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  3. Amlexanox

Amlexanox (Synonyms: AA673; Amoxanox; CHX3673)

Cat. No.: HY-B0713 Purity: 99.73%
Handling Instructions

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

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
10 mg USD 60 In-stock
Estimated Time of Arrival: December 31
50 mg USD 96 In-stock
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100 mg USD 120 In-stock
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Customer Review

Based on 9 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Amlexanox purchased from MCE. Usage Cited in: Cell Death Dis. 2017 Aug 31;8(8):e3022.

    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.

    Amlexanox purchased from MCE. Usage Cited in: PLoS Pathog. 2018 Mar 8;14(3):e1006948.

    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 MCE. Usage Cited in: PLoS Pathog. 2018 Mar 8;14(3):e1006948.

    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 MCE. Usage Cited in: PLoS Pathog. 2018 Mar 8;14(3):e1006948.

    Cell lysates are analyzed via western blot using anti-HN and anti-GAPDH antibodies in CHX trestment.

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    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

    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].

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

    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].

    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.

    68302-57-8

    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 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (335.24 mM; Need ultrasonic)

    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
    10 mM 0.3352 mL 1.6762 mL 3.3524 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

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

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

    • 2.

      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

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

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

    *All of the co-solvents are provided by MCE.
    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
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    Keywords:

    AmlexanoxAA673 Amoxanox CHX3673AA 673AA-673CHX3673CHX 3673CHX-3673IKKIκB kinaseI kappa B kinaseInhibitorinhibitorinhibit

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