Chemical Name: N-[(4S)-1-[(Cyanoamino)[[3-(difluoromethoxy)phenyl]imino]methyl]-3-(3,4-dichlorophenyl)-4,5-dihydro-1H-pyrazol-4-yl]-N-ethyl-2-hydroxyacetamide
Biological ActivityPotent 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.
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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.
A chemical biology toolbox to study protein methyltransferases and epigenetic signaling.
Scheer et al.
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.
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