BAY-598

BAY-598 is a potent and selective competitive inhibitor of SMYD2 lysine methyltransferase (IC₅₀ values are 27 and 58 nM for biochemical and cellular activity assays, respectively). It displays >100-fold selectivity for SMYD2 over a panel of 32 other methyltransferases including SMYD3, SUV420H1, and SUV420H2. Decreases p53K370me levels in HEK293 cells. Reduces methylation in tumor cells in a mouse xenograft model.