| 规格: | 98% |
| 分子量: | 646.21 |
| 包装 | 价格(元) |
| 250mg | 电议 |
| 500mg | 电议 |
Background:
Dot1L-IN-1 is a highly potent, selective and structurally novel Dot1L inhibitor with a Ki of 2 pM.
Dot1L-IN-1 potently suppresses H3K79 dimethylation (IC50 = 3 nM), the direct product of the Dot1Lcatalyzed reaction, as well as the activity of the HoxA9 promoter (IC50 = 17 nM) in HeLa and Molm-13 cells, respectively[1]. Dot1L-IN-1 effectively inhibits proliferation of the human MLL-rearranged leukemia cell line MV4-11 carrying the oncogenic MLL-AF4 fusion (IC50 = 5 nM)[1].
[1]. M?bitz H, et al. Discovery of Potent, Selective, and Structurally Novel Dot1L Inhibitors by a Fragment Linking Approach. ACS Med Chem Lett. 2017 Feb 14;8(3):338-343.
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