JQEZ-5

SKU: orb1225813

Description

A novel potent, selective, SAM-competitive EZH2 inhibitor with IC50 of 80 nM (inhibition of enzymatic function of PRC2); demonstrates acutely reduced level of H3K27me3 without affecting mono- and di-methylation, suppresses the proliferation of EZH2-overexpression H661 and H522 cell lines, more effectively than GSK-126 and GSK-343; promotes the regression of EZH2-driven tumors in vivo.

Key Properties

• CAS Number: 1913252-04-6
• MW: 542.688
• Purity: >98% (HPLC)
• Formula: C₃₀H₃₈N₈O₂
• SMILES: CC(C)N1N=CC2=C(C=C(N=C12)C3=CC=C(N4CCN(CC4)C)N=C3)C(NCC5=C(CCC)C=C(C)NC5=O)=O
• Target: HMTase
• Solubility: DMSO : 25 mg/mL 46.07 mM;H2O : < 0.1 mg/mL

Bioactivity

• In Vivo:
  JQEZ5 (75 mg/kg; intraperitoneal injection; daily; for 3 weeks) treatment exhibits rapid and pronounced tumor regression over the three week treatment course. And H3K27me3 levels are largely reduced with treatment further confirming the on-target effect of JQEZ5 in mice.
• In Vitro:
  JQEZ5 inhibits enzymatic functionality of PRC2 with a biochemical IC50 of 80 nM. JQEZ5 exhibits S-adenosyl methionine (SAM)-competitive inhibition of PRC2.H661 cells treated with increasing concentrations of JQEZ5 demonstrate acutely reduced levels of H3K27me3 without affecting H3K27 mono- or di-methylation. JQEZ5 suppresses the proliferation of EZH2-overexpressing H661 and H522 cells after treatment for 4 days without affecting the proliferation of cell lines that were deemed insensitive to EZH2 knockdown.

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

EZ-005 | EZ005 | JQEZ5

Quick Database Links

Gene Symbol

HMTase