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EED226

Chemical Structure : EED226

CAS No.: 2083627-02-3

EED226 (EED 226;EED-226)

Catalog No.: PC-42321Not For Human Use, Lab Use Only.

EED226 (EED 226) is a potent, selective, orally bioavailable PRC2 inhibitor that directly binds to the H3K27me3 binding pocket of EED (IC50=22 nM).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

EED226 (EED 226) is a potent, selective, orally bioavailable PRC2 inhibitor that directly binds to the H3K27me3 binding pocket of EED (IC50=22 nM).
EED226 shows remarkable selectivity over 21 other PRMTs, with one exception EZH1.
EED226 potently reduces global H3K27Me3 mark in cells and demonstrates selectively cell killing effects in cells carrying a heterozygous Y641N mutation.
EED226 induces robust and sustained tumor regression in EZH2MUT pre-clinical DLBCL model.

Physicochemical Properties

M.Wt 369.3977
Formula C17H15N5O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 29 mg/mL

Chemical Name/SMILES

1,2,4-Triazolo[4,3-c]pyrimidin-5-amine, N-(2-furanylmethyl)-8-[4-(methylsulfonyl)phenyl]-

References

1. Qi W, et al. Nat Chem Biol. 2017 Apr;13(4):381-388.

2. Huang Y, et al. J Med Chem. 2017 Mar 23;60(6):2215-2226.

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