Bromodomain inhibitor. SARS-CoV-2 transmembrane protein E binds to the bromodomain-containing proteins BRD2 and BRD4. Gordon et al. bioRxiv, Mar 23 2020, https://doi.org/10.1101/2020.03.22.002386.
- Applications:Tool compound
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 (data for + isomer) (1). 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 (1). It also induces squamous differentiation in NMC cell lines and inhibits tumor growth in NMC xenografts (2), blocks inflammation and bone loss in periodontitis (4) and displays reversible contraceptive effects in male mice (3).