Biochemicals & reagents
1) Filippakopoulos et al. (2010), Selective inhibition of BET bromodomains; Nature, 468 1067
JQ1 (+/-) is a potent BET bromodomain inhibitor with an IC50 = 17.7, 32.6, 76.9 and 12942 nM for BRD2 (N-terminal (N)), BRD4 (C-terminal (C)), BRD4 (N) and CREBBP respectively. The 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 (1).