产品描述:
(+)-JQ1 (free acid) is an inhibitor of bromodomain and extra terminal domain (BET) family proteins (Kds = 128, 59.5, 49.0, and 190 nM for JQ1 binding to bromodomains of BRD2, BRD3, BRD4, and BRDT, respectively), blocking their interaction with acetylated histones.{19044,28490} Enantiomerically pure (+)-JQ1 (Item No. 11187) binds to BRD4 bromodomains 1 and 2 with Kd values of ~50 and 90 nM, respectively, whereas the (−)-JQ1 (Item No. 11232) stereoisomer has no appreciable affinity to BET bromodomains.{19044} JQ1 has been used as a chemical probe to investigate the role of BET bromodomains in the transcriptional regulation of oncogenesis.{19044,28490,20263,20272,20182} See the Structural Genomics Consortium (SGC) website for more information.