YUKA1 is a cell permeable, potent inhibitor of KDM5A, showing little to no activity against KDM5B, KDM6A, and KDM6B. YUKA1 was shown to increase H3K4me3 levels in human cells and selectively inhibit the proliferation of cancer cells whose growth depends on KDM5A.
YUKA1 is a potent and cell permeable Lysine demethylase 5A (KDM5A) inhibitor, with an IC50 of 2.66 μM, less active on KDM5C (IC50, 7.12 μM), and is inactive on KDM5B, KDM6A or KDM6B. YUKA1 increases H3K4me3 levels in human cells with anti-cancer activity[1].
