Amlexanox

Biological Activity

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.

Technical Data

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.

Background References

1. Hsp90 is a direct target of the anti-allergic drugs disodium cromoglycate and amle.
   Okada et al.
   Biochem.J., 2003;374:433
2. 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.
   Makino et al.
   Int.Arch.Allergy Appl.Immunol., 1987;82:66
3. An inhibitor of the protein kinases TBK1 and IKK-ε improves obesity-related metabolic dysfunctions in mice.
   Reilly et al.
   Nat.Med., 2012;19:313

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