溶解性 | 25°C: DMSO |
存贮条件 | 储存温度-20°C |
产品介绍 | EI1是EZH2选择性抑制剂,对野生型EZH2和EZH2 Y641F突变型的IC50分别为15 nM和13 nM。 |
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. Although 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, although 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 |
别名 | EI-1;EI 1;6-氰基-N-[(1,2-二氢-4,6-二甲基-2-氧代-3-吡啶基)甲基]-1-(1-乙基丙基)-1H-吲哚-4-甲酰胺;Ezh2 inhibitor;6-Cyano-N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-1-(1-ethylpropyl)-1H-indole-4-carboxamide |
EI1,EZH2抑制剂
EI1 (订货以英文为准)
编号:E125706
CAS号:1418308-27-6
分子式:C23H26N4O2
分子量:390.48
产品名称 | EI1 |
中文名称 | EI1,EZH2抑制剂 |
CAS号 | 1418308-27-6 |
分子式(M.F.) | C23H26N4O2 |
分子量(M.W.) | 390.48 |
储存条件 | 避光;-20°C储存 |
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