CPI-455

• CAT Number: I002105
• CAS Number: 1628208-23-0
• Molecular Formula: C₁₆H₁₄N₄O
• Molecular Weight: 278.31
• Purity: ≥95%
• Synonyms: 6-isopropyl-7-oxo-5-phenyl-4,7-dihydropyrazolo[1,5-a]pyrimidine-3-carbonitrile hydrochloride
• Target: Histone Demethylase
• Solubility: DMSO: ≥ 34 mg/mL
• Storage: Store at -20°C
• IUPAC Name: 7-oxo-5-phenyl-6-propan-2-yl-1H-pyrazolo[1,5-a]pyrimidine-3-carbonitrile
• InChI: InChI=1S/C16H14N4O/c1-10(2)13-14(11-6-4-3-5-7-11)19-15-12(8-17)9-18-20(15)16(13)21/h3-7,9-10,18H,1-2H3
• InChIKey: VGXRQCOVGLGFIM-UHFFFAOYSA-N
• SMILES: CC(C)C1=C(N=C2C(=CNN2C1=O)C#N)C3=CC=CC=C3

CPI-455 is a potent pan-KDM5 inhibitor that effectively inhibits KDM5A with an IC50 of 10 nM. By inhibiting KDM5, CPI-455 increases the levels of H3K4me3 globally, and reduces the number of drug-tolerant persister cancer cells across various cancer cell line models treated with standard chemotherapy or targeted agents.

Reference

[1]. Vinogradova M, et al. An inhibitor of KDM5 demethylases reduces survival of drug-tolerant cancer cells. Nat Chem Biol. 2016 Jul;12(7):531-8.

[2]. Benjamin R. Leadem. NOVEL HISTONE DEMETHYLASE INHIBITORS SYNERGISTICALLY
ENHANCE THE EFFECTS OF A DNA HYPOMETHYLATING AGENT IN BREAST
CANCER CELLS. Baltimore, MD March, 2015.