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. Reduces methylation in tumor cells in a mouse xenograft model.
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For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
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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