Catalog No.S3648 Synonyms: AA-673, CHX-3673
Molecular Weight(MW): 298.29
Amlexanox is an anti-inflammatory antiallergic immunomodulator and also an inhibitor of the protein kinases TBK1 and IKK-ε.
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|Description||Amlexanox is an anti-inflammatory antiallergic immunomodulator and also an inhibitor of the protein kinases TBK1 and IKK-ε.|
Dose-response relationship of amlexanox inhibition of IKK-ɛ and TBK1 activity as determined by MBP phosphorylation showing an IC50 of approximately 1-2 μM. Amlexanox also blocks the activity of TBK1 at approximately the same concentrations but has no effect on IKK-α or IKK-β and at these concentrations do not block any other kinases from a broad panel representing most kinase families. Inhibition of IKK-ɛ or TBK1 by amlexanox is competitive for its substrate ATP, indicating that it interacts with the enzymes in the ATP-binding site. Amlexanox increases the phosphorylation of TBK1 at Ser172 in 3T3-L1 adipocytes and blocks polyinosinic:polycytidylic acid (poly I:C)-stimulated phosphorylation of interferon responsive factor-3 (IRF3), a presumed substrate of IKK-ɛ and TBK1.
|In vivo||Treatment of obese mice with amlexanox elevates energy expenditure through increased thermogenesis, producing weight loss, improves insulin sensitivity and decreases steatosis.|
|In vitro||DMSO||59 mg/mL (197.79 mM)|
|Ethanol||1 mg/mL (3.35 mM)|
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