DATASHEET
Formulation
powder
Storage:
RT
Product Information:
Molecular Weight:457
Formula:C23H25ClN4O2S
Purity:>98%
Solubility:Soluble in DMSO (up to 60 mg/ml) or in Ethanol (up to 46 mg/ml)
Chemical Name:(6S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetic acid 1,1-dimethylethyl ester
Description:
JQ1 (+) is a 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 models1. Induces squamous differentiation in NMC cell lines and inhibits tumor growth in NMC xenografts2. Displays reversible contraceptive effects in male mice3. Blocks inflammation and bone loss in periodontitis4. Reverses CAR T cell extinction5.