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AB142825

Amlexanox, TBK1 and IKKepsilon inhibitor

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(11 Publications)

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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Chemical Structure - Amlexanox, TBK1 and IKKepsilon inhibitor (AB142825)
  • Chemical Structure

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Chemical Structure - Amlexanox, TBK1 and IKKepsilon inhibitor (AB142825)

2D chemical structure image of ab142825, Amlexanox, TBK1 and IKKepsilon inhibitor

Key facts

CAS number

68302-57-8

Purity

>99%

Form

Solid

form

Molecular weight

298.29 Da

Molecular formula

C<sub>1</sub><sub>6</sub>H<sub>1</sub><sub>4</sub>N<sub>2</sub>O<sub>4</sub>

PubChem

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

Properties and storage information

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 information

This supplementary information is collated from multiple sources and compiled automatically.

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.

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.

Product protocols

Publications (11)

Recent publications for all applications. Explore the full list and refine your search

Npj gut and liver 2: PubMed40519640

2025

Unlocking therapeutic potential of amlexanox in MASH with insights into bile acid metabolism and microbiome.

Applications

Unspecified application

Species

Unspecified reactive species

Wenjing You,Jianfei Ji,Danwan Wen,Chen Wang,Xiaoli Sun,Peng Zhao

International journal of biological sciences 20:5254-5271 PubMed39430247

2024

Amlexanox Enforces Osteogenic Differentiation and Bone Homeostasis Through Inhibiting Ubiquitin-Dependent Degradation of β-Catenin.

Applications

Unspecified application

Species

Unspecified reactive species

Qian He,Zhouboran Liu,Xuan Xia,Jun Zeng,Yuling Liu,Jingqiong Xun,Meilu Liu,Yueming Mei,Ruchun Dai

JCI insight 7: PubMed35917178

2022

The TBK1/IKKε inhibitor amlexanox improves dyslipidemia and prevents atherosclerosis.

Applications

Unspecified application

Species

Unspecified reactive species

Peng Zhao,Xiaoli Sun,Zhongji Liao,Hong Yu,Dan Li,Zeyang Shen,Christopher K Glass,Joseph L Witztum,Alan R Saltiel

PLoS pathogens 18:e1010350 PubMed36044516

2022

TBK1 and GABARAP family members suppress Coxsackievirus B infection by limiting viral production and promoting autophagic degradation of viral extracellular vesicles.

Applications

Unspecified application

Species

Unspecified reactive species

Savannah Sawaged,Thomas Mota,Honit Piplani,Reetu Thakur,Deepti Lall,Elizabeth McCabe,Soojung Seo,Fayyaz S Sutterwala,Ralph Feuer,Roberta A Gottlieb,Jon Sin

Frontiers in cardiovascular medicine 8:719805 PubMed34901202

2021

Isoproterenol-Induced Cardiomyopathy Recovery Intervention: Amlexanox and Forskolin Enhances the Resolution of Catecholamine Stress-Induced Maladaptive Myocardial Remodeling.

Applications

Unspecified application

Species

Unspecified reactive species

Gabriel 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 Sun

Frontiers in cell and developmental biology 9:719351 PubMed34631707

2021

Amlexanox and Forskolin Prevents Isoproterenol-Induced Cardiomyopathy by Subduing Cardiomyocyte Hypertrophy and Maladaptive Inflammatory Responses.

Applications

Unspecified application

Species

Unspecified reactive species

Gabriel 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 Sun

EBioMedicine 70:103515 PubMed34365092

2021

Translational readthrough of ciliopathy genes BBS2 and ALMS1 restores protein, ciliogenesis and function in patient fibroblasts.

Applications

Unspecified application

Species

Unspecified reactive species

Jonathan Eintracht,Elizabeth Forsythe,Helen May-Simera,Mariya Moosajee

Cell metabolism 32:1012-1027.e7 PubMed33152322

2020

TANK-Binding Kinase 1 Regulates the Localization of Acyl-CoA Synthetase ACSL1 to Control Hepatic Fatty Acid Oxidation.

Applications

Unspecified application

Species

Unspecified reactive species

Jin 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 Saltiel

Nature communications 9:863 PubMed29491406

2018

FcαRI co-stimulation converts human intestinal CD103 dendritic cells into pro-inflammatory cells through glycolytic reprogramming.

Applications

Unspecified application

Species

Unspecified reactive species

Ivo S Hansen,Lisette Krabbendam,Jochem H Bernink,Fabricio Loayza-Puch,Willianne Hoepel,Johan A van Burgsteden,Elsa C Kuijper,Christianne J Buskens,Willem A Bemelman,Sebastiaan A J Zaat,Reuven Agami,Gestur Vidarsson,Gijs R van den Brink,Esther C de Jong,Manon E Wildenberg,Dominique L P Baeten,Bart Everts,Jeroen den Dunnen

Cell 172:731-743.e12 PubMed29425491

2018

TBK1 at the Crossroads of Inflammation and Energy Homeostasis in Adipose Tissue.

Applications

Unspecified application

Species

Unspecified reactive species

Peng Zhao,Kai In Wong,Xiaoli Sun,Shannon M Reilly,Maeran Uhm,Zhongji Liao,Yuliya Skorobogatko,Alan R Saltiel
View all publications

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