普罗塔克;PROTAC;;InformationdBET57 is a novel, potent and selective degrader of BRD4 BD1 based on the PROTAC technology with DC 50/5h of 500 nM. dBET57 is inactive on BRD4 BD2 .TargetsBRD4BD1 (Cell-free assay) 500 nM(DC50)
1. Si-Qi Jia, et al. The BRD4 Inhibitor dBET57 Exerts Anticancer Effects by Targeting Superenhancer-Related Genes in Neuroblastoma. J Immunol Res. 2022 Nov 16:2022:7945884. 2. Nowak RP, et al. Plasticity in binding confers selectivity in ligand-induced protein degradation. Nat Chem Biol. 2018 Jul;14(7):706-714.