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EPZ005687 - CAS# 1396772-26-1 lapril 58 μM on HCT116 cells

SKU: 74476814038

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EPZ005687 - CAS# 1396772-26-1 lapril 58 μM on HCT116 cellsEPZ005687 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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Description

58 μM on HCT116 cells

1586/17476348

by in vitro binding experiments

or PC-3 tumor-bearing mice (6

CAS Number: 124750-99-8

EPZ005687 - CAS# 1396772-26-1 lapril 58 μM on HCT116 cellsEPZ005687 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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