EED226|EED-226|PRC2 inhibitor
DC Chemicals, Website: www.dcchemicals.com
Product Name: EED-226|Cas Number: 2083627-02-3| Catalog Number: DC10017|Other Nmaes: EED226,EED 226
EED226 is a potent and selective PRC2 inhibitor
that directly binds to the H3K27me3 binding pocket of EED.
EED226 is a potent and selective PRC2 inhibitor
that directly binds to the H3K27me3 binding pocket of EED. EED226 inhibits PRC2 activity via an allosteric mechanism and offers an opportunity for treatment of PRC2-dependent cancers. EED226 induces a conformational change upon binding EED, leading to loss of PRC2 activity. EED226 shows similar activity to SAM-competitive inhibitors in blocking H3K27 methylation of PRC2 target genes and inducing regression of human lymphoma xenograft tumors. Interestingly, EED226 also effectively inhibits PRC2 containing a mutant EZH2 protein resistant to SAM-competitive inhibitors.
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