EI1
货号：
19146-1mg 基本售价：
406.0 元 规格：
1 mg
产品信息
概述| 货号 | 19146-1mg |
| 描述 | The lysine methyltransferase EZH2 (KMT6), part of polycomb repressive complex 2 (PRC2), catalyzes trimethylation of lysine 27 on histone H3 (H3K27) and is involved in proliferation and aggressive cell growth associated with neoplastic cells.1 EI1 is an EZH2 inhibitor that has activity against both wild-type and Y641F mutant EZH2 (IC50s = 15 and 13 nM, respectively).2 It displays 90-fold selectivity for EZH2 over EZH1 and >10,000-fold over other lysine methyltransferases. EI1 blocks cellular H3K27 methylation and activates PRC2-specific gene expression.2 Inhibition of EZH2 by EI1 in diffused large B cell lymphoma cells carrying Y641 mutations results in decreased proliferation, cell cycle arrest, and apoptosis.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.Qi, W.,Chan, H.M.,Teng, L., et al. Selective inhibition of Ezh2 by a small molecule inhibitor blocks tumor cells proliferation. Proceedings of the National Academy of Sciences of the United States of America 109(52), 21360-21365 (2012).
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| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 390.5 |
| 分子式 | C23H26N4O2 |
| CAS号 | 1418308-27-6 |
| 稳定性 | ≥ 2 years |
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