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Chemical Structure : MAK683
CAS No.: 1951408-58-4
Catalog No.: PC-35591Not For Human Use, Lab Use Only.
MAK683 (MAK-683) is a potent and selective EED inhibitor with biochemical IC50 of 9 nM, and allosteric inhibitor of polycomb repressive complex 2 (PRC2), selectively binds to the domain of EED that interacts with H3K27me3).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $138 | In stock | |
| 10 mg | $218 | In stock | |
| 25 mg | $388 | In stock | |
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| 100 mg | Get quote |
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MAK683 (MAK-683) is a potent and selective EED inhibitor with biochemical IC50 of 9 nM, and allosteric inhibitor of polycomb repressive complex 2 (PRC2), selectively binds to the domain of EED that interacts with H3K27me3).
MAK683 leads to a conformational change in the EED H3K27me3-binding pocket and prevents the interaction of EED with the histone methyltransferase enhancer zeste homolog 2 (EZH2).
MAK683 inhibits tumor cell proliferation in EZH2-mutated and PRC2-dependent cancer cells.
| M.Wt | 376.39 | |
| Formula | C20H17FN6O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
N-[(5-fluoro-2,3-dihydro-1-benzofuran-4-yl)methyl]-8-(2-methylpyridin-3-yl)-[1,2,4]triazolo[4,3-c]pyrimidin-5-amine |
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1. Huang Y, et al. J Med Chem. 2022 Apr 14;65(7):5317-5333.
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