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
BET Bromodomain inhibitor
Molecular Weight:
456.99
Purity:
98% by HPLC NMR conforms
Form:
White solid
CAS Number:
[1268524-70-4]
Formula:
C23H25ClN4O2S
Application Notes:
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
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