TC-E 5002

TC-E 5002 is an inhibitor of the histone lysine demethylase (KDM) subfamily KDM2/7. It potently inhibits KDM2A, KDM7A and KDM7B with an IC₅₀ of 6.8 μM, 0.2 μM and 1.2 μM respectively. It inhibits the growth of KYSE150 and HeLa cells with GI₅₀ values of 16 µM and 40 µM respectively and arrests cells in the G0/G1 phase of the cell cycle. It inhibits demethylation of H3K27me2 at similar concentrations.