Highly potent and SAM-competitive EZH2 lysine methyltransferase inhibitor (IC50
= 0.7 nM). Inhibits proliferation of Karpas-422 cells (non-Hodgkin's lymphoma) in vitro
, and halts tumor growth and reduces intratumoral H3K27Me3 levels in mice.
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Design and synthesis of pyridone-containing 3,4-dihydroisoquinoline-1(2H)-ones as a novel class of enhancer of zeste homolog 2 (EZH2) inhibitors.
Kung et al.