GSK126
货号：
15415-1mg 基本售价：
686.0 元 规格：
1 mg
产品信息
概述| 货号 | 15415-1mg |
| 描述 | The histone H3 lysine 27 (H3K27) methyltransferase EZH2 plays an important role in regulating gene expression, and its aberrant activity is linked to the onset and progression of cancer.1 GSK126 is a selective, S-adenosyl-methionine-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).2 It is more than 1,000-fold selective for EZH2 over other histone methyltranferases, including both SET-domain-containing and non-SET-domain-containing methyltransferases.2 At concentrations of 7-252 nM, it has been shown to inhibit global H3K27 trimethylation levels and to reactivate silenced PRC2 target genes.2 Furthermore, GSK126 can inhibit 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.2 |
性能| 供应商 | Cayman |
| 应用文献 |
1.Simon, J.A. and Lange, C.A. Roles of the EZH2 histone methyltransferase in cancer epigenetics. Mutation Research 647, 21-29 (2008).
2.McCabe, M.T.,Ott, H.M.,Ganji, G., et al. EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations. Nature 492(7427), 108-112 (2012).
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| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 526.7 |
| 分子式 | C31H38N6O2 |
| CAS号 | 1346574-57-9 |
| 稳定性 | ≥ 2 years |
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