EPZ005687 - CAS# 1396772-26-1 lapril by in vitro binding experiments
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EPZ005687 - CAS# 1396772-26-1 lapril by in vitro binding experimentsEPZ005687 is a potent inhibitor of EZH2 (K(i) of 24 nM). EPZ005687 has greater than 500 fold selectivity against 15 other protein methyltransferases and has 50 fold selectivity against the closely related enzyme EZH1. The compound reduces H3K27 methylation in various lymphoma cells; this translates into apoptotic cell killing in heterozygous Tyr641 or Ala677 mutant cells, with minimal effects on the proliferation of wild type cells. Product
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