EED226

SKU: orb1223193

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.

Key Properties

• CAS Number: 2083627-02-3
• MW: 369.4
• Purity: >98% (HPLC)
• Formula: C₁₇H₁₅N₅O₃S
• SMILES: c1(n2c(c(cn1)c1ccc(cc1)S(=O)(=O)C)nnc2)NCc1occc1
• Target: EED| PRC2
• Solubility: DMSO : ≥ 29 mg/mL. 78.51 mM; H2O : < 0.1 mg/mL

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

EED226 | EED-226 | EED 226

Quick Database Links

Gene Symbol

EED| PRC2