MW 298.29 Da, Purity >99%. Selective TBK1 and IKKε inhibitor (IC50 = 1-2 μM). Shows antiallergic, antiobesogenic and anti-inflammatory effects in vivo. Orally active.
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- JCI insight 7:2022The TBK1/IKKε inhibitor amlexanox improves dyslipidemia and prevents atherosclerosis.Applications:Unspecified applicationReactive species:Unspecified reactive speciesPeng Zhao,Xiaoli Sun,Zhongji Liao,Hong Yu,Dan Li,Zeyang Shen,Christopher K Glass,Joseph L Witztum,Alan R SaltielPubMed 35917178
- PLoS pathogens 18:e10103502022TBK1 and GABARAP family members suppress Coxsackievirus B infection by limiting viral production and promoting autophagic degradation of viral extracellular vesicles.Applications:Unspecified applicationReactive species:Unspecified reactive speciesSavannah Sawaged,Thomas Mota,Honit Piplani,Reetu Thakur,Deepti Lall,Elizabeth McCabe,Soojung Seo,Fayyaz S Sutterwala,Ralph Feuer,Roberta A Gottlieb,Jon SinPubMed 36044516
- Frontiers in cardiovascular medicine 8:7198052021Isoproterenol-Induced Cardiomyopathy Recovery Intervention: Amlexanox and Forskolin Enhances the Resolution of Catecholamine Stress-Induced Maladaptive Myocardial Remodeling.Applications:Unspecified applicationReactive species:Unspecified reactive speciesGabriel Komla Adzika,Hongjian Hou,Adebayo Oluwafemi Adekunle,Ruqayya Rizvi,Joseph Adu-Amankwaah,Wenkang Shang,Kexue Li,Qi-Ming Deng,Richard Mprah,Marie Louise Ndzie Noah,Hong SunPubMed 34901202
- Frontiers in cell and developmental biology 9:7193512021Amlexanox and Forskolin Prevents Isoproterenol-Induced Cardiomyopathy by Subduing Cardiomyocyte Hypertrophy and Maladaptive Inflammatory Responses.Applications:Unspecified applicationReactive species:Unspecified reactive speciesGabriel Komla Adzika,Hongjian Hou,Adebayo Oluwafemi Adekunle,Ruqayya Rizvi,Seyram Yao Adzraku,Kexue Li,Qi-Ming Deng,Richard Mprah,Marie Louise Ndzie Noah,Joseph Adu-Amankwaah,Jeremiah Ong'achwa Machuki,Wenkang Shang,Tongtong Ma,Stephane Koda,Xianluo Ma,Hong SunPubMed 34631707
- EBioMedicine 70:1035152021Translational readthrough of ciliopathy genes BBS2 and ALMS1 restores protein, ciliogenesis and function in patient fibroblasts.Applications:Unspecified applicationReactive species:Unspecified reactive speciesJonathan Eintracht,Elizabeth Forsythe,Helen May-Simera,Mariya MoosajeePubMed 34365092
- Cell metabolism 32:1012-1027.e72020TANK-Binding Kinase 1 Regulates the Localization of Acyl-CoA Synthetase ACSL1 to Control Hepatic Fatty Acid Oxidation.Applications:Unspecified applicationReactive species:Unspecified reactive speciesJin Young Huh,Shannon M Reilly,Mohammad Abu-Odeh,Anne N Murphy,Sushil K Mahata,Jinyu Zhang,Yoori Cho,Jong Bae Seo,Chao-Wei Hung,Courtney R Green,Christian M Metallo,Alan R SaltielPubMed 33152322
- Nature communications 9:8632018FcαRI co-stimulation converts human intestinal CD103 dendritic cells into pro-inflammatory cells through glycolytic reprogramming.Applications:Unspecified applicationReactive species:Unspecified reactive speciesIvo S Hansen et. al.PubMed 29491406
- Cell 172:731-743.e122018TBK1 at the Crossroads of Inflammation and Energy Homeostasis in Adipose Tissue.Applications:Unspecified applicationReactive species:Unspecified reactive speciesPeng Zhao,Kai In Wong,Xiaoli Sun,Shannon M Reilly,Maeran Uhm,Zhongji Liao,Yuliya Skorobogatko,Alan R SaltielPubMed 29425491
- Addiction biology 23:889-9032017Chronic ethanol consumption: role of TLR3/TRIF-dependent signaling.Applications:Unspecified applicationReactive species:Unspecified reactive speciesGizelle M McCarthy,Anna S Warden,Courtney R Bridges,Yuri A Blednov,R Adron HarrisPubMed 28840972
Key facts
- CAS number
- 68302-57-8
- Purity
- > 99%
- Form
- Solid
- Molecular weight
- 298.29 Da
- Molecular formula
- C16H14N2O4
- PubChem identifier
- 2161
- Nature
- Synthetic
Target data
Alternative names
EC 2.7.11.1, FLJ11330, FTDALS4, I-kappa-B kinase epsilon, IKK related kinase epsilon, IKK-epsilon, IKK-i, IKKE_HUMAN, IkBKE, Inducible I kappa-B kinase, Inhibitor of kappa light polypeptide gene enhancer in B cells kinase epsilon, Inhibitor of kappa light polypeptide gene enhancer in B cells, kinase of, epsilon, Inhibitor of nuclear factor kappa-B kinase subunit epsilon, KIAA0151, MGC125294, MGC125295, MGC125297, NAK, NF kB activating kinase, NF-kappa-B-activating kinase, Serine/threonine-protein kinase TBK1, T2K, TANK-binding kinase 1, TBK1_HUMAN
Recommended products
MW 298.29 Da, Purity >99%. Selective TBK1 and IKKε inhibitor (IC50 = 1-2 μM). Shows antiallergic, antiobesogenic and anti-inflammatory effects in vivo. Orally active.
