BAY 598

Biological Activity

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.

External Portal Information

Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of BAY 598 is reviewed on the chemical probes website.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Background References

1. A chemical biology toolbox to study protein methyltransferases and epigenetic signaling.
   Scheer et al.
   Nat.Commun., 2019;10:19
2. Discovery and characterization of a highly potent and selective aminopyrazoline-based in vivo probe (BAY-598) for the protein lysine methyltransferase SMYD2.
   Eggert et al.
   J.Med.Chem., 2016;59:4578

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