Dot1L-IN-2
| 中文名称 | Dot1L-IN-2 |
|---|---|
| 中文同义词 | 化合物 T11082 |
| 英文名称 | Dot1L-IN-2 |
| 英文同义词 | Dot1L-IN-2;2,4-Pyrimidinediamine, N4-methyl-N2-[2-methyl-1-[2-[(3-methyl-3H-imidazo[4,5-b]pyridin-6-yl)oxy]phenyl]-1H-indol-6-yl]-;Dot1L IN 2,Dot1LIN2,Dot-1L-IN-2 |
| CAS号 | 1940206-71-2 |
| 分子式 | C27H24N8O |
| 分子量 | 476.53 |
| EINECS号 | |
| 相关类别 | 对照品 |
| Mol文件 | 1940206-71-2.mol |
| 结构式 |  |
Dot1L-IN-2 性质
| 沸点 | 681.6±65.0 °C(Predicted) |
|---|---|
| 密度 | 1.36±0.1 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | 溶于二甲基亚砜 |
| 酸度系数(pKa) | 6.81±0.10(Predicted) |
Dot1L-IN-2 是一种有效的，选择性的，可口服的 Dot1L (一种 histone methyltransferase)，IC50 值和 Ki 值分别为 0.4 nM 和 0.08 nM。
IC50: 0.4 nM (Dot1L)
Ki: 0.08 nM (Dot1L)
Dot1L-IN-2 is a potent, selective Dot1L inhibitor, with an IC 50 and K i of 0.4 nM and 0.08 nM, respectively. Dot1L-IN-2 potently inhibits H3K79 dimethylation (IC 50 , 16 nM), and blocks the activity of the HoxA9 promoter (IC 50 , 340 nM) in cellular systems. Dot1L-IN-2 also dramatically suppresses proliferation of the human MLL-rearranged leukemia cell line MV4-11 carrying the oncogenic MLL-AF4 fusion (IC 50 , 128 nM).