背景介绍 Bromodomains have an important role in the targeting of chromatin-modifying enzymes to specific sites, including methyltransferases, HATs and transcription factors and regulate diverse biological processes from cell proliferation and differentiation to energy homeostasis and neurological processes. Optimized to retain excellent BET target potency and selectivity while enhancing the in vivo pharmacokinetics and terminal half-life to enable prolonged in vivo studies. 产品介绍 I-BET151(GSK1210151A) is a BET bromodomain inhibitor. I-BET151 displays potent binding affinity to BRD2, BRD3 and BRD4 with Kd of 0.02-0.1 µM. I-BET151 (0.5 or 5 µM) inhibits the binding of BETs (BRD2, BRD3, BRD4, and BRD9) but not the binding of 23 other bromodomain proteins. I-BET151 also blocks recruitment of BET to chromatin.