| 产品描述: | 组蛋白乙酰转移酶抑制剂;Histone Acetyltransferase Inhibitors;NEO2734 (EP31670) 是一种新型的、 p300/CBP 和 BET bromodomain 的选择性双重抑制剂,对应的IC50值均<30 nM。;InformationNEO2734 NEO2734 (EP31670) is a novel, orally active and selective dual inhibitor of p300/CBP and BET bromodomain with IC50 of both <30 nM.Targetsp300/CBP (Cell-free assay); BET (Cell-free assay) <30 nM; <30 nMIn vitroTreatment of NMC cells with the novel dual p300/CBP and BET bromodomain–selective inhibitor, NEO2734, potently inhibits growth and induces differentiation of NMC cells in vitro; findings that correspond with potentiated transcriptional effects from combined BET and p300 bromodomain inhibition.In vivoIn three disseminated NMC xenograft models, NEO2734 provides greater growth inhibition, with tumor regression and significant survival benefit seen in two of three models, compared with a lead clinical BET inhibitor or “standard” chemotherapy.Cell Research(from reference)Cell lines:NUT carcinoma patient cell lines (TC-797, 14169, 10-15, PER-403) Concentrations:1 μM Incubation Time:24 h |