Amlexanox
Based on 28 publication(s) in Google Scholar
Amlexanox (AA673; Amoxanox; CHX3673) is a specific inhibitor of IKKε and TBK1, and inhibits the IKKε and TBK1 activity determined by MBP phosphorylation with an IC50 of approximately 1-2 μM.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.70%
- CAS. Nr.: 68302-57-8
- Formel: C16H14N2O4
- Molecular Weight:298.29
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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Publications Citing Use of MedChemExpress (MCE) Amlexanox
More- Cancer Res. 2020 Sep 1;80(17):3580-3592. [Abstract]
- Sci Transl Med. 2025 Apr 16;17(794):eadj9095. [Abstract]
- Adv Sci (Weinh). 2026 Jun 2:e75921. [Abstract]
- Cell Death Dis. 2017 Aug 31;8(8):e3022. [Abstract]
- Cell Commun Signal. 2026 Apr 28;24(1):347. [Abstract]
- Cell Chem Biol. 2022 Jul 21;29(7):1113-1125.e6. [Abstract]
- BMC Med. 2024 Mar 5;22(1):96. [Abstract]
- J Med Chem. 2021 Oct 14;64(19):14344-14357. [Abstract]
- Oncoimmunology. 2022 Jul 1;11(1):2093054. [Abstract]
- Commun Biol. 2025 Apr 17;8(1):624. [Abstract]
- Bone Joint Res. 2025 Nov 1;14(11):927-940. [Abstract]
- Invest Ophthalmol Vis Sci. 2023 Jul 3;64(10):1. [Abstract]
- J Enzyme Inhib Med Chem. 2026 Dec;41(1):2607808. [Abstract]
- Toxicology. 2020 Oct:443:152555. [Abstract]
- Sci Rep. 2021 Dec 13;11(1):23907. [Abstract]
- Sci Rep. 2021 May 18;11(1):10481. [Abstract]
- PLoS Pathog. 2018 Mar 8;14(3):e1006948. [Abstract]
- Cell Signal. 2021 Sep:85:110068. [Abstract]
- FASEB J. 2026 Jul 15;40(13):e72080. [Abstract]
- Eur J Cell Biol. 2019 Jan;98(1):36-50. [Abstract]
- J Virol. 2022 Apr 13;96(7):e0188821. [Abstract]
- Anticancer Drugs. 2025 Jul 7. [Abstract]
- Exp Lung Res. 2023;49(1):49-62. [Abstract]
- bioRxiv. 2026 Mar 12.
- bioRxiv. 2025 Oct 15.
- SSRN. 2025 Aug 14.
- Res Sq. 2024 Aug 01.
- Elife. 2022 Jun 28;11:e78044. [Abstract]
Customer Validation & Images
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IHC
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IHC
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Biologische Aktivität
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IKKε 1-2 μM (IC50) |
TBK1 1-2 μM (IC50) |
Amlexanox increases phosphorylation of TBK1 on 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 IKKε and TBK1[1].
Amlexanox potently inhibits the release of histamine and leukotrienes from mast cells, basophils and neutrophils in in vitro settings, possibly through increasing intracellular cyclic AMP content in inflammatory cells, a mem-brane-stabilising effect or inhibition of calcium influx[2].
In primary bone marrow derived macrophages (BMMs), amlexanox inhibits osteoclast formation and bone resorption. At the molecular level, amlexanox suppresses RANKL-induced activation of nuclear factor-κB (NF-κB), mitogen-activated protein kinase (MAPKs), c-Fos and NFATc1. Amlexanox decreases the expression of osteoclast-specific genes, including TRAP, MMP9, Cathepsin K and NFATc1[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Amlexanox before the first application of the paste and at each has been shown to suppress both immediate and evaluation thereafter. A categorical scale is also delayed-type hypersensitivity reactions[2].
