| 产品描述: | 表观遗传阅读器域抑制剂;Epigenetic Reader Domain Inhibitors;;InformationBI 894999 BI 894999 is a potent and selective BET inhibitor with IC50 of 5 nM and 41 nM for the binding of BRD4-BD1 and BRD4-BD2 to acetylated histones, respectively. BI 894999 is highly selective for BRD2/3/4 and BRDT (Kd of 0.49-1.6 nM), with at least a 200-fold selectivity vs. BRD4-BD1.TargetsBET ; BRD4-BD1 (Cell-free assay); BRD4-BD2 (Cell-free assay) ; 5 nM; 41 nMIn vitroBI 894999 is highly active in AML cell lines, primary patient samples. BI 894999 targets super-enhancer-regulated oncogenes and other lineage-specific factors, which are involved in the maintenance of the disease state.In vivoBI 894999 is active as monotherapy in AML xenografts, and in addition leads to strongly enhanced antitumor effects in combination with CDK9 inhibitors.Cell Research(from reference)Cell lines:MV-4-11B, THP-1, MOLM-13 Concentrations:10 nM, 100 nM, various concentrations Incubation Time:4h, 24h, 79 h, 96 h |