Background:

IC50: 10 nM

CPI-455 is a KDM5 inhibitor.

The KDM5 family of histone demethylases catalyzes the demethylation of histone H3 on lysine 4 (H3K4) and is required for the survival of drug-tolerant persister cancer cells (DTPs).

In vitro: Previous study found that CPI-455 could potently inhibit the fulllength KDM5A in enzymatic assays with a half-maximal inhibitory concentration of 10 ± 1 nM. CPI-455 inhibited KDM5A, KDM5B and KDM5C to similar levels but showed significantly weaker potency toward KDM4C and KDM7B (