| 货号 | 16173-500ug |
| 描述 | DOT1L is a protein methyltransferase. It is the only enzyme known to methylate histone 3 at lysine 79, 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 EPZ004777 is a potent inhibitor of DOT1L (IC50 = 400 pM) that selectively kills mixed lineage leukemia (MLL) cells in vitro and prolongs survival in an MLL xenograft mouse model.3,4,5,6 It displays >1,000-fold selectivity for DOT1L relative to a panel of histone methyltransferases.3 DOT1L inhibition by EPZ004777 has also been shown to accelerate the reprogramming of somatic cells into induced pluripotent stem cells.7 |
| 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.Daigle, S.R.,Olhava, E.J.,Therkelsen, C.A., et al. Selective killing of mixed lineage leukemia cells by a potent small-molecule DOT1L inhibitor. Cancer Cell. 20(1), 53-65 (2011). 4.Chen, L.,Deshpande, A.J.,Banka, D., et al. Abrogation of MLL-AF10 and CALM-AF10-mediated transformation through genetic inactivation or pharmacological inhibition of the H3K79 methyltransferase Dot1l. Leukemia 27(4), 813-822 (2013). 5.Deshpande, A.J.,Chen, L.,Fazio, M., et al. Leukemic transformation by the MLL-AF6 fusion oncogene requires the H3K79 methyltransferase Dot1l. Blood 121(13), 2533-2541 (2013). 6.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). 7.Ye, J.,Ge, J.,Zhang, X., et al. Pluripotent stem cells induced from mouse neural stem cells and small intestinal epithelial cells by small molecule compounds. Cell Research 26, 34-45 (2016). | |
| 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 | 585.7 |
| 分子式 | C28H41N7O4 • CH2O2 |
| 稳定性 | ≥ 2 years |
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