Amlexanox

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

Amlexanox Chemical Structure

Molecular Weight(MW): 298.29

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

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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

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 MlXOSpVv[3Srb36gZZN{[Xl? MnTLNUDPxE1? M4rET2lvcGmkaYTpc44hd2ZiVFLLNUBjgSCDbXz4JEgy6oDHwsXNLUBz\WS3Y3XzJGhINWmwZIXj[YQhdWm2b4DoZYdq[yCobIX4 MUezNVAzOzZ2NR?=
HCT-116 NXXlVm1RTnWwY4Tpc44h[XO|YYm= MlvoNVAxKM7:TR?= M17zXFQ5KGh? NFTEN5pCdWyneHHuc5ghe3SrbYXsZZRmeyCneIDy[ZN{cW:wIH\yc40h[SCQTVSgdoVxd3K2ZYKgeoVkfG:{Lh?= M{\MR|MxPzF7MUKy
PC3 M37vRmZ2dmO2aX;uJIF{e2G7 NHLTd44zOCCwTTygNVAxKG6PLDCx{txOKGGwZDC1JO69VQ>? MYTs[YFleyC2bzDkc5Ni\2VvZHXw[Y5l\W62IHTve45z\We3bHH0bY9vKG:oIFXNWE1qdmS3Y3nu[{B1emGwc3PybZB1cW:wYXyg[oFkfG:{czDa[YIyKGGwZDDOMYNi\GincnnuMEBidmRidYDy[Yd2dGG2aX;uJI9nKGWyaYTo[Yxq[Wxvc4DlZ4lncWNicILveIVqdiCHLXPh[Ihmemmw MYizNFI4QTd{OB?=
DU145 NUnicmVWTnWwY4Tpc44h[XO|YYm= NH7YNWkzOCCwTTygNVAxKG6PLDCx{txOKGGwZDC1JO69VQ>? MorHcIVi\HNidH:g[I9{[WenLXTldIVv\GWwdDDkc5dvemWpdXzheIlwdiCxZjDFUXQucW6mdXPpcochfHKjboPjdolxfGmxbnHsJIZi[3SxcoOgXoVjOSCjbnSgUk1k[WSqZYLpckwh[W6mIIXwdoVofWyjdHnvckBw\iCncHn0bIVtcWGuLYPw[YNq\mmlIIDyc5RmcW5iRT3jZYRp\XKrbh?= NWjESWdIOzB{N{m3Nlg>
U87 NYfDVVBkWHKxbHnm[ZJifGmxbjDhd5NigQ>? NUf4V3JQOC1|MECg{txO NUXYXZRDOjRuIES4MEA4OiCjbnSgPVYhcA>? NIrqW2pVcGViSVO1NEB3[Wy3ZYOg[o9zKDd{4pEJbEBw\iCjbXzlfIFvd3hidILlZZRu\W62IIfldoUh[XCycn;4bY1ifGWueTCxOFDjiIoQvF2gbY4hXTh5IHPlcIx{Ng>? MVmyPVA1QDR|MB?=
U251 MYTQdo9tcW[ncnH0bY9vKGG|c3H5 MWewMVMxOCEQvF2= MYmyOEwhPDhuIEeyJIFv\CB7NjDo NIHL[WJVcGViSVO1NEB3[Wy3ZYOg[o9zKDd{4pEJbEBw\iCjbXzlfIFvd3hidILlZZRu\W62IIfldoUh[XCycn;4bY1ifGWueTCxNlDjiIoQvF2gbY4hXTJ3MTDj[Yxtey5? NFf3bFEzQTB2OESzNC=>
NIH 3T3 cells MlPUSpVv[3Srb36gZZN{[Xl? MWSxJI1OKG:{IECuN|c2KG2P NFrwToEzPCCq Ml;5R4VtdHNiZYjobYJqfGWmIHGg[JJidWG2aXOgZ4hidmenIHnuJJRp\Wm{IH3vdpBpd2yxZ4mgeIhifCCrbnPseYRm\CCjIHzhdodmeiCjbnSgcY9z\SCobHH0eIVv\WRicHjlco91gXCnIHHu[EBw\nSnbjDkbZNxdGG7ZXSgcI9v\yCycn;j[ZN{\XNidHjheEBiemVic4ThZoxmKG[xcjDheEBt\WG|dDCxNEBl[Xm| MkjHNVA6OjF7MUO=
HUVEC NVX3UGhHTnWwY4Tpc44h[XO|YYm= M4LvTlEhdU1ib4KgNE4{PzVibV2= M1;xXlI1KGh? MUjtc4Rq\nliY3XscEBud3KyaH;sc4d6 M3\SflExQTJzOUGz
Swiss 3T3 M3vLcmZ2dmO2aX;uJIF{e2G7 NV7GUINHOSCvTR?= MWmxNE0{PjBibXnu NXLm[mF3SW2uZYjhco95KHejczDhZoxmKHSxIIP0bY12dGG2ZTD0bIUhfHm{b4PpcoUheGixc4Doc5J6dGG2aX;uJI9nKGOxcoThZ5RqdiCrbjDhJJJieGmmIHHu[EB{fXO2YXnu[YQhdWGwbnXyMi=> MkjDNVA6OjF7MUO=

... Click to View More Cell Line Experimental Data

Assay
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. 

29048430
In vivo Treatment of obese mice with amlexanox elevates energy expenditure through increased thermogenesis, producing weight loss, improves insulin sensitivity and decreases steatosis[1].

Protocol

Cell Research:[1]
+ Expand
  • 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]
+ Expand
  • Animal Models: C57BL/6
  • Formulation: drinking water
  • 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)
Ethanol 1 mg/mL (3.35 mM)
Water Insoluble

* 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
Formula

C16H14N2O4

CAS No. 68302-57-8
Storage powder
in solvent
Synonyms AA-673, CHX-3673

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID