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Catalog No.S3648 Synonyms: AA-673, CHX-3673

4 publications

Amlexanox Chemical Structure

CAS No. 68302-57-8

Amlexanox (AA-673, CHX-3673) is an anti-inflammatory antiallergic immunomodulator and also an inhibitor of the protein kinases TBK1 and IKK-ε.

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Selleck's Amlexanox has been cited by 4 publications

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Biological Activity

Description Amlexanox (AA-673, CHX-3673) is an anti-inflammatory antiallergic immunomodulator and also an inhibitor of the protein kinases TBK1 and IKK-ε.
TBK1 [1]
IKK-ε [1]
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 Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
ARPE-19 cells MXjGeY5kfGmxbjDhd5NigQ>? NET6T3QyKM7:TR?= NIWwW|FKdmirYnn0bY9vKG:oIGTCT|Eh[nliQX3sfEApOeLChdM1UUkhemWmdXPld{BJTy2rbnT1Z4VlKG2rdH;wbIFocWNiZnz1fC=> MUCzNVAzOzZ2NR?=
HCT-116 NWfKXo5jTnWwY4Tpc44h[XO|YYm= MmjPNVAxKM7:TR?= Mlf1OFghcA>? Ml3LRY1t\Xijbn;4JJN1cW23bHH0[ZMh\XiycnXzd4lwdiCocn;tJIEhVk2GIILldI9zfGW{II\lZ5Rwei5? MlzMN|A4OTlzMkK=
PC3 MXvGeY5kfGmxbjDhd5NigQ>? MYmyNEBvVSxiMUCwJI5ONCBzzszNJIFv\CB3IN88US=> NGO4TZRt\WGmczD0c{Bld3OjZ3Wt[IVx\W6mZX70JIRwf26{ZXf1cIF1cW:wIH;mJGVOXC2rbnT1Z4lv\yC2cnHud4NzcXC2aX;uZYwh\mGldH;yd{Bb\WJzIHHu[EBPNWOjZHjldolvNCCjbnSgeZBz\We3bHH0bY9vKG:oIHXwbZRp\WyrYXytd5Bm[2moaXOgdJJwfGWrbjDFMYNi\Gincnnu MnTvN|AzPzl5Mki=
DU145 NIjRfGdHfW6ldHnvckBie3OjeR?= MYSyNEBvVSxiMUCwJI5ONCBzzszNJIFv\CB3IN88US=> MYXs[YFleyC2bzDkc5Ni\2VvZHXw[Y5l\W62IHTve45z\We3bHH0bY9vKG:oIFXNWE1qdmS3Y3nu[{B1emGwc3PybZB1cW:wYXyg[oFkfG:{czDa[YIyKGGwZDDOMYNi\GincnnuMEBidmRidYDy[Yd2dGG2aX;uJI9nKGWyaYTo[Yxq[Wxvc4DlZ4lncWNicILveIVqdiCHLXPh[Ihmemmw M1HnSVMxOjd7N{K4
U87 MVTQdo9tcW[ncnH0bY9vKGG|c3H5 MljzNE0{ODBizszN M3n5OFI1NCB2ODygO|Ih[W6mIEm2JIg> NXPLV2Z5XGinIFnDOVAhfmGudXXzJIZweiB5MvMAjYghd2ZiYX3s[Zhidm:6IITy[YF1dWWwdDD3[ZJmKGGycILvfIlu[XSnbImgNVQx6oDLzszNJIlvKFV6NzDj[Yxtey5? M3zu[FI6ODR6NEOw
U251 MVfQdo9tcW[ncnH0bY9vKGG|c3H5 MV2wMVMxOCEQvF2= NGfyVo4zPCxiNEisJFczKGGwZDC5OkBp MnfPWIhmKEmFNUCgeoFtfWW|IH\vdkA4OuLCiXigc4Yh[W2uZYjhco95KHS{ZXH0cYVvfCC5ZYLlJIFxeHKxeHntZZRmdHliMUKw5qCK|ryPIHnuJHUzPTFiY3XscJMv NFXBdFkzQTB2OESzNC=>
NIH 3T3 cells NFHwcXNHfW6ldHnvckBie3OjeR?= NGTnXGQyKG2PIH;yJFAvOzd3IH3N NFG3dYkzPCCq NIjsWo5E\WyuczDlfIhq[mm2ZXSgZUBlemGvYYTpZ{BkcGGwZ3WgbY4hfGinaYKgcY9zeGixbH;nfUB1cGG2IHnuZ4x2\GWmIHGgcIFz\2W{IHHu[EBud3KnIH\sZZR1\W6nZDDwbIVvd3S7cHWgZY5lKG:odHXuJIRqe3CuYYnl[EBtd26pIIDyc4Nme3OnczD0bIF1KGG{ZTDzeIFjdGViZn;yJIF1KGynYYP0JFExKGSjeYO= M3vvUFExQTJzOUGz
HUVEC MoGzSpVv[3Srb36gZZN{[Xl? M36wOlEhdU1ib4KgNE4{PzVibV2= MYeyOEBp NGXNbWhud2SrZomgZ4VtdCCvb4LwbI9td2e7 MXWxNFkzOTlzMx?=
Swiss 3T3 NIHPXnNHfW6ldHnvckBie3OjeR?= MX[xJI1O NHrO[JkyOC1|NkCgcYlv MYrBcYxmgGGwb4ige4F{KGGkbHWgeI8he3SrbYXsZZRmKHSqZTD0fZJwe2mwZTDwbI9{eGixconsZZRqd25ib3[gZ49zfGGldHnuJIlvKGFicnHwbYQh[W6mIIP1d5RicW6nZDDtZY5v\XJw MojxNVA6OjF7MUO=

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
IKKε / TBK1 / IKKβ ; 

PubMed: 23396211     

Dose response of amlexanox inhibition of IKKε and TBK1 activity as determined by MBP phosphorylation showing an IC50 of approximately 1-2 µM. Results were replicated in more than three experiments. 

MMP2 / MMP9 ; 

PubMed: 29048430     

The protein levels of MMP-2 and MMP-9 were evaluated by western blot. The results shown are representative of at least three independent experiments. Data are shown as the means±S.D. *P<0.05 and **P<0.01 compared with the control group

IKBKE / MST1 / MST2 / p-MST / LAST1 / LAST2 / p-YAP1 / YAP1 / Axl / c-Myc / Cyr61 ; 

PubMed: 29048430     

Amlexanox reduced the protein expression of the Hippo pathway through downregulation of IKBKE. (a) U87 and U251 cells were treated with various concentrations of amlexanox for 72 h. The cells were harvested, and the effects of amlexanox on the protein expression of the Hippo pathway were detected by western blot. (b) U87 and U251 cells were treated with amlexanox at 150 μM for 24, 48 and 72 h. Cell lysates were collected, and the protein expression were detected by western blot as in (a).

p-p65 / p-IκBα / S100A13 ; 

PubMed: 30670674     

HCT116 cells were treated with Dox (100 nM) for 4 days in the presence of the indicated doses of Amlexanox. Then, cell lysates were subjected to western blot analysis for the indicated proteins.

23396211 29048430 30670674
Growth inhibition assay
Cell viability; 

PubMed: 29048430     

(a and b) U87 and U251 cells were treated with amlexanox (0–300 μM) for 24, 48, 72 and 96 h, and cell vibility was detected using CCK-8 assay. 

In vivo Treatment of obese mice with amlexanox elevates energy expenditure through increased thermogenesis, producing weight loss, improves insulin sensitivity and decreases steatosis[1].


Cell Research:[1]
- Collapse
  • 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.
    (Only for Reference)
Animal Research:[1]
- Collapse
  • Animal Models: C57BL/6
  • Dosages: 25 or 100 mg per kg body weight
  • Administration: oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 59 mg/mL (197.79 mM)
Water Insoluble
Ethanol '1 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 298.29


CAS No. 68302-57-8
Storage powder
in solvent
Synonyms AA-673, CHX-3673
Smiles CC(C)C1=CC2=C(C=C1)OC3=NC(=C(C=C3C2=O)C(=O)O)N

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID