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), which displays >100-fold selectivity for SMYD2 over a panel of 32 other methyltransferases including SMYD3, SUV420H1, and SUV420H2. BAY 598 enhances apoptotic responses to doxorubicin (Cat. No. 2252) in cancer cell lines, and decreases p53K370me levels in HEK293 cells. It also reduces methylation in tumor cells in a mouse xenograft model.
To request the negative control for BAY 598, please fill out the BAY 369 request form on the SGC website.