Home Immunology & Inflammation Immunology & Inflammation related modulator - TBK1 inhibitor - IκB/IKK inhibitor Amlexanox For research use only.

Amlexanox

Synonyms: CHX-3673, Amoxanox, AA-673

Amlexanox is an anti-inflammatory antiallergic immunomodulator and also an inhibitor of the protein kinases TBK1 and IKK-ε.

Amlexanox Chemical Structure

Amlexanox Chemical Structure

CAS: 68302-57-8

Selleck's Amlexanox has been cited by 12 publications

Purity & Quality Control

Batch: Purity: 99.93%
99.93

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
ARPE-19 cells Function assay 1 μM Inhibition of TBK1 by Amlx (1 µM) reduces HG-induced mitophagic flux 31023645
HCT-116 Function assay 100 μM 48 h Amlexanox stimulates expression from a NMD reporter vector. 30719122
PC3 Function assay 20 nM, 100 nM, 1μM and 5 μM leads to dosage-dependent downregulation of EMT-inducing transcriptional factors Zeb1 and N-cadherin, and upregulation of epithelial-specific protein E-cadherin 30279728
DU145 Function assay 20 nM, 100 nM, 1μM and 5 μM leads to dosage-dependent downregulation of EMT-inducing transcriptional factors Zeb1 and N-cadherin, and upregulation of epithelial-specific protein E-cadherin 30279728
U87 Proliferation assay 0-300 μM 24, 48, 72 and 96 h The IC50 values for 72 h of amlexanox treatment were approximately 140 μM in U87 cells. 29048430
U251 Proliferation assay 0-300 μM 24, 48, 72 and 96 h The IC50 values for 72 h of amlexanox treatment were approximately 120 μM in U251 cells. 29048430
NIH 3T3 cells Function assay 1 mM or 0.375 mM 24 h Cells exhibited a dramatic change in their morphology that included a larger and more flattened phenotype and often displayed long processes that are stable for at least 10 days 10921913
HUVEC Function assay 1 mM or 0.375 mM 24 h modify cell morphology 10921913
Swiss 3T3 Function assay 1 mM 10-360 min Amlexanox was able to stimulate the tyrosine phosphorylation of cortactin in a rapid and sustained manner. 10921913
Click to View More Cell Line Experimental Data

Biological Activity

Description Amlexanox is an anti-inflammatory antiallergic immunomodulator and also an inhibitor of the protein kinases TBK1 and IKK-ε.
Targets
TBK1 [1] IKK-ε [1]
In vitro
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].
Cell Research Cell lines 3T3-L1 adipocytes
Concentrations 12, 25, 50 μM
Incubation Time 1 h
Method 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot IKKε / TBK1 / IKKβ MMP2 / MMP9 IKBKE / MST1 / MST2 / p-MST / LAST1 / LAST2 / p-YAP1 / YAP1 / Axl / c-Myc / Cyr61 p-p65 / p-IκBα / S100A13 23396211
Growth inhibition assay Cell viability 29048430
In Vivo
In vivo Treatment of obese mice with amlexanox elevates energy expenditure through increased thermogenesis, producing weight loss, improves insulin sensitivity and decreases steatosis[1].
Animal Research Animal Models C57BL/6
Dosages 25 or 100 mg per kg body weight
Administration oral gavage

Chemical lnformation & Solubility

Molecular Weight 298.29 Formula

C16H14N2O4
CAS No. 68302-57-8 SDF Download Amlexanox SDF
Smiles CC(C)C1=CC2=C(C=C1)OC3=NC(=C(C=C3C2=O)C(=O)O)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 59 mg/mL ( (197.79 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble


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In vivo
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