JQ1 (+)
BET Bromodomain inhibitor / Potent BET bromodomain inhibitor and is the active isomer. 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 (data for + isomer).1 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 Induces squamous differentiation in NMC cell lines and inhibits tumor growth in NMC xenografts.2 Displays reversible contraceptive effects in male mice.3 Blocks inflammation and bone loss in periodontitis.4 Reverses CAR T cell extinction.5
Biochemicals & reagents
1268524-70-4
Filippakopoulos et al. (2010), Selective inhibition of BET bromodomains; Nature, 468 1067 Herrmann et al. (2012), Small-molecule inhibition of BRD4 as a new potent approach to eliminate leukemic stem- and progenitor cells in acute myeloid leukemia AML; Oncotarget, 3 1588 Matzuk et al. (2012), Small-molecule inhibition of BRDT for male contraception; Cell 150 673 Meng et al. (2014), BET Inhibitor JQ1 Blocks Inflammation and Bone Destruction;, J. Dent. Res. 93 657 Kong et al. (2021), BET bromodomain protein inhibition reverses chimeric antigen receptor extinction and reinvigorates exhausted T cells in chronic lymphocytic leukemia; J. Clin. Invest., 131 e145459
-20°C
TARGET: Bromodomain -- PATHWAY: Chromatin; Posttranslational modification; Proliferation -- RESEARCH AREA: Epigenetics -- DISEASE AREA: Cancer; Inflammation