| 货号 | 4904/50 |
| 别名 | N-[(1,2-Dihydro-6-methyl-2-oxo-4-pr |
| 供应商 | Tocris |
| 生物活性 | Potent and SAM-competitive EZH2/EZH1 lysine methyltransferase inhibitor (IC50 values are 2 and 45 nM respectively). Selective for EZH2/EZH1 over a panel of other methyltransferases and non-epigenetic targets. Reduces H3K27me3 levels in vitro. Prolongs survival of MLL-AF9 bearing mice. Orally bioavailable. |
| 运输条件 | Blue Ice |
| 存放说明 | 4℃ |
| 纯度 | >99 % |
| 计算分子量 | 569.74 |
| 分子式 | C33H43N7O2 |
| 可溶性/溶解性 | Soluble to 100 mM in 1eq. HCl and to 20 mM in DMSO |
| 参考文献 | Xuet al (2015) Selective inhibition of EZH2 and EZH1 enzymatic activity by a small molecule suppresses MLL-rearranged leukemia. Blood 125 346. PMID: 25395428. Konzeet al (2013) An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1. ACS Chem.Biol. 8 1324. PMID: 23614352. |