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MAK-683 C화학적 특성, 용도, 생산
개요
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). 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.
용도
MAK-683 is a useful intermediate for the preparation of triazolopyrimidine compounds useful in the treatment of diseases or disorders mediated by EED and/or PRC2. EED inhibitor-1.