EED 226

Product Description

EED 226 is a potent (IC₅₀ = 23.4 nM) and selective EED inhibitor. It inhibits PRC2 activity by binding to the H3K27me3 pocket of EED. The compound shows selectivity for PRC2 complex over protein methyltransferases, kinases, and other protein classes. In vitro, EED 226 regulates histone H3K27 methylation and PRC2 target gene expression. In vivo, it induces tumor regression in a mouse xenograft model. EED 226 is orally bioavailable.

Solubility

Preparing Stock Solutions for EED 226

The following data is based on the product molecular weight 369.40

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.71 mL	13.54 mL	27.07 mL
5 mM	0.54 mL	2.71 mL	5.41 mL
10 mM	0.27 mL	1.35 mL	2.71 mL
50 mM	0.05 mL	0.27 mL	0.54 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Qi An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED. Nat.Chem.Biol. 2017 PMID: 28135235