KDM5A-IN-1 is an orally available, potent and selective inhibitor of the pan-histidine lysine demethylase 5 KDM5, inhibiting KDM5A, KDM5B, and KDM5C with IC50 values of 45 nM, 56 nM, and 55 nM, respectively.KDM5A-IN-1 inhibits PC9 H3K4Me3, and may be useful in cancer research.

CPI-455 is a specific KDM5 inhibitor with IC50 value of 10 ± 1 nM for full-length KDM5A in enzymatic assays, elevating global levels of H3K4 trimethylation (H3K4me3) and decreased the number of DTPs in multiple cancer cell line models treated with target

KDM5-C49 (KDOAM-20) hydrochloride is a potent, selective inhibitor of the KDM5 family of demethylases, demonstrating IC50 values of 40 nM for KDM5A, 160 nM for KDM5B, and 100 nM for KDM5C, respectively. This compound is utilized in cancer research [1].