SGC0946
货号：
13967-50mg 基本售价：
10682.0 元 规格：
50 mg
产品信息
概述| 货号 | 13967-50mg |
| 描述 | DOT1L is a protein methyltransferase (PMT). It is the only enzyme known to methylate histone 3 at lysine 79 (H3K79), where it catalyzes mono-, di-, and trimethylation.1 Proper DOT1L function is necessary for transcriptional activation of many genes, DNA damage repair, and cell cycle regulation.2 SGC0946 is a potent inhibitor of DOT1L (IC50 = 0.3 nM) developed by the Structural Genomics Consortium (SGC). It is over 100-fold selective over other PMTs. It is active in cells, reducing H3K79 dimethylation in A431 and MCF10A cells (IC50s = 2.6 and 8.8 nM, respectively). SGC0946 is a brominated analog of EPZ004777, an S-adenosylmethionine-competitive inhibitor of DOT1L.3 Both SGC0946 and EPZ004777 selectively kill mixed lineage leukemia (MLL) cells, in which DOT1L is aberrantly localized via interaction with an oncogenic MLL fusion protein.3 |
性能| 供应商 | Cayman |
| 应用文献 |
1.Bernt, K.M. and Armstrong, S.A. A role for DOT1L in MLL-rearranged leukemias. Epigenomics 3(6), 667-670 (2011).
2.Nguyen, A.T.,He, J.,Taranova, O., et al. Essential role of DOT1L in maintaining normal adult hematopoiesis. Cell Research 21(9), 1370-1373 (2011).
3.Yu, W.,Chory, E.J.,Wernimont, A.K., et al. Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors. Nat.Commun. 3, 1-12 (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 | 618.6 |
| 分子式 | C28H40BrN7O4 |
| CAS号 | 1561178-17-3 |
| 稳定性 | ≥ 2 years |
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