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EED-226 (EED226)
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).
Catalog NO: CT-EED226
Synonym: EED226
CAS NO: 2083627-02-3
Mol. Formula: C17H15N5O3S
MW: 369.4 (or refer to the Certificate of Analysis, batch-specific)
** in vivo grade material. 99.9% Purity, white powder, textbook quality (original QC docs attached), clean and impeccable (with multiple cycles of recrystallizations), Bulk stock! Same day shipping.