Amlexanox (20 mg/kg) enhances osteoblast differentiation of BMSCs. In ovariectomized (OVX) mouse model, amlexanox prevents OVX-induced bone loss by suppressing osteoclast activity[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 68302-57-8
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Appearance Solid
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Molecular Weight 298.29
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Formel C16H14N2O4
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Color White to off-white
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SMILES
O=C(C1=C(N)N=C2C(C(C3=CC(C(C)C)=CC=C3O2)=O)=C1)O
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Synonyms
AA673; Amoxanox; CHX3673
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (28)
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Journal Impact Factor
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Most Recent
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Cancer Res
FIP200 Suppresses Immune Checkpoint Therapy Responses in Breast Cancers by Limiting AZI2/TBK1/IRF Signaling Independent of Its Canonical Autophagy Function. [Abstract]2020 Sep 1;80(17):3580-3592. PMID: 32580962 -
Sci Transl Med
Condensation of cellular prion protein promotes renal fibrosis through the TBK1-IRF3 signaling axis. [Abstract]2025 Apr 16;17(794):eadj9095. PMID: 40238918 -
Adv Sci (Weinh)
NMI Regulates Adipose Adaptive Thermogenesis Through TLR4/IRF3 Signaling to Promote Obesity. [Abstract]2026 Jun 2:e75921. PMID: 42228052 -
Cell Death Dis
Amlexanox, a selective inhibitor of IKBKE, generates anti-tumoral effects by disrupting the Hippo pathway in human glioblastoma cell lines. [Abstract]2017 Aug 31;8(8):e3022. PMID: 29048430
Amlexanox purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2017 Aug 31;8(8):e3022. [Abstract]
Amlexanox reduces the protein expression of the Hippo pathway through downregulation of IKBKE. (a) U87 and U251 cells are treated with various concentrations of Amlexanox for 72 h. The cells are harvested, and the effects of Amlexanox on the protein expression of the Hippo pathway are detected by western blot. (b) U87 and U251 cells are treated with Amlexanox at 150 μM for 24, 48 and 72 h. Cell lysates are collected, and the protein expression are detected by western blot.
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Cell Commun Signal
Cytoplasmic retention of IRF3 binding Vimentin competitively with ERK1/2 mitigates acute myeloid leukemia through TFEB nuclear translocation. [Abstract]2026 Apr 28;24(1):347. PMID: 42045951 -
Cell Chem Biol
Identifying enhancers of innate immune signaling as broad-spectrum antivirals active against emerging viruses. [Abstract]2022 Jul 21;29(7):1113-1125.e6. PMID: 35728599 -
BMC Med
TBK1, a prioritized drug repurposing target for amyotrophic lateral sclerosis: evidence from druggable genome Mendelian randomization and pharmacological verification in vitro. [Abstract]2024 Mar 5;22(1):96. PMID: 38443977 -
J Med Chem
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors. [Abstract]2021 Oct 14;64(19):14344-14357. PMID: 34547896 -
Oncoimmunology
Oncolytic adenovirus promotes vascular normalization and nonclassical tertiary lymphoid structure formation through STING-mediated DC activation. [Abstract]2022 Jul 1;11(1):2093054. PMID: 35800155 -
Commun Biol
2025 Apr 17;8(1):624. PMID: 40247055 -
Bone Joint Res
Therapeutic potential of IκB kinase epsilon inhibition in preventing meniscal degeneration of early osteoarthritis. [Abstract]2025 Nov 1;14(11):927-940. PMID: 41173032 -
Invest Ophthalmol Vis Sci
TBK1 Knockdown Alleviates Axonal Transport Deficits in Retinal Ganglion Cells Via mTORC1 Activation in a Retinal Damage Mouse Model. [Abstract]2023 Jul 3;64(10):1. PMID: 37395713 -
J Enzyme Inhib Med Chem
Discovery of N8: a novel IKKε inhibitor with potent anticancer activity via cytotoxicity, migration suppression, and autophagy modulation. [Abstract]2026 Dec;41(1):2607808. PMID: 41492864 -
Toxicology
2020 Oct:443:152555. PMID: 32763286 -
Sci Rep
Non-canonical function of FIP200 is required for neural stem cell maintenance and differentiation by limiting TBK1 activation and p62 aggregate formation. [Abstract]2021 Dec 13;11(1):23907. PMID: 34903812 -
Sci Rep
G protein-coupled receptor kinase 5 deletion suppresses synovial inflammation in a murine model of collagen antibody-induced arthritis. [Abstract]2021 May 18;11(1):10481. PMID: 34006987 -
PLoS Pathog
Inclusion bodies of human parainfluenza virus type 3 inhibit antiviral stress granule formation by shielding viral RNAs. [Abstract]2018 Mar 8;14(3):e1006948. PMID: 29518158
Amlexanox purchased from MedChemExpress. Usage Cited in: PLoS Pathog. 2018 Mar 8;14(3):e1006948. [Abstract]
HeLa cells are treated with AS (0.5 mM) for 30 min and subsequently treated with or without CHX in the presence of AS for another 1 h.
