KDM5-C70

KDM5-C70 (also known as KDOAM-21) is a cell-permeable, potent, and selective pan-KDM5 histone demethylase inhibitor. It is the ethyl ester prodrug of KDM5-C49 (KDOAM-20), designed to mask the highly polar carboxylate group of KDM5-C49 and improve cellular permeability. KDM5-C70 inhibits the Jumonji C (JmjC) domain-containing histone demethylases KDM5A, KDM5B, KDM5C, and KDM5D, which catalyze the removal of di- and tri-methyl groups from lysine 4 of histone H3 (H3K4me2/3). By blocking KDM5 activity, KDM5-C70 increases global H3K4me3 levels, leading to antiproliferative effects in multiple myeloma and breast cancer cells, and promoting astrocytic differentiation in neural stem cells. It has also been investigated for its potential to attenuate renal inflammation and fibrosis following acute kidney injury.

Other names

KDM5-C49 ethyl esterKDM-5-C49 ethyl esterKDM 5-C49 ethyl esterKDOAM-20 ethyl esterKDOAM20 ethyl esterKDOAM 20 ethyl esterethyl 2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-oxoethyl)amino)methyl)isonicotinate