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MAK683

Chemical Structure : MAK683

CAS No.: 1951408-58-4

MAK683 (MAK-683;MAK683)

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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Biological Activity

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.

Physicochemical Properties

M.Wt 376.39
Formula C20H17FN6O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

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

References

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

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