acid 1,1-dimethylethyl ester
JQ1 is a potent BET bromodomain inhibitor. 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). 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. Induces
squamous differentiation in NMC cell lines and inhibits tumor growth in NMC
xenografts. Blocks inflammation and bone loss in periodontitis4.
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.
Physical Properties: White powder
Analysis: >98% (TLC); NMR
Solubilization: May be dissolved in DMSO (40 mg/ml); or ethanol (40 mg/ml)
Storage: Store desiccated as
supplied at ambient temperature for up to 1 year. Store solutions at -20°C for
up to two months.
Amount: 5 mg