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tMAK683 is an inhibitor of embryonic ectoderm development protein (EED) with potential antineoplastic activity. MAK683 binds to the domain of EED that interacts with trimethylated lysine 27 on histone 3 (H3K27me3), leading to a conformational change in the EED H3K27me3-binding pocket and preventing the interaction of EED with the histone methyltransferase enhancer zeste homolog 2 (EZH2). MAK683 is undergoing phase II clinical trials for the identification of antitumor activity.
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MAK683 - CAS 1951408-58-4 MAK683 is an inhibitor of embryonic ectoderm development protein (EED) with potential antineoplastic activity. MAK683 binds to the domain of EED that interacts with trimethylated lysine 27 on histone 3 (H3K27me3), leading to a conformational change in the EED H3K27me3-binding pocket and preventing the interaction of EED with the histone methyltransferase enhancer zeste homolog 2 (EZH2). MAK683 is undergoing phase II clinical trials for the identification of antitumor activity.