【产品介绍】：

产品名称 EI1 英文名称 EI1 规格或纯度 ≥96% 别名 EI-1;EI 1 英文别名 Ezh2 inhibitor；6-Cyano-N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-1-(1-ethylpropyl)-1H-indole-4-carboxamide 运输条件 超低温冰袋运输 生化机理 EI1 demonstrated potent, concentration-dependent inhibition of the enzymatic activity against both Ezh2 wild-type and Y641F mutant enzymes with IC50 of 15 ± 2 nM and 13 ± 3 nM, respectively. Althoμgh SAM is the common cofactor for all HMTs, EI1 showed remarkable selectivity against Ezh2 over other HMTs. EI1 dramatically inhibited the H3K27me3 and H3K27me2 levels in these cells in a dose-dependent manner, but H3K27me1 was largely unchanged. The effect was similar in these cell lines, althoμgh they have different basal H3K27me3 and H3K27me2 levels. For example, in WSU-DLCL2, SU-DHL6, and Karpas422 with Ezh2 mutations, the H3K27me3 level was much higher than that in DLBCL cells with wild-type Ezh2.Potent (IC 50 = 15 nM for wild-type enzyme; 13 nM for Y641F mutant enzyme) EZH2 inhibitor. Selective versus EZH1 (142-fold). Highly selective (>10,000-fold) against\xa0 a panel of 10 other human methyltransferases.CAS编号 1418308-27-6 溶解性 25°C: DMSO 储存温度 -20°C储存 分子量 390.48 分子式 C23H26N4O2 PubChem CID 72199293