EPZ005687
货号：
13966-50mg 基本售价：
6636.0 元 规格：
50 mg
产品信息
概述| 货号 | 13966-50mg |
| 描述 | EPZ005687 is a potent, selective inhibitor of the lysine methyltranferase EZH2 (Ki = 24 nM), the enzymatic subunit of polycomb repressive complex 2 (PRC2).1 It acts competitively with the EZH2 substrate S-adenosylmethionine.1,2,3 EPZ005687 has greater than 500-fold selectivity against 15 other protein methyltransferases and has 50-fold selectivity against EZH1.1 It blocks trimethylation of the PRC2 target histone 3 lysine 27 (IC50 = 80 nM), decreasing the proliferation of lymphoma cells carrying mutant, but not wild-type, EZH2.1 |
性能| 供应商 | Cayman |
| 应用文献 |
1.Knutson, S.K.,Wigle, T.J.,Warholic, N.M., et al. A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells. Nature Chemical Biology 8(11), 890-896 (2012).
2.Wigle, T.J. and Copeland, R.A. Drugging the human methylome: An emerging modality for reversible control of aberrant gene transcription. Current Opinion in Chemical Biology 17(3), 369-378 (2013).
3.Konze, K.D.,Ma, A.,Li, F., et al. An orally bioavailable chemical probe of the lysine methyltransferases EZH2 and EZH1. ACS Chemical Biology 8, 1324-1334 (2013).
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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 | 539.7 |
| 分子式 | C32H37N5O3 |
| CAS号 | 1396772-26-1 |
| 稳定性 | ≥ 2 years |
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