【产品介绍】：

产品名称 UNC1999 英文名称 UNC1999 规格或纯度 ≥98% 别名 UNC-1999;UNC 1999 英文别名 UNC-1999;UNC 1999;n-((1,2-dihydro-6-methyl-2-oxo-4-propyl-3-pyridinyl)methyl)-1-(1-methylethyl)-6-(6-(4-(1-methylethyl)-1-piperazinyl)-3-pyridinyl)-1h-indazole-4-carboxamide; 1-Isopropyl-6-(6-(4-isopropylpiperazin-1-yl)pyridin-3-yl)-N-((6-methyl-2-oxo-4-p 运输条件 超低温冰袋运输 生化机理 UNC1999 was the first orally bioavailable EZH2 inhibitor that has high in vitro potency for wild-type and mutant EZH2 as well as EZH1, UNC1999 was highly selective for EZH2 and EZH1 over a broad range of epigenetic and non-epigenetic targets, competitive with the cofactor SAM and non-competitive with the peptide substrate. This inhibitor potently reduced H3K27me3 levels in cells and selectively killed diffused large B cell lymphoma cell lines harboring the EZH2Y641N mutant. Importantly, UNC1999 was orally bioavailable in mice, making this inhibitor a valuable tool for investigating the role of EZH2 and EZH1 in chronic animal studies. We also designed and synthesized UNC2400, a close analogue of UNC1999 with potency >1,000-fold lower than that of UNC1999 as a negative control for cell-based studies.Potent, selective cell-permeable dual inhibitor of EZH2 and EZH1 methyltransferase inhibitor (IC 50 = 45 nM and 2 nM respectively) (Konze et al.\xa0) . Inhibits H3K27 methylation (IC 50 = 124 nM, MCF10A cells).CAS编号 1431612-23-5 溶解性 DMSO 储存温度 -20°C储存 分子量 569.74 分子式 C33H43N7O2 PubChem CID 72551585