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Abcam UNC1999, EZH2 methyltransferase inhibitor, 25MG
Supplier: Abcam AB14615225MG
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.
The product is subject to the following: Abcam Restricted Use Statement
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