MAK-683 is an inhibitor of trimethylation of histone 3 lysine 27 (H3K27) by polycomb repressive complex 2 (PRC2), a complex that includes embryonic ectoderm development protein (EED).1 MAK-683 has an IC50 value of 5.9 nM in an EED-H3K27me3 peptide competition binding assay and inhibits H3K27 trimethylation in G401 cells (IC50 = 2.6 nM). It inhibits proliferation of KARPAS422 B cell lymphoma cells with an IC50 value of 3 nM.
1.Chan, H.M., Gu, X.-J., Huang, Y., et al.Triazolopyrimidine compounds and uses thereof(2016)
















