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GSK126,EZH2甲基转移酶抑制剂

GSK126 （订货以英文为准）

编号：G124898
CAS号：1346574-57-9
分子式：C31H38N6O2
分子量：526.67
货号 品牌 包装 目录价 您的价格 库存 数量 购买
G124898-10mg 阿拉丁 10mg ¥803.90
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G124898-50mg 阿拉丁 50mg ¥2465.90
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G124898-5mg 阿拉丁 5mg ¥564.90
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产品名称 GSK126
中文名称 GSK126,EZH2甲基转移酶抑制剂
CAS号 1346574-57-9
分子式（M.F.） C31H38N6O2
分子量（M.W.） 526.67
储存条件 -20°C储存
溶解性25°C: DMSO
存贮条件储存温度-20°C
产品介绍GSK126是高活性，S-腺苷-蛋氨酸竞争性EZH2甲基转移酶抑制剂，Ki为0.5 nM。
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: Although 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
别名GSK-126;GSK 126;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
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