Amlexanox

製品コードS3648 バッチS364803

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  
 
 
* <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.

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. 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].

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

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：

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
Amlexanox enhances the antitumor effect of anti-PD-1 antibody [ Biochem Biophys Res Commun, 2021, 560:1-6] PubMed: 33965784
IKKε phosphorylates kindlin-2 to induce invadopodia formation and promote colorectal cancer metastasis. [ Theranostics, 2020, 10(5):2358-2373] PubMed: 32104508

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。