EED226

Research use only, not for human use.

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

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.

EED226; EED-226; EED 226

Others

Other Targets

EED; PRC2

Cancer

——

2083627-02-3

369.4

C17H15N5O3S

98%

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

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

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

(-20℃)

With Ice Pack

≥ 2 years