UNC1999 is an orally active, highly selective inhibitor of both wild-type and mutant EZH1 and EZH2 lysine methyltransferases (IC50’s = 45 nM and 2 nM respectively). Inhibition of EZH2 with UNC1999 enhanced the efficacy of gefitinib in suppressing the proliferation of colon cancer cells. It...
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UNC1999 is an orally active, highly selective inhibitor of both wild-type and mutant EZH1 and EZH2 lysine methyltransferases (IC50’s = 45 nM and 2 nM respectively). Inhibition of EZH2 with UNC1999 enhanced the efficacy of gefitinib in suppressing the proliferation of colon cancer cells. It suppresses global H3K27 trimethylation/demethylation and inhibits the growth of mixed lineage leukemia (MLL)-rearranged leukemia cells
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