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Potent and selective competitive inhibitor of SMYD2 lysine methyltransferase (IC50 values are 27 and 58 nM for biochemical and cellular activity assays, respectively). Displays >100-fold selectivity for SMYD2 over a panel of 32 other methyltransferases including SMYD3, SUV420H1, and SUV420H2. Enhances apoptotic responses to doxorubicin (Cat. No. 2252) in cancer cell lines. Decreases p53K370me levels in HEK293 cells. 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.
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the BAY 598 probe summary on the SGC website.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 525.34. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.9 mL||9.52 mL||19.04 mL|
|5 mM||0.38 mL||1.9 mL||3.81 mL|
|10 mM||0.19 mL||0.95 mL||1.9 mL|
|50 mM||0.04 mL||0.19 mL||0.38 mL|
References are publications that support the biological activity of the product.
Eggert et al (2016) Discovery and characterization of a highly potent and selective aminopyrazoline-based in vivo probe (BAY-598) for the protein lysine methyltransferase SMYD2. J.Med.Chem. 59 4578 PMID: 27075367
Scheer et al (2019) A chemical biology toolbox to study protein methyltransferases and epigenetic signaling. Nat.Commun. 10 19 PMID: 30604761
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Keywords: BAY 598, BAY 598 supplier, BAY598, lysine, methyltransferase, inhibitors, inhibits, potent, selective, SMYD2, SET, and, MYND, domain, contain, protein, 2, Other, Lysine, Methyltransferases, 5991, Tocris Bioscience
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