MAK-683

MAK-683 is a potent EED (embryonic ectoderm development protein) inhibitor and an allosteric inhibitor of polycomb repressive complex 2 (PRC2), with potential antineoplastic activity. MAK683 selectively binds to the domain of EED that interacts with trimethylated lysine 27 on histone 3 (H3K27me3), which 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).