Biological Activity
Potent and selective inhibitor of the homologous protein lysine methyltransferases, G9a and GLP (IC50 values are 6 nM and 15 nM for G9a and GLP, respectively). Potently blocks G9a/GLP methyltransferase activity in cells (IC50 = 10 nM in MCF7 cells); exhibits low cellular toxicity (EC50 = 4.7 μM in MCF7 cells). Selective for G9a/GLP over a range of other protein lysine methyltransferases and protein arginine methyltransferases.
Compound Libraries
UNC 0646 is also offered as part of the Tocriscreen Plus and Tocriscreen Epigenetics Toolbox. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 621.9 |
| Formula | C36H59N7O2 |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 1320288-17-2 |
| PubChem ID | 53315882 |
| InChI Key | OUKWLRHRXOPODD-UHFFFAOYSA-N |
| Smiles | CC(C)N(CC6)CCCN6C1=NC(NC3CCN(C5CCCCC5)CC3)=C2C(C=C(OCCCN4CCCCC4)C(OC)=C2)=N1 |
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 | |||
| DMSO | 62.19 | 100 | |
| ethanol | 62.19 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 621.9. 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 | 1.61 mL | 8.04 mL | 16.08 mL |
| 5 mM | 0.32 mL | 1.61 mL | 3.22 mL |
| 10 mM | 0.16 mL | 0.8 mL | 1.61 mL |
| 50 mM | 0.03 mL | 0.16 mL | 0.32 mL |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
References
References are publications that support the products' biological activity.
Liu et al (2011) Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines. J.Med.Chem. 54 6139 PMID: 21780790
Keywords: UNC 0646, supplier, UNC0646, epigenetics, SGC, G9a, GLP, histone, protein, lysine, methyltransferases, PKMTs, HMTs, potent, selective, inhibitors, inhibits, Lysine, Methyltransferases, Lysine, Methyltransferases, Lysine, Methyltransferases, Tocris Bioscience
