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Submit ReviewAmlexanox is a selective inhibitor of TANK-binding kinase 1 (TBK1) and IKKε (IC50 values are ~1-2 μM). Displays no effect on IKKα or IKKβ at these concentrations. Reversibly lowers weight, increases insulin sensitivity, and reduces inflammation and steatosis in three mouse models of obesity. Exhibits antiallergic activity; inhibits the release of histamine from rat mast cells. Also binds to Hsp90 and inhibits C-terminal chaperone activity in vitro.
Amlexanox is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library, Tocriscreen Antiviral Library and Tocriscreen FDA-Approved Drugs. 了解 Tocris 化合物库的更多信息。
分子量 | 298.29 |
公式 | C16H14N2O4 |
储存 | Store at -20°C |
纯度 | ≥99% (HPLC) |
CAS Number | 68302-57-8 |
PubChem ID | 2161 |
InChI Key | SGRYPYWGNKJSDL-UHFFFAOYSA-N |
Smiles | CC(C)C1=CC=C2C(C(C(C=C(C(O)=O)C(N)=N3)=C3O2)=O)=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 29.83 | 100 |
以下数据基于产品分子量 298.29。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 3.35 mL | 16.76 mL | 33.52 mL |
5 mM | 0.67 mL | 3.35 mL | 6.7 mL |
10 mM | 0.34 mL | 1.68 mL | 3.35 mL |
50 mM | 0.07 mL | 0.34 mL | 0.67 mL |
参考文献是支持产品生物活性的出版物。
Reilly et al (2012) An inhibitor of the protein kinases TBK1 and IKK-ε improves obesity-related metabolic dysfunctions in mice. Nat.Med. 19 313 PMID: 23396211
Okada et al (2003) Hsp90 is a direct target of the anti-allergic drugs disodium cromoglycate and amle. Biochem.J. 374 433 PMID: 12803546
Makino et al (1987) Mechanism of action of an antiallergic agent, amle. (AA-673), in inhibiting histamine release from mast cells. Acceleration of cAMP generation and inhibition of phosphodiesterase. Int.Arch.Allergy Appl.Immunol. 82 66 PMID: 2433225
If you know of a relevant reference for Amlexanox, please let us know.
关键词: Amlexanox, Amlexanox supplier, diabetes, obese, obesity, mouse, mice, anti-inflammatory, anti-inflammatories, metabolic, disorders, diseases, IkB, kinase, IkappaB, IκB, IKK, TBK1, TANK-binding, 1, noncanonical, Kinase, NF-kB/IkB, Histaminergic-Related, Compounds, TANK, binding, (TBK), 4857, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Amlexanox 的部分引用包括:
Neysan et al (2021) Genotoxic stress in constitutive trisomies induces autophagy and the innate immune response via the cGAS-STING pathway. Commun Biol 4 831 PMID: 34215848
Lin et al (2021) A naturally derived small molecule NDSM253 inhibits IKK1 to suppress inflammation response and promote bone healing after fracture. Am J Transl Res 13 24-37 PMID: 33527006
Harold I et al (2021) Tank Binding Kinase 1 modulates spindle assembly checkpoint components to regulate mitosis in breast and lung cancer cells. Biochim Biophys Acta Mol Cell Res 1868 118929 PMID: 33310066
Alrahbeni et al (2015) Full UPF3B function is critical for neuronal differentiation of neural stem cells. Br J Pharmacol 8 33 PMID: 26012578
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