JQ1 (+/-)

Aliases: JQ1 (+/-), JQ1 racemic, (6R,S)-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
Catalog No: 14066 Format: 25 mg ¥84,000 Buy
Catalog No: 14067 Format: 5 mg ¥22,000 Buy
Application: Bromodomains

Chemical Properties

MW = 457.0
C23H25ClN4O2S
CAS 1268524-70-4
>98% (TLC); NMR (Conforms)

Description

Pharmacology: JQ1 is a potent BET bromodomain inhibitor. (IC50 = 17.7, 32.6, 76.9 and 12942 nM respectively for BRD2 (N-terminal), BRD4 (C-terminal) and CREBBP (data for + isomer))(ref 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 (ref 1). Induces squamous differentiation in NMC cell lines and inhibits tumor growth in NMC xenografts (ref 2). Blocks inflammation and bone loss in periodontitis (ref 3). Displays reversible contraceptive effects in male mice (ref 4).
Note: This product is racemic (+/-) making the IC50 nominally 2-fold greater than literature values for the (+) isomer.

Contents

White powder. May be dissolved in DMSO (40 mg/ml); Ethanol (40 mg/ml).

Storage Conditions

Store desiccated as supplied at room temperature for up to 1 year. Store solutions at -20°C for up to 2 months.

References

1. P Filippakopoulos et al. Nature 2010, 468:1067
2. H Hermann et al. Oncotarget 2012, 3:1588
3. S Meng et al. Dent. Res. 2014, 93:657
4. MM Matzuk et al. Cell 2012, 150:673

 

Chemical Structure of JQ1 (+/-).