CPI-455

CPI-455 is a specific, pan-KDM5 inhibitor with an IC50 of 10 nM for KDM5A. CPI-455 mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agents[1].

Product Specifications

CAS Number

[1628208-23-0]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Histone Demethylase

Type

Reference compound

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/CPI-455.html

Concentration

10mM

Purity

98.95

Solubility

DMSO : 31.25 mg/mL (ultrasonic)

Smiles

N#CC1=C2NC(C3=CC=CC=C3)=C(C(C)C)C(N2N=C1)=O

Molecular Formula

C16H14N4O

Molecular Weight

278.31

Precautions

H302, H315, H319, H335

References & Citations

[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|[3]Xiang Yuan, et al. Blockade of Immune-Checkpoint B7-H4 and Lysine Demethylase 5B in Esophageal Squamous Cell Carcinoma Confers Protective Immunity against P. gingivalis Infection. Cancer Immunol Res. 2019 Sep;7 (9) :1440-1456.