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.
Licensing Information
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.
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 LLY 507 is reviewed on the chemical probes website.
Technical Data
| M. Wt | 574.76 |
| Formula | C36H42N6O |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1793053-37-8 |
| PubChem ID | 91623361 |
| InChI Key | PNYRDVBFYVDJJI-UHFFFAOYSA-N |
| Smiles | CC(C5=C4C=CC=C5)=CN4CCN(CC3)CCN3C1=C(C2=CC(C#N)=CC(C(NCCCN6CCCC6)=O)=C2)C=CC=C1 |
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.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 1eq. HCl | 57.48 | 100 | |
| DMSO | 57.48 | 100 | |
| ethanol | 57.48 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 574.76. Batch specific molecular weights may vary from batch to batch due to solvent 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 | 1.74 mL | 8.7 mL | 17.4 mL |
| 5 mM | 0.35 mL | 1.74 mL | 3.48 mL |
| 10 mM | 0.17 mL | 0.87 mL | 1.74 mL |
| 50 mM | 0.03 mL | 0.17 mL | 0.35 mL |
Molarity Calculator
Reconstitution Calculator
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Product Datasheets
References
References are publications that support the products' biological activity.
Nguyen et al (2015) LLY-507, a cell-active, potent, and selective inhibitor of protein-lysine methyltransferase SMYD2. J.Biol.Chem. 290 13641 PMID: 25825497
Keywords: LLY 507, supplier, LLY507, potent, selective, SMYD2, inhibitors, inhibits, lysine, methyltransferases, p53, Lysine, Methyltransferases, Lysine, Methyltransferases, Lysine, Methyltransferases, Tocris Bioscience
