JQ1 (+/-), Bromodomain inhibitor (TBI1361)

Description

Product Details

Formal Name: (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

Molecular Formula: C₂₃H₂₅ClN₄O₂S

Formula Weight: 457.00

CAS Number: 1268524-69-1

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to 9 mg/ml) or in Ethanol (up to 9 mg/ml) with warming.

Storage: RT

Stability: ≥ 1 year.

Applications

Bromodomain inhibitor

Functions

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. 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 establishing proof-of-concept for targeting protein-protein interactions of epigenetic readers.

Application Procedures

First dissolved in DMSO (up to 9 mg/ml) or in Ethanol (up to 9 mg/ml) with warming, then diluted to aqueous buffer. Solutions in DMSO or ethanol may be stored at -20° for up to 2 months.