Name | Dot1L-IN-2 |
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Description | Dot1L-IN-2 is a potent, selective and orally bioavailable inhibitor of Dot1L (a histone methyltransferase), with an IC50 and Ki of 0.4 nM and 0.08 nM, respectively. |
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Related Catalog | |
Target |
IC50: 0.4 nM (Dot1L)[1] Ki: 0.08 nM (Dot1L)[1] |
In Vitro | Dot1L-IN-2 is a potent, selective Dot1L inhibitor, with an IC50 and Ki of 0.4 nM and 0.08 nM, respectively. Dot1L-IN-2 potently inhibits H3K79 dimethylation (IC50, 16 nM), and blocks the activity of the HoxA9 promoter (IC50, 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 (IC50, 128 nM)[1]. |
References |
Molecular Formula | C27H24N8O |
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Molecular Weight | 476.53 |