Amlexanox

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Cat.No. 4857 - Amlexanox | C16H14N2O4 | CAS No. 68302-57-8
Description: Inhibitor of TBK1 and IKKε; antiallergic agent
Chemical Name: 2-Amino-7-(1-methylethyl)-5-oxo-5H-[1]benzopyrano[2,3-b]pyridine-3-carboxylic acid
Purity: ≥99% (HPLC)
Datasheet
Citations (1)
Literature

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.

Select a batch to recalculate based on the batch molecular weight:
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

Safety Datasheet

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


If you know of a relevant reference for Amlexanox, please let us know.

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View all IκB Kinase Inhibitors

Keywords: diabetes obese obesity mouse mice anti-inflammatory anti-inflammatories metabolic disorders diseases IkB kinase IkappaB IκB IKK TBK1 TANK-binding kinase 1 noncanonical IkB Kinase

1 Citation for Amlexanox

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


Do you know of a great paper that uses Amlexanox from Tocris? If so please let us know.

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