CPI-455

SKU: orb1226026

Description

A potent, specific histone demethylase pan-KDM5 inhibitor with biochemical IC50 of 10, 3 and 14 nM for KDM5A, KDM5B and KDM5C, respectively; shows substantially weaker potency toward KDM4C and KDM7B (200- and 770-fold, respectively) and no inhibition of KDM2B, KDM3B or KDM6A; dose-dependently increases in H3K4 methylation in multiple cell lines, decreases the number of drug-tolerant persister cancer cells (DTPs) in multiple cancer cell line models treated with standard chemotherapy or targeted agents.

Key Properties

• CAS Number: 1628208-23-0
• MW: 278.3086
• Purity: >98% (HPLC)
• Formula: C₁₆H₁₄N₄O
• SMILES: N#CC1=C(NC(C2=CC=CC=C2)=C(C(C)C)C3=O)N3N=C1
• Target: Histone Demethylase
• Solubility: DMSO: ≥ 34 mg/mL

Bioactivity

• In Vivo:
  Animal model: Six-week-old male C57BL/6 mice (One-to 2-mm fragments of P. gingivalis–positive PDXs were implanted subcutaneously into the flank region of humanized mice.). Dosage: 50 mg/kg or 70 mg/kg (combined with anti–B7-H4). Administration: IP, daily, 14-28 days. Result: Histopathology analysis revealed no inflammation in either group at 2 weeks in response to the primary infection. However, at 8 weeks after inoculation, mice receiving monotherapy exhibited mild inflammation, whereas the combined treatment presented with heavy to severe inflammation, which persisted at 12 and 16 weeks after challenge. Treatment with CPI-455 to selectively target H3K4-specific JmjC demethylases increased CXCL11, CXCL9, and CXCL10 following infection, with maximum levels observed 48 hours after infection.

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

CPI455 | CPI 455

Quick Database Links

Gene Symbol

Histone Demethylase