纯度:98% by HPLC NMR conforms
分子式:C23H25ClN4O2S
分子量:456.99
溶剂:DMSO (up to 60 mg/ml) or in Ethanol (up to 46 mg/ml)
性状:White solid
存储:-20°C
Activity (short version):BET Bromodomain inhibitor
Function / Pharmacology:Potent BET bromodomain inhibitor and is the active isomer. IC50 = 17.7, 32.6, 76.9 and 12942 nM respectively for BRD2 (N-terminal (N)), BRD4 (C-terminal (C)), BRD4 (N) and CREBBP respectively (data for + isomer).1 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.1 Induces squamous differentiation in NMC cell lines and inhibits tumor growth in NMC xenografts.2 Displays reversible contraceptive effects in male mice.3 Blocks inflammation and bone loss in periodontitis.4 Reverses CAR T cell extinction.5