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EED226
Axon 2701
CAS:
2083627-02-3
Purity:
99%
- Soluble in DMSO
- MF: C17H15N5O3S
- MW: 369.4
Description
EED226 is a first-in-class, potent, selective and orally bioavailable PRC2 inhibitor (IC50 values of 23.4 nM and 53.5 nM with H3K27me0 peptide and the mononucleosome as the substrates, respectively) that directly binds to the H3K27me3 binding pocket of EED. EED226 effectively induced tumor regression in a mouse xenograft model.
More Information
| Parent CAS No. | 2083627-02-3 |
|---|---|
| Chemical Name | N-(Furan-2-ylmethyl)-8-(4-(methylsulfonyl)phenyl)-[1,2,4]triazolo[4,3-c]pyrimidin-5-amine |
| SMILES | C1C=C(C2=CN=C(NCC3OC=CC=3)N3C=NN=C23)C=CC=1S(C)(=O)=O |
| MFCD | N.A. |
| InChi | InChI=1S/C17H15N5O3S/c1-26(23,24)14-6-4-12(5-7-14)15-10-19-17(22-11-20-21-16(15)22)18-9-13-3-2-8-25-13/h2-8,10-11H,9H2,1H3,(H,18,19) |
| InChiKey | DYIRSNMPIZZNBK-UHFFFAOYSA-N |
| CID | 123132228 |
| Short Description | PRC2 inhibitor |
References
- 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.
- W Qi et al. An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED. Nat Chem Biol. 2017 Apr;13(4):381-388.
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