I-BET151 inhibits BRD2, BRD3, and BRD4 with IC₅₀ values of 0.5, 0.25, and 0.79 µM, respectively (Kline et al.; Vidler et al.; Hewings et al.; Dawson et al. 2012).

REPROGRAMMING

• Enhances reprogramming of mouse fibroblasts to neurons, in combination with ISX-9, Forskolin, and CHIR99021 (Li et al.)

CANCER RESEARCH

• Induces early cell cycle arrest and apoptosis in human and mouse MLL-fusion leukemia cell lines by blocking transcription of key genes including BCL2, C-MYC, and CDK6 (Dawson et al. 2011).