(-)-JQ1
(-)-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.
≥98%
Yellowish, white crystalline powder
C23H25ClN4O2S
Filippakopoulos, P., et al. Nature. 2010 Dec 23;468(7327):1067-73
Application Reference:
1. A Cre-conditional MYCN-driven neuroblastoma mouse model as an improved tool for preclinical studies (2014)
2. BET bromodomain inhibitors block growth of pancreatic cancer cells in three-dimensional collagen (2014)
3. Dual kinase-bromodomain inhibitors for rationally designed polypharmacology (2014)
4. Bromodomain and extra-terminal domain (BET) proteins regulate melanocyte differentiation (2020)