【产品介绍】：

产品名称 GSK126 英文名称 GSK126 规格或纯度 ≥98% 别名 GSK-126;GSK 126 英文别名 EZH2 inhibitor;GSK-126;GSK 126;N-[(4,6-Dimethyl-2-oxo-1,2-dihydro-3-pyridinyl)methyl]-3-methyl-1-((1S)-1-methylpropyl)-6-[6-(1-piperazinyl)-3-pyridinyl]-1H-indole-4-carboxamide 运输条件 超低温冰袋运输 生化机理 Description:IC50 Value: 0.5nM (Ki)GSK126, a potent, highly selective, S-adenosyl-methionine-competitive, small-molecule inhibitor of EZH2 methyltransferase activity, decreases global H3K27me3 levels and reactivates silenced PRC2 target genes. GSK126 may provide a promising treatment for EZH2 mutant lymphoma.in vitro: Althoμgh GSK126 induced loss of H3K27me3 independent of EZH2 mutation status, six of seven lymphoma cell lines sensitive to GSK126 treatment were EZH2-mutation(+), while only two of 11 lymphoma cell lines less sensitive to GSK126 were EZH2-mutation(+) [1]. SCLC cell lines were then treated with a selective EZH2 inhibitor, GSK126, at different doses of 0.5, 2, and 8 μM [1].in vivo: GSK126 effectively inhibits the proliferation of EZH2 mutant DLBCL cell lines and markedly inhibits the growth of EZH2 mutant DLBCL xenografts in mice [2].Clinical trial: N/A .Potent inhibitor EZH2 methyltransferase inhibitor (K i = 93 pM). Selective (>150-fold) versus EZH1. Greater than 1000-fold selective against a panel of 20 other human methyltransferases including both SET-domain-containing and non-SET-domain-containing meCAS编号 1346574-57-9 溶解性 25°C: DMSO 储存温度 -20°C储存 分子量 526.67 分子式 C31H38N6O2 PubChem CID 68210102