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EED 226

Cat. No. 7762 Submit a Review Datasheet / COA / SDS
Pricing Availability   Qty
Description: Potent and selective EED inhibitor
Chemical Name: N-(2-Furanylmethyl)-8-[4-(methylsulfonyl)phenyl]-1,2,4-triazolo[4,3-c]pyrimidin-5-amine
Purity: ≥98% (HPLC)
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Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for EED 226

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.

Technical Data for EED 226

M. Wt 369.4
Formula C17H15N5O3S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2083627-02-3
PubChem ID 123132228
InChI Key DYIRSNMPIZZNBK-UHFFFAOYSA-N
Smiles O=S(=O)(C1=CC=C(C=C1)C2=CN=C(NCC=3OC=CC3)N4C=NN=C24)C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for EED 226

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 36.94 100

Preparing Stock Solutions for EED 226

The following data is based on the product molecular weight 369.4. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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

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References for EED 226

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

Qi et al (2017) An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED. Nat.Chem.Biol. 13 381 PMID: 28135235

If you know of a relevant reference for EED 226, please let us know.

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Citations for EED 226

Citations are publications that use Tocris products.

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