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|---|---|---|
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| 250 mg | Get quote | |
| 500 mg | Get quote | |
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| Cat. No. : | HY-111390 |
| M.Wt: | 476.53 |
| Formula: | C27H24N8O |
| Purity: | >98 % |
| Solubility: | 10 mM in DMSO |
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.
IC50 & 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].
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