Active Motif's JQ1 is a potent BET bromodomain inhibitor. (IC50 = 17.7, 32.6, 76.9 and 12942 nM respectively for BRD2 (N-terminal), BRD4 (C-terminal) and CREBBP (data for + isomer)). Competitive binding by JQ1 displaces the BRD4 fusion oncoprotein from chromatin, prompting squamous differentiation and specific antiproliferative effects in BRD4-dependent cell lines and patient-derived xenograft models. JQ1 induces squamous differentiation in NMC cell lines and inhibits tumor growth in NMC xenografts It also blocks inflammation and bone loss in periodontitis, and displays reversible contraceptive effects in male mice. Note: This product is racemic (+/-), making the IC50 nominally 2-fold greater than literature values for the (+) isomer.
