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Technical Data
| Formula | C16H14N2O4 |
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| Molecular Weight | 298.29 | CAS No. | 68302-57-8 | |
| Solubility (25°C)* | In vitro | DMSO | 15 mg/mL (50.28 mM) | |
| Water | Insoluble | |||
| Ethanol | Insoluble | |||
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* <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.) |
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Biological Activity
| Description | Amlexanox is an anti-inflammatory antiallergic immunomodulator and also an inhibitor of the protein kinases TBK1 and IKK-ε. | ||
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| 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] |
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| Animal Study:[1] |
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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 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
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.