A selective, SAM-competitive small molecule inhibitor of EZH2 methyltransferase activity (Ki = 0.57 nM; IC50 = 9.9 nM versus that of EZH1: Ki = 89 nM; IC50 = 680 nM); inhibits global H3K27me3 levels, inhibiting the proliferation of EZH2 mutant DLBCL cell lines (IC50 = 28-61 nM) as well as the growth of EZH2 mutant DLBCL xenografts in mice receiving a daily dose of 50 mg/kg
Size
5 mg
Concentration
n/a
Applications
n/a
Other Names
histone H3-lysine H3 H3K27 methyltransferase EZH2 inhibitor inhibit HMT cancer GSK-126 S-adenosyl-methionine SAM S-adenosyl methionine S-adenosylmethionine trimethylation trimethylate PRC2 PRC-2 gene DLBCL xenografts chromatin research epigenetic modification KMT6