Amlexanox purchased from MedChemExpress. Usage Cited in: PLoS Pathog. 2018 Mar 8;14(3):e1006948. [Abstract]
HeLa cells are treated with AS (0.5 mM) for 30 min and subsequently treated with or without CHX in the presence of AS for another 1 h.
Amlexanox purchased from MedChemExpress. Usage Cited in: PLoS Pathog. 2018 Mar 8;14(3):e1006948. [Abstract]
Cell lysates are analyzed via western blot using anti-HN and anti-GAPDH antibodies in CHX trestment.
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Cell Signal
USP39 promotes tumorigenesis by stabilizing and deubiquitinating SP1 protein in hepatocellular carcinoma. [Abstract]2021 Sep:85:110068. PMID: 34197957 -
FASEB J
Targeting the HMGB1 Pathway With Glycyrrhizic Acid and Amlexanox Attenuates RSV-Induced Injury and Viral Propagation. [Abstract]2026 Jul 15;40(13):e72080. PMID: 42359623 -
Eur J Cell Biol
Overexpression of Toll-like receptor 4 enhances LPS-induced inflammatory response and inhibits Salmonella Typhimurium growth in ovine macrophages. [Abstract]2019 Jan;98(1):36-50. PMID: 30522781 -
J Virol
2022 Apr 13;96(7):e0188821. PMID: 35319228 -
Anticancer Drugs
Combined amlexanox and anti-MCP-1 therapy suppresses tumor progression in a murine Lewis lung carcinoma model. [Abstract]2025 Jul 7. PMID: 40626452 -
Exp Lung Res
House dust mite-induced endoplasmic reticulum stress mediates MUC5AC hypersecretion via TBK1 in airway epithelium. [Abstract]2023;49(1):49-62. PMID: 36719141
Amlexanox purchased from MedChemExpress. Usage Cited in: Exp Lung Res. 2023;49(1):49-62. [Abstract]
Amlexanox (25 μM; pretreat for 2 h) reverses HDM-induced MUC5AC overexpression in human bronchial epithelial cells.
