Fig. 7
From: Assessing histone demethylase inhibitors in cells: lessons learned
Cytotoxic activity of different KDM inhibitors in live cells and 2-OG dependency of KDM inhibition in vitro. Immunofluorescence assays of cells transfected with KDM5B or KDM4A and treated with the newly developed inhibitors CCT365599 and CCT366293, respectively. Effect on H3K4me3 methylation is shown in the left panel in a dose-dependent manner and on H3K9me3 in the right panel. Number of cells in 20 fields, based on DAPI staining, is shown in b, c. Percentage of healthy, apoptotic and necrotic HeLa cells treated with CCT365599 and CCT366293, respectively, in a dose-dependent manner, d IC50 values in dependency of different 2-OG concentrations determined in AlphaScreen assay for different KDMs