EED226
| CAS No. | 2083627-02-3 | Cat. No. | BCP19849 |
| Name | EED226 | ||
| Synonyms | EED-226; EED 226; | ||
| Formula | C17H15N5O3S | M. Wt | 369.40 |
| Description | EED226 is a potent, selective, and orally bioavailable EED inhibitor. induces robust and sustained tumor regression in EZH2MUT preclinical DLBCL model. 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. EED226 inhibits PRC2 activity via an allosteric mechanism and offers an opportunity for treatment of PRC2-dependent cancers. demonstrated very impressive antitumor activities in mouse xenograft model. | ||
| Pathways | Epigenetics | ||
| Targets | Histone Methyltransferase | ||
Structure
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