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Submit ReviewAmlexanox
Description: Selective inhibitor of TBK
Chemical Name: 2-Amino-7-(1-methylethyl)-5-oxo-5H-[1]benzopyrano[2,3-b]pyridine-3-carboxylic acid
Purity: ≥99% (HPLC)
Biological Activity for Amlexanox
Amlexanox is a 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 for Amlexanox
Amlexanox is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library, Tocriscreen Antiviral Library and Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.
Technical Data for Amlexanox
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Amlexanox
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 29.83 | 100 |
Preparing Stock Solutions for Amlexanox
The following data is based on the product molecular weight 298.29. Batch specific molecular weights may vary from batch to batch due to the degree 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 for Amlexanox
References for Amlexanox
References are publications that support the biological activity of the product.
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 amle. Biochem.J. 374 433 PMID: 12803546
Makino et al (1987) Mechanism of action of an antiallergic agent, amle. (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
If you know of a relevant reference for Amlexanox, please let us know.
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Keywords: Amlexanox, Amlexanox supplier, diabetes, obese, obesity, mouse, mice, anti-inflammatory, anti-inflammatories, metabolic, disorders, diseases, IkB, kinase, IkappaB, IκB, IKK, TBK1, TANK-binding, 1, noncanonical, Kinase, NF-kB/IkB, Histaminergic-Related, Compounds, TANK, binding, (TBK), 4857, Tocris Bioscience
4 Citations for Amlexanox
Citations are publications that use Tocris products. Selected citations for Amlexanox include:
Neysan et al (2021) Genotoxic stress in constitutive trisomies induces autophagy and the innate immune response via the cGAS-STING pathway. Commun Biol 4 831 PMID: 34215848
Lin et al (2021) A naturally derived small molecule NDSM253 inhibits IKK1 to suppress inflammation response and promote bone healing after fracture. Am J Transl Res 13 24-37 PMID: 33527006
Harold I et al (2021) Tank Binding Kinase 1 modulates spindle assembly checkpoint components to regulate mitosis in breast and lung cancer cells. Biochim Biophys Acta Mol Cell Res 1868 118929 PMID: 33310066
Alrahbeni et al (2015) Full UPF3B function is critical for neuronal differentiation of neural stem cells. Br J Pharmacol 8 33 PMID: 26012578
Do you know of a great paper that uses Amlexanox from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Autophagy Scientific Review
Written by Patricia Boya and Patrice Codogno, this review summarizes the molecular mechanisms, physiology and pathology of autophagy. The role of autophagy in cell death and its links to disease are also discussed. Compounds available from Tocris are listed.
Autophagy Poster
Autophagy is a cellular process used by cells for degradation and recycling. Written by Patricia Boya and Patrice Codogno, this poster summarizes the molecular machinery, physiology and pathology of autophagy. Compounds available from Tocris are listed.
Pathways for Amlexanox
NF-κB Signaling Pathway
NF-κB signaling plays an important role in inflammation, the innate and adaptive immune response and stress. Dysregulated signaling can occur in inflammatory and autoimmune diseases.