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Background Information:
EED-226 (EED226) is a first-in-class, potent, selective and orally bioavailable allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED (Embryonic Ectoderm Development), with enzymatic IC50 values of 23.4 nM and 53.5 nM with H3K27me0 peptide and the mononucleosome as the substrates, respectively. It allosterically induces a conformational change upon binding to EED, leading to loss of PRC2 activity. EED-226 effectively induced robust and sustained tumor regression in EZH2MUT preclinical DLBCL model (refs 1, 2).
Reference:
1. Y. Huang, et al, Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy. J Med Chem. 2017 Mar 23;60(6):2215-2226.
2. W Qi et al. An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED. Nat Chem Biol. 2017 Apr;13(4):381-388.
APIM050300: EED-226 (EED226)
CAS No.: 2083627-02-3.
Molecular Formula: C17H15N5O3S.
Molecular Weight: 369.4 (or refer to the Certificate of Analysis, batch-specific).
Purity: 99.9% by HPLC.
QC: HPLC-MS, NMR and Elemental Analysis Report.
Solubility: Refer to Certificate of Analysis.
Storage: Refer to Certificate of Analysis.
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