BAY-598 is a potent, peptide-competitive chemical probe for SET and MYND domain-containing protein 2 (SMYD2), a lysine methyl transferase inhibitor that dimethylates histone H3K36 and methylates histone H3K4. SMYD2 also methylates Lys-370 of p53, leading to decreased DNA-binding activity. SMYD2 is over-expressed in several cancers with poor prognosis. BAY-598 inhibits
in vitro methylation of p53K370 with an IC
50 value of 27 nM and in cells with an IC
50 value < 1 μM. BAY-598 is more than 100-fold selective over other histone methyltransferases and non-epigenetic targets. BAY-598 can be used with
in vivo experiments. For full characterization details, please visit the
BAY-598 probe summary on the Structural Genomics Consortium (SGC) website.
BAY-369 is the negative control for the active probe, BAY-598. To request a sample of the negative control from the SGC,
click here.
To learn about other SGC chemical probes for epigenetic targets, visit
sigma.com/sgc