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).
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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 |
1. Huang Y, et al. J Med Chem. 2022 Apr 14;65(7):5317-5333.
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