Cat. No. 4857
Chemical Name: 2-Amino-7-(1-methylethyl)-5-oxo-5H-
Biological ActivitySelective 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.
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.
Certificate of Analysis / Safety Data Sheet
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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Citations are publications that use Tocris products. Selected citations for Amlexanox include:
Alrahbeni et al (2015) Full UPF3B function is critical for neuronal differentiation of neural stem cells. Br J Pharmacol 8 33. PMID: 26012578.
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Keywords: Amlexanox, supplier, diabetes, obese, obesity, mouse, mice, anti-inflammatory, anti-inflammatories, metabolic, disorders, diseases, IkB, kinase, IkappaB, IκB, IKK, TBK1, TANK-binding, kinase, 1, noncanonical, Tocris Bioscience, IκB Kinase Inhibitor products
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