Dot1L-IN-1 |
| カタログ番号GC33208 |
Dot1L-IN-1 は、2 pM の Ki を持つ、非常に強力で選択的で構造的に新規な Dot1L 阻害剤です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2088518-50-5
Sample solution is provided at 25 µL, 10mM.
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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.
Average Rating: 5 (Based on Reviews and 34 reference(s) in Google Scholar.)
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