2. NF-κB
  3. IKK
  4. Amlexanox

Amlexanox  (Synonyms: AA673; Amoxanox; CHX3673)

Cat. No.: HY-B0713 Purity: 99.74%
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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.

For research use only. We do not sell to patients.

Amlexanox Chemical Structure

Amlexanox Chemical Structure

CAS No. : 68302-57-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 73 In-stock
Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Solid
5 mg USD 42 In-stock
10 mg USD 66 In-stock
50 mg USD 106 In-stock
100 mg USD 132 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 21 publication(s) in Google Scholar

Other Forms of Amlexanox:

Amlexanox Related Antibodies

Top Publications Citing Use of Products

    Amlexanox purchased from MedChemExpress. Usage Cited in: Exp Lung Res. 2023 Jan 31;1-14.  [Abstract]

    Amlexanox (25 μM; pretreat for 2 h) reverses HDM-induced MUC5AC overexpression in human bronchial epithelial cells.

    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.

    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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    IKK-α IKK-β IKK IKKε TBK1

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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.

    IC50 & Target[1]

    IKKε

    1-2 μM (IC50)

    TBK1

    1-2 μM (IC50)

    In Vitro

    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 Related Antibodies
    In Vivo

    Amlexanox (100 mg/kg, p.o.) prevents and reverses diet-induced or genetic obesity, and produces reversible weight loss in obese mice. Amlexanox also causes a significant decrease in adipose tissue mass in these mice, and an increase in circulating adiponectin. Amlexanox (25 mg/kg) significantly improves insulin sensitivity in mice with established DIO, and after four weeks of treatment, amlexanox produces marked improvements in glucose[1].
    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.
    Clinical Trial
    Molecular Weight

    298.29

    Formula

    C16H14N2O4
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(C1=C(N)N=C2C(C(C3=CC(C(C)C)=CC=C3O2)=O)=C1)O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.3524 mL 16.7622 mL 33.5244 mL
    5 mM 0.6705 mL 3.3524 mL 6.7049 mL
    View the 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.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    V2

    In Vivo:

    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.

    • Protocol 1

      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.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (8.38 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    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.

    • Protocol 1

      Add each solvent one by one:  0.5% CMC-Na/saline water

      Solubility: 20 mg/mL (67.05 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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.
    Purity & Documentation

    Purity: 99.74%

    COA (247 KB) LCMS (94 KB)

    Handling Instructions (2659 KB)
    References
    Kinase Assay
    [1]

    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.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Cell Assay
    [3]

    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.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    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.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References

    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
    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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    Amlexanox Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Amlexanox68302-57-8AA673 Amoxanox CHX3673AA 673AA-673CHX3673CHX 3673CHX-3673IKKIκB kinaseI kappa B kinaseInhibitorinhibitorinhibit

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