Biological Activity
Selective inhibitor of TANK-binding kinase 1 (TBK1) and IKKε (IC50 values are ~1-2 μM). Displays no effect on IKKα or IKKβ at these concentrations. Reversibly lowers weight, increases insulin sensitivity, and reduces inflammation and steatosis in three mouse models of obesity. Exhibits antiallergic activity; inhibits the release of histamine from rat mast cells. Also binds to Hsp90 and inhibits C-terminal chaperone activity in vitro.
Compound Libraries
Amlexanox is also offered as part of the Tocriscreen Plus, Tocriscreen Kinase Inhibitor Toolbox II and Tocriscreen Library of FDA-Approved Compounds. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 298.29 |
| Formula | C16H14N2O4 |
| Storage | Store at -20°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 68302-57-8 |
| PubChem ID | 2161 |
| InChI Key | SGRYPYWGNKJSDL-UHFFFAOYSA-N |
| Smiles | CC(C)C1=CC=C2C(C(C(C=C(C(O)=O)C(N)=N3)=C3O2)=O)=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 | |||
| DMSO | 29.83 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 298.29. 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 | 3.35 mL | 16.76 mL | 33.52 mL |
| 5 mM | 0.67 mL | 3.35 mL | 6.7 mL |
| 10 mM | 0.34 mL | 1.68 mL | 3.35 mL |
| 50 mM | 0.07 mL | 0.34 mL | 0.67 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Reilly et al (2012) An inhibitor of the protein kinases TBK1 and IKK-ε improves obesity-related metabolic dysfunctions in mice. Nat.Med. 19 313 PMID: 23396211
Okada et al (2003) Hsp90 is a direct target of the anti-allergic drugs disodium cromoglycate and amlexanox. Biochem.J. 374 433 PMID: 12803546
Makino et al (1987) Mechanism of action of an antiallergic agent, amlexanox (AA-673), in inhibiting histamine release from mast cells. Acceleration of cAMP generation and inhibition of phosphodiesterase. Int.Arch.Allergy Appl.Immunol. 82 66 PMID: 2433225
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