Amlexanox

製品コードS3648 バッチS364804

印刷

化学情報

Chemical Structure Synonyms CHX-3673, Amoxanox, AA-673 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C16H14N2O4
分子量 298.29 CAS No. 68302-57-8
Solubility (25°C)* 体外 DMSO 60 mg/mL (201.14 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Amlexanox is an anti-inflammatory antiallergic immunomodulator and also an inhibitor of the protein kinases TBK1 and IKK-ε.
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. This compound 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 this chemical is competitive for its substrate ATP, indicating that it interacts with the enzymes in the ATP-binding site. It 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].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 3T3-L1 adipocytes
濃度 12, 25, 50 μM
反応時間 1 h
実験の流れ 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.
動物実験 動物モデル C57BL/6
投薬量 25 or 100 mg per kg body weight
投与方法 oral gavage

参考

  • https://pubmed.ncbi.nlm.nih.gov/23396211/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Development of a TBK1 and ALK dual inhibitor for alleviating depressive behavior via anti-inflammatory effects [ Biomed Pharmacother, 2025, 186:117991] PubMed: 40117902
Development of translational read-through-inducing drugs as novel therapeutic options for patients with Fanconi anemia [ Cell Death Discov, 2025, 11(1):286] PubMed: 40544182
Noncanonical role of Golgi-associated macrophage TAZ in chronic inflammation and tumorigenesis [ Sci Adv, 2025, 11(4):eadq2395] PubMed: 39841821
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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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