EED-226 (EED226)

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.