Amlexanox

Catalog No.S3648 Batch:S364805

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Technical Data

Formula

C16H14N2O4
Molecular Weight 298.29 CAS No. 68302-57-8
Solubility (25°C)* In vitro DMSO 60 mg/mL (201.14 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
2.1mg/ml Taking the 1 mL working solution as an example, add 50 μL of 42 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
2.1mg/ml Taking the 1 mL working solution as an example, add 50 μL of 42 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Amlexanox is an anti-inflammatory antiallergic immunomodulator and also an inhibitor of the protein kinases TBK1 and IKK-ε.
Targets
TBK1 [1] IKK-ε [1]
In vitro 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[1].
In vivo Treatment of obese mice with amlexanox elevates energy expenditure through increased thermogenesis, producing weight loss, improves insulin sensitivity and decreases steatosis[1].

Protocol (from reference)

Cell Assay:[1]
  • Cell lines

    3T3-L1 adipocytes

  • Concentrations

    12, 25, 50 μM

  • Incubation Time

    1 h

  • Method

    TBK1 phosphorylation (pTBK1) at Ser172 and IRF3 phosphorylation at Ser396 (pIRF3) in 3T3-L1 adipocytes treated with amlexanox or cayman and with or without poly I:C are examined.

Animal Study:[1]
  • Animal Models

    C57BL/6

  • Dosages

    25 or 100 mg per kg body weight

  • Administration

    oral gavage

Selleck's Amlexanox has been cited by 15 publications

Targeting TANK-binding kinase 1 attenuates painful diabetic neuropathy via inhibiting microglia pyroptosis [ Cell Commun Signal, 2024, 22(1):368] PubMed: 39030571
Therapeutic modulation of ROCK overcomes metabolic adaptation of cancer cells to OXPHOS inhibition and drives synergistic anti-tumor activity [ bioRxiv, 2024, 2024.09.16.613317] PubMed: 39345502
TRIM28 promotes the escape of gastric cancer cells from immune surveillance by increasing PD-L1 abundance [ Signal Transduct Target Ther, 2023, 8(1):246] PubMed: 37357254
TRIM28 promotes the escape of gastric cancer cells from immune surveillance by increasing PD-L1 abundance [ Signal Transduct Target Ther, 2023, 8(1):246] PubMed: 37357254
FACT subunit SUPT16H associates with BRD4 and contributes to silencing of interferon signaling [ Nucleic Acids Res, 2022, 50(15):8700-8718] PubMed: 35904816
Mouse Ocilrp2/Clec2i negatively regulates LPS-mediated IL-6 production by blocking Dap12-Syk interaction in macrophage [ Front Immunol, 2022, 13:984520] PubMed: 36300111
Host MOV10 is induced to restrict herpes simplex virus 1 lytic infection by promoting type I interferon response [ PLoS Pathog, 2022, 18(2):e1010301] PubMed: 35157734
CDK1/2/5 inhibition overcomes IFNG-mediated adaptive immune resistance in pancreatic cancer [ Gut, 2021, 70(5):890-899] PubMed: 32816920
Activation of the STAT3 Signaling Pathway by the RNA-Dependent RNA Polymerase Protein of Arenavirus [ Viruses, 2021, 13(6)976] PubMed: 34070281
Amlexanox Enhances Temozolomide-Induced Antitumor Effects in Human Glioblastoma Cells by Inhibiting IKBKE and the Akt-mTOR Signaling Pathway [ ACS Omega, 2021, 6(6):4289-4299] PubMed: 33644550

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.