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Elife
Domain fusion TLR2-4 enhances the autophagy-dependent clearance of Staphylococcus aureus in the genetic engineering goat. [Abstract]2022 Jun 28;11:e78044. PMID: 35762728
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (335.24 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.38 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 0.5% CMC-Na/saline water
Solubility: 20 mg/mL (67.05 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
The in vitro kinase assays is performed by incubating purified kinase (IKKε or TBK1) in kinase buffer containing 25 mM Tris (pH7.5), 10 mM MgCl2, 1 mM DTT, and 10 µM ATP for 30 minutes at 30°C in the presence of 0.5 µCi γ-[32P]-ATP and 1 µg MBP per sample as a substrate. The kinase reaction is stopped by adding 4x sodium dodecyl sulfate (SDS) sample buffer and boiling for 5 minutes at 95°C. Supernatants are resolved by SDS-polyacrylamide gel electrophoresis, transferred to nitrocellulose, and analyzed by autoradiography using a Typhoon 9410 phosphorimager.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
To examine cell proliferation, a Cell Counting Kit-8 is used according to the manufacturer’s instructions. BMMs are seeded at a density of 5×103 cells/well in 96-well plates. After 24 hours, cells are treated with different concentrations of AmLexanox (0, 1.5, 3, 6, 12, 25 μM) every 2 days in the presence of M-CSF (30 ng/mL) for 7 days. After 1, 3, 5 and 7 days, the culture medium is replaced by the medium containing 10% CCK-8 and cells are incubated at 37°C for an additional 2 h. The absorbance is then measured at a wavelength of 450 nm on an ELX800 absorbance microplate reader.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Wildtype male C57BL/6 mice are fed with a HFD consisting of 45% of calories from fat starting at eight weeks of age for 12-24 weeks, while ND C57BL/6 controls are maintained on normal chow diet consisting of 4.5% fat. C57BL/6 diets are fed containing ω-3 fatty acids. Rosiglitazone treatment is administered for three weeks by addition of the compound to the diet in mice that have been on HFD for 16 weeks. Each mouse consumes on average 3.5 mg per kg rosiglitazone per day. AmLexanox is administered by daily oral gavage. For the prevention groups, amLexanox (25 mg per kg or 100 mg per kg) administration is begun concurrently with HFD feeding at eight weeks of age. For the treatment groups, 25 mg per kg amLexanox treatment is begun at 20 weeks of age after 12 weeks of HFD. To test the effect of amLexanox withdrawal, mice in the treatment group are switched from amLexanox gavage to vehicle control after eight weeks of amLexanox treatment. Control and ob/ob mice are fed with a normal chow diet and gavaged with 100 mg per kg amLexanox or vehicle control beginning at ten weeks of age. Animals are housed in a specific pathogen-free facility with a 12-hour light/12-hour dark cycle and given free access to food and water.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (280 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Reilly SM, et al. An inhibitor of the protein kinases TBK1 and IKK-e improves obesity-related metabolic dysfunctions in mice. Nat Med. 2013 Mar;19(3):313-21. [Content Brief]
[2]. Bell, J. AmLexanox for the treatment of recurrent aphthous ulcers. Clin Drug Investig, 2005. 25(9): p. 555-66. [Content Brief]
[3]. Zhang Y, et al. AmLexanox Suppresses Osteoclastogenesis and Prevents Ovariectomy-Induced Bone Loss. Sci Rep. 2015 Sep 4;5:13575. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 3.3524 mL | 16.7622 mL | 33.5244 mL | 83.8111 mL |
| 5 mM | 0.6705 mL | 3.3524 mL | 6.7049 mL | 16.7622 mL | |
| 10 mM | 0.3352 mL | 1.6762 mL | 3.3524 mL | 8.3811 mL | |
| 15 mM | 0.2235 mL | 1.1175 mL | 2.2350 mL | 5.5874 mL | |
| 20 mM | 0.1676 mL | 0.8381 mL | 1.6762 mL | 4.1906 mL | |
| 25 mM | 0.1341 mL | 0.6705 mL | 1.3410 mL | 3.3524 mL | |
| 30 mM | 0.1117 mL | 0.5587 mL | 1.1175 mL | 2.7937 mL | |
| 40 mM | 0.0838 mL | 0.4191 mL | 0.8381 mL | 2.0953 mL | |
| 50 mM | 0.0670 mL | 0.3352 mL | 0.6705 mL | 1.6762 mL | |
| 60 mM | 0.0559 mL | 0.2794 mL | 0.5587 mL | 1.3969 mL | |
| 80 mM | 0.0419 mL | 0.2095 mL | 0.4191 mL | 1.0476 mL | |
| 100 mM | 0.0335 mL | 0.1676 mL | 0.3352 mL | 0.8381 mL |
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