产品描述
| 溶解性 | DMSO |
| 存贮条件 | 储存温度-20°C |
| 产品介绍 | EPZ005687是一种有效的，选择性<的b>EZH2抑制剂，Ki为24 nM，比作用于EZH1选择性高50倍，比作用于15种其他蛋白甲基转移酶选择性高500倍。 |
| 生化机理 |
EZH2 is the catalytic subunit of the polycomb repressive complex 2 (PRC2) and is involved in repressing gene expression through methylation of histone H3 on lysine 27 (H3K27). EZH2 overexpression is implicated in tumorigenesis and correlates with poor prognosis in several tumour types. EPZ005687, a potent inhibitor of EZH2 (K(i) of 24 nM). EPZ005687 reduces H3K27 methylation in various lymphoma cells; this translates into apoptotic cell killing in heterozygous Tyr641 or Ala677 mutant cells, with minimal effects on the proliferation of wild-type cells. |
| 别名 | EPZ-005687;EPZ 005687;EPZ-005687;EPZ 005687;1-Cyclopentyl-N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-6-[4-(4-morpholinylmethyl)phenyl]-1H-indazole-4-carboxamide |
