UNC1999, EZH2 methyltransferase inhibitor

Description

MW 569.7 Da, Purity >98 %. Potent, selective cell-permeable dual inhibitor of EZH2 and EZH1 methyltransferase inhibitor IC50 = 45 nM and 2 nM respectively Konze et al. . Inhibits H3K27 methylation IC50 = 124 nM, MCF10A cells . Competitive with the cofactor SAM, and non-competitive with the peptide substrate. Inhibition of EZH2 with UNC1999 enhanced the efficacy of gefitinib in suppressing the proliferation of colon cancer cells Katona et al. . It suppresses global H3K27 trimethylation/demethylation and inhibits the growth of mixed lineage leukemia MLL -rearranged leukemia cells Xu et al. . Orally bioavailable.