JQ1 (+/-)
Bromodomain inhibitor / 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 readers1.
Biochemicals & reagents
1268524-69-1
1) Filippakopoulos et al. (2010), Selective inhibition of BET bromodomains; Nature, 468 1067
RT
TARGET: Bromodomain -- PATHWAY: Chromatin; Posttranslational modification; Proliferation -- RESEARCH AREA: Epigenetics -- DISEASE AREA: Cancer