Catalog Number: 5365
Chemical Name: 3-Cyano-5-[2-[4-[2-(3-methyl-1H-indol-1-yl)ethyl]piperazin-1-yl]phenyl]-N-[3-(pyrrolidin-1-yl)propyl]benzamide
Biological Activity
Potent SMYD2 inhibitor (IC50 = 15 nM). Exhibits >100-fold selectivity for SMYD2 over 25 other methyltransferases including SMYD3, SUV420H1 and SUV420H2. Inhibits SMYD2-mediated p53 methylation in vitro. Also inhibits proliferation of a range of esophageal, liver and breast cancer cell lines.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 100 mM in 1eq. HCl and to 100 mM in DMSO
  • Purity:
  • Storage:
    Store at -20°C
  • CAS No:
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Additional Information
Licensing Caveats:
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the LLY 507 probe summary on the SGC website.
Background References
  1. LLY-507, a cell-active, potent, and selective inhibitor of protein-lysine methyltransferase SMYD2.
    Nguyen et al.
    J.Biol.Chem., 2015;290:13641
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