Key facts
- CAS number
- 68302-57-8
- Purity
- > 99%
- Form
- Solid
- Molecular weight
- 298.29 Da
- Molecular formula
- C16H14N2O4
- PubChem identifier
- 2161
- Nature
- Synthetic
- Solubility
Soluble in DMSO to 100 mM.
- Biochemical name
- Amlexanox
- Biological description
Selective TBK1 and IKKε inhibitor (IC50 = 1-2 μM). Shows antiallergic, antiobesogenic and anti-inflammatory effects in vivo. Orally active.
- Canonical SMILES
- CC(C)C1=CC2=C(C=C1)OC3=NC(=C(C=C3C2=O)C(=O)O)N
- InChI
- InChI=1S/C16H14N2O4/c1-7(2)8-3-4-12-9(5-8)13(19)10-6-11(16(20)21)14(17)18-15(10)22-12/h3-7H,1-2H3,(H2,17,18)(H,20,21)
- InChIKey
- SGRYPYWGNKJSDL-UHFFFAOYSA-N
- IUPAC name
- 2-amino-5-oxo-7-propan-2-ylchromeno[2,3-b]pyridine-3-carboxylic acid
Storage
- Shipped at conditions
- Ambient - Can Ship with Ice
- Appropriate short-term storage conditions
- Ambient
- Appropriate long-term storage conditions
- Ambient
- Storage information
- The product can be stored for up to 12 months
Supplementary info
- This supplementary information is collated from multiple sources and compiled automatically.
- Activity summary
The NAK/TBK1 also known by its alternate names IKKi or IKKε is a serine/threonine kinase enzyme with a molecular mass of about 84 kDa. This protein is highly expressed in tissues including the spleen thymus and pancreas. It functions mechanically by phosphorylating target substrates which modifies their activity and impacts downstream signaling processes. TBK1 and IKKε share a similar structure and therefore can perform overlapping roles in cell signaling reflecting their critical importance in maintaining cellular responses.
- Biological function summary
This kinase plays a role in the innate immune response and acts as an important regulator for synthesizing type I interferons. TBK1 and IKKε are part of a larger complex that includes other kinases such as TRAF3 and TRAF6 which activate transcription factors like IRF3 and NF-κB. Through this regulation TBK1 and IKKε enzymes execute functions necessary for antiviral defense and inflammation impacting cell proliferation and survival.
- Pathways
TBK1 and IKKε are integral to the Toll-like receptor (TLR) and RIG-I-like receptor (RLR) signaling pathways. These pathways drive the production of pro-inflammatory cytokines and type I interferons orchestrating a robust antiviral response. TBK1 collaborates with proteins such as IRF3 and IRF7 to propagate signals that help in counteracting viral replication. Its role in these pathways enhances the body's ability to recognize and respond to pathogenic threats.
- Associated diseases and disorders
TBK1 and IKKε are linked to conditions such as cancer and inflammatory diseases. Dysregulation of TBK1 activity often associates with heightened inflammation and malignancies including lung adenocarcinomas. Co-factors like TRAF3 can regulate TBK1-related signaling in pathological conditions influencing cell survival and immune evasion in tumors. The understanding of TBK1 and IKKε in these contexts highlights their importance as potential targets for therapeutic intervention.
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Chemical Structure - Amlexanox, TBK1 and IKKepsilon inhibitor (ab142825)
2D chemical structure image of ab142825, Amlexanox, TBK1 and IKKepsilon inhibitor
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