Biological Activity
Potent and selective G9a/GLP histone lysine methyltransferase inhibitor (IC50 = 3.3 nM). Exhibits >1000-fold selectivity for G9a/GLP over 21 other methyltransferases. Decreases levels of lysine 9 dimethylation on histone H3 (H3K9Me2) in PC3 cells.
Licensing Information
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the A 366 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 A 366 is reviewed on the chemical probes website.
Compound Libraries
A 366 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 | 329.44 |
| Formula | C19H27N3O2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1527503-11-2 |
| PubChem ID | 76285486 |
| InChI Key | BKCDJTRMYWSXMC-UHFFFAOYSA-N |
| Smiles | COC1=C(OCCCN4CCCC4)C=C(N=C(N)C32CCC3)C2=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 | 32.94 | 100 | |
| DMSO | 32.94 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 329.44. 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 | 3.04 mL | 15.18 mL | 30.35 mL |
| 5 mM | 0.61 mL | 3.04 mL | 6.07 mL |
| 10 mM | 0.3 mL | 1.52 mL | 3.04 mL |
| 50 mM | 0.06 mL | 0.3 mL | 0.61 mL |
Molarity Calculator
Reconstitution Calculator
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Product Datasheets
References
References are publications that support the products' biological activity.
Sweis et al (2014) Discovery and development of potent and selective inhibitors of histone methyltransferase G9a. ACS Med.Chem.Lett. 5 205 PMID: 24900801
Keywords: A 366, supplier, A366, G9a, histone, methyltransferases, potent, selective, lysine, GLP, sgc, Lysine, Methyltransferases, Lysine, Methyltransferases, Lysine, Methyltransferases, Tocris Bioscience
