| 货号 | 17285-25mg |
| 描述 | Protein arginine methyltransferases (PRMTs) target nuclear and cytoplasmic substrates and can alter protein actions and gene expression.1,2 PRMT5, which can methylate histones H2A, H3, and H4, ribonucleoproteins, and other proteins, is upregulated in several human cancers, including lymphomas.3 Moreover, suppression of PRMT5 expression induces lymphoma cell death.4 EPZ015666 is a potent, orally bioavailable inhibitor of PRMT5 (Ki = 5 nM).5 It displays more than 20,000-fold selectivity for PRMT5 over other PMTs. EPZ015666 acts by blocking the association of PRMT5 with methylosome protein 50, which is necessary for the formation of an active methyltransferase complex. EPZ015666 (100 mg/kg twice daily) blocks the growth of mantle cell lymphoma Z-138 xenografts, without significant body weight loss, in mice.5 |
| 别名 | GSK3235025; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Bissinger, E.M.,Heinke, R.,Sippl, W., et al. Targeting epigenetic modifiers: Inhibitors of histone methyltransferases. Med.Chem.Commun. (2010). 2.Copeland, R.A.,Solomon, M.E., and Richon, V.M. Protein methyltransferases as a target class for drug discovery. Nature Reviews.Drug Discovery 8, 724-732 (2009). 3.Li, Y.,Chitnis, N.,Nakagawa, H., et al. PRMT5 is required for lymphomagenesis triggered by multiple oncogenic drivers. Cancer Discov. 5, 288-303 (2015). 4.Chung, J.,Karkhanis, V.,Tae, S., et al. Protein arginine methyltransferase 5 (PRMT5) inhibition induces lymphoma cell death through reactivation of the retinoblastoma tumor suppressor pathway and polycomb repressor complex 2 (PRC2) silencing. The Journal of Biological Chemisty 288(49), 35534-35547 (2013). 5.Chan-Penebre, E.,Kuplast, K.G.,Majer, C.R., et al. A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models. Nature Chemical Biology 11(6), 432-437 (2015). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 383.4 |
| 分子式 | C20H25N5O3 |
| CAS号 | 1616391-65-1 |
| 稳定性 | ≥ 2 years |
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