EPZ005687 - CAS# 1396772-26-1 lapril CAS Number: 124750-99-8

CAS Number: 124750-99-8

by in vitro binding experiments

It inhibits phosphorylation of the mTORC1 substrates 4E-BP1 and S6K1 as well as the mTORC2 substrate AKT in diverse cancer models in vitro and in vivo

Formula: C17H26ClN3O2S

GSK-2118436A

EPZ005687 - CAS# 1396772-26-1 lapril CAS Number: 124750-99-8EPZ005687 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