EED226

EED226 is a potent and allosteric inhibitor of the histone H3K27me3 methyltransferase activity of polycomb repressive complex 2 (PRC2, IC50 = 23.4 nM in an enzyme assay with H3K27me0 peptide as the substrate). It exhibits dose-dependent displacement of H3K27me3 binding to the EED subunit of PCR2 but has no effect on the binding of S-adenosylmethionine-cofactor-competitive inhibitor EI1 (Cay-19146) to the EZH2 catalytic subunit, indicating EED226 is an allosteric modulator of PRC2 function. EED226 decreases global H3K27me3 and H3K27me2 in G401 cells and H3K27me3 in Karpas422 lymphoma cells in a dose-dependent manner. It also reduces proliferation of Karpas422 lymphoma cells in vitro and slows growth of Karpass422 xenografts in vivo.Formal Name: N-(2-furanylmethyl)-8-[4-(methylsulfonyl)phenyl]-1,2,4-triazolo[4,3-c]pyrimidin-5-amine. CAS Number: 2083627-02-3. Molecular Formula: C17H15N5O3S. Formula Weight: 369.4. Purity: >99%. Formulation: (Request formulation change), A solid. Solubility: DMF: 33 mg/ml, DMSO: 33 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml. lambdamax: 228, 331 nm. SMILES: CS(C(C=C1)=CC=C1C2=CN=C(NCC3=CC=CO3)N4C2=NN=C4)(=O)=O. InChi Code: 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). InChi Key: DYIRSNMPIZZNBK-UHFFFAOYSA-N.