EED226( EED226 | EED-226 | EED 226 )

Catalog No. M17425 CAS No. 2083627-02-3

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Datasheet

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Product Name

EED226
Note

Research use only, not for human use.
Brief Description

EED226 is a potent, selective, and orally bioavailable embryonic ectoderm development (EED) inhibitor with an IC50 of 22 nM.
Description

EED226 is a potent, selective, and orally bioavailable EED inhibitor. induces robust and sustained tumor regression in EZH2MUT preclinical DLBCL model. EED226 induces a conformational change upon binding EED, leading to loss of PRC2 activity. EED226 shows similar activity to SAM-competitive inhibitors in blocking H3K27 methylation of PRC2 target genes and inducing regression of human lymphoma xenograft tumors. Interestingly, EED226 also effectively inhibits PRC2 containing a mutant EZH2 protein resistant to SAM-competitive inhibitors. EED226 inhibits PRC2 activity via an allosteric mechanism and offers an opportunity for treatment of PRC2-dependent cancers. demonstrated very impressive antitumor activities in mouse xenograft model.
In Vitro

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In Vivo

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Synonyms

EED226 | EED-226 | EED 226
Pathway

Others
Target

Other Targets
Recptor

EED| PRC2
Research Area

Cancer
Indication

——

CAS Number

2083627-02-3
Formula Weight

369.4
Molecular Formula

C17H15N5O3S
Purity

>98% (HPLC)
Solubility

DMSO : ≥ 29 mg/mL. 78.51 mM; H2O : < 0.1 mg/mL
SMILES

c1(n2c(c(cn1)c1ccc(cc1)S(=O)(=O)C)nnc2)NCc1occc1
Chemical Name

N-(Furan-2-ylmethyl)-8-(4-(methylsulfonyl)phenyl)[1,2,4]-triazolo[4,3-c]pyrimidin-5-amine

1.Huang Y, et al. J Med Chem. 2017 Mar 23;60(6):2215-2226.

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