A potent and allosteric inhibitor of PRC2 (IC50 = 23.4 nM in an enzyme assay with H3K27me0 peptide as the substrate); exhibits dose-dependent displacement of H3K27me3 binding to the EED subunit of PRC2; decreases global H3K27me3 and H3K27me2 in G401 cells and H3K27me3 in Karpas422 lymphoma cells in a dose-dependent manner; reduces proliferation of Karpas422 lymphoma cells in vitro and slows growth of Karpass422 xenografts in vivo

EED226 – 1 mg

Brand:
Cayman
CAS:
2083627-02-3
Storage:
-20
UN-No:
De Minimis - 3077 / 9

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).{33981} 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 (Item No. 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.  

 

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Description

A potent and allosteric inhibitor of PRC2 (IC50 = 23.4 nM in an enzyme assay with H3K27me0 peptide as the substrate); exhibits dose-dependent displacement of H3K27me3 binding to the EED subunit of PRC2; decreases global H3K27me3 and H3K27me2 in G401 cells and H3K27me3 in Karpas422 lymphoma cells in a dose-dependent manner; 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

Synonyms: 

Molecular weight: 369.4

CAS: 2083627-02-3

Purity: ≥99%

Formulation: A solid

Product Type|Biochemicals|Small Molecule Inhibitors|Methyltransferases||Research Area|Epigenetics, Transcription, & Translation|Writers|Histone Methylation

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