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| 品牌 | absin | CAS | 1346574-57-9 |
|---|---|---|---|
| 分子式 | C31H38N6O2 | 纯度 | ＞98% |
| 分子量 | 526.67 | 货号 | abs810322 |
| 规格 | 5mg | 供货周期 | 现货 |
| 主要用途 | is a potent, highly selective, S-adenos | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
GSK126 1346574-57-9
| 产品描述 | |
| 描述 | GSK126 is a potent, highly selective, S-adenosyl-methionine-competitive, small-molecule inhibitor of EZH2 methyltransferase with Ki value of 0.5 nM. |
| 纯度 | >98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | EZH2 inhibitor; GSK-126; GSK 126；GSK2816126A |
| 外观 | White to yellow Solid |
| 可溶性/溶解性 | DMSO : 12.5 mg/mL (23.73 mM) |
| 生物活性 | |
| 靶点 | EZH2 |
| In vitro(体外研究) | In vitro, GSK126 most potently inhibits H3K27me3, followed by H3K27me2 in both EZH2 wild-type and mutant DLBCL cell lines. GSK126 also effectively inhibits the proliferation of EZH2 mutant DLBCL cell lines, and induces transcriptional activation of EZH2 target genes in sensitive cell lines. In A687V EZH2-mutant cells, GSK126 treatment results in a global decrease in H3K27me3, robust gene activation, caspase activation, and decreased proliferation. In parental H2087 cells, GSK126 inhibits the expression of VEGF-A and phosphorylated Ser(473)-AKT, and thus causes the inhibition of cell proliferation, migration and metastasis. |
| In vivo(体内研究) | In mice bearing KARPAS-422 and Pfeiffer xenografts, GSK126 (150 mg/kg/d, i.p.) decreases global H3K27me3, increases gene expression, and thus causes marked tumour regression. |
| 研究领域 | |
| 研究领域 | EpigeneticsChromatin RemodelingPolycomb SilencingPRC2 Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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