KDM4-IN-2 (Compound 19a) is a potent and selective KDM4/KDM5 dual inhibitor with Kis of 4 and 7?nM for KDM4A and KDM5B, respectively[1]. Ki: 4 nM (KDM4A ), 7?nM (KDM5B)[1]IC50: 100±41 nM (KDM4A), 43±21 nM (KDM4B), 38 nM (KDM5B), 123 nM (KDM5C), 4.50 μM (KDM2A), 5.78 μM (KDM3A), 90.22?μM (KDM6B)[1]
[1]. Le Bihan YV, et al. C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays. Eur J Med Chem. 2019 Sep 1;177:316-337.