Description
(-)-JQ1 is the inactive stereoisomer of the potent, cell-permeable, small molecule bromodomain inhibitor (+)-JQ1 that competitively binds to acetyl-lysine recognition motifs. (+)-JQ1 competitively binds to the bromodomain displacing the BRD4 fusion oncoprotein from chromatin, which induces squamous differentiation and specific anti-proliferative effect in BRD4-dependent cell lines and patient-derived xenograft models. However, study results have shown that (-)-JQ1 fails to significantly interact with any bromodomain tested and exhibits inhibition against BRD4(1) with and IC50 of 10,000 nM.
Alias
UNQ262/PRO299, UNQ26
Appearance
Yellowish, white crystalline powder.
Molecular Weight
457.0 kDa
Stability
Store at or below -80°C. Stable for less than 6 months when stored as directed.
Synonyms
(R)-tert-butyl 2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetate
Molecular Formula
C23H25ClN4O2S
Solubility
Soluble in DMSO or ethanol at 100 mM