EZH2 (Enhancer of zeste homolog 2) is a histone-lysine N-methyltransferase enzyme EZH2 that participates in DNA methylation and, ultimately, transcriptional repression. EZH2 catalyzes the addition of methyl groups to histone H3 at lysine 27, by using the cofactor S-adenosyl-L-methionine. Methylation activity of EZH2 facilitates heterochromatin formation thereby silences gene function. Remodeling of chromosomal heterochromatin by EZH2 is also required during cell mitosis. Mutation or over-expression of EZH2 has been linked to many forms of cancer.
  • GSK126 EY1820

    GSK126是一种高活性,S-腺苷-蛋氨酸竞争性EZH2甲基转移酶抑制剂,Ki为0.5 nM。

  • EPZ005687 EY1515

    EPZ-005687是EZH2选择性抑制剂,Ki为24 nM,比作用于EZH1选择性高50倍,对其它15种甲基转移酶有500倍的选择性。

  • 3-Deazaneplanocin A HCl EY1110

    3-Deazaneplanocin A(DZNep)盐酸盐能抑制EZH2蛋白胞内增强子,具有抗肿瘤活性。

  • GSK343 EY0356

    GSK343是一种选择性EZH2抑制剂,IC50为4 nM,比作用于EZH1选择性高60倍,比作用于其他组蛋白甲基转移酶选择性高1000倍以上。

  • Current page1, Total Pages1, Total Record4 First Prev 1 Next Last Goto