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JQ1 (R,S)

Your Price:$80.00
In Stock.
Part Number:EI-BRD-002

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JQ-1 (+/-)   

(6R,S)-4-(4-Chlorophenyl)-2,3,9-trime?thyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]di?azepine-6-acetic 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

MW=457.0          C23H25ClN4O2S 

Analysis:  >98% (TLC); NMR (Conforms)

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 

With the largest functional kinase activity assay panel in the industry, RBC provides kinase, epigenetic, and other profiling services to over 590 companies worldwide. RBC specializes in custom assay conditions, high quality reproducible data, and outstanding service.

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