Amlexanox (AA-673)

Catalog No.S3648 Synonyms: CHX-3673, Amoxanox

For research use only.

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

Amlexanox (AA-673) Chemical Structure

CAS No. 68302-57-8

Selleck's Amlexanox (AA-673) has been cited by 8 Publications

Purity & Quality Control

Choose Selective Immunology & Inflammation related Inhibitors

Biological Activity

Description Amlexanox (AA-673, CHX-3673, Amoxanox) 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 NIPGNVNHfW6ldHnvckBie3OjeR?= NUDDcmJuOSEQvF2= M2rlN2lvcGmkaYTpc44hd2ZiVFLLNUBjgSCDbXz4JEgy6oDHwsXNLUBz\WS3Y3XzJGhINWmwZIXj[YQhdWm2b4DoZYdq[yCobIX4 MUezNVAzOzZ2NR?=
HCT-116 M17NPWZ2dmO2aX;uJIF{e2G7 MkL6NVAxKM7:TR?= Mo\KOFghcA>? NXO3UYtjSW2uZYjhco95KHO2aX31cIF1\XNiZYjwdoV{e2mxbjDmdo9uKGFiTl3EJJJmeG:{dHXyJJZm[3Sxcj6= M2XlWlMxPzF7MUKy
PC3 MXnGeY5kfGmxbjDhd5NigQ>? NUDvfYFWOjBibl2sJFExOCCwTTygNe69VSCjbnSgOUDPxE1? NWH2SHNzdGWjZIOgeI8h\G:|YXflMYRmeGWwZHXueEBld3ewcnXneYxifGmxbjDv[kBGVVRvaX7keYNqdmdidILhcpNkemmydHnvcoFtKG[jY4TvdpMhYmWkMTDhcoQhVi2lYXTo[ZJqdixiYX7kJJVxemWpdXzheIlwdiCxZjDldIl1cGWuaXHsMZNx\WOrZnnjJJBzd3SnaX6gSU1k[WSqZYLpci=> M2ruPVMxOjd7N{K4
DU145 M4O1dWZ2dmO2aX;uJIF{e2G7 NVTCZow{OjBibl2sJFExOCCwTTygNe69VSCjbnSgOUDPxE1? NGXGVJBt\WGmczD0c{Bld3OjZ3Wt[IVx\W6mZX70JIRwf26{ZXf1cIF1cW:wIH;mJGVOXC2rbnT1Z4lv\yC2cnHud4NzcXC2aX;uZYwh\mGldH;yd{Bb\WJzIHHu[EBPNWOjZHjldolvNCCjbnSgeZBz\We3bHH0bY9vKG:oIHXwbZRp\WyrYXytd5Bm[2moaXOgdJJwfGWrbjDFMYNi\Gincnnu MX2zNFI4QTd{OB?=
U87 Mk\LVJJwdGmoZYLheIlwdiCjc4PhfS=> NXn4dGZZOC1|MECg{txO NGmzWHkzPCxiNEisJFczKGGwZDC5OkBp NVnuSVJ2XGinIFnDOVAhfmGudXXzJIZweiB5MvMAjYghd2ZiYX3s[Zhidm:6IITy[YF1dWWwdDD3[ZJmKGGycILvfIlu[XSnbImgNVQx6oDLzszNJIlvKFV6NzDj[Yxtey5? MXOyPVA1QDR|MB?=
U251 MUPQdo9tcW[ncnH0bY9vKGG|c3H5 M1freFAuOzByIN88US=> MluwNlQtKDR6LDC3NkBidmRiOU[gbC=> MlLQWIhmKEmFNUCgeoFtfWW|IH\vdkA4OuLCiXigc4Yh[W2uZYjhco95KHS{ZXH0cYVvfCC5ZYLlJIFxeHKxeHntZZRmdHliMUKw5qCK|ryPIHnuJHUzPTFiY3XscJMv NW\4bYkyOjlyNEi0N|A>
NIH 3T3 cells NIPLWnBHfW6ldHnvckBie3OjeR?= NUnoSHlxOSCvTTDvdkAxNjN5NTDtUS=> MkjUNlQhcA>? M2LUSmNmdGy|IHX4bIljcXSnZDDhJIRz[W2jdHnjJINp[W6pZTDpckB1cGWrcjDtc5JxcG:ub3f5JJRp[XRiaX7jcJVl\WRiYTDsZZJo\XJiYX7kJI1wemViZnzheJRmdmWmIIDo[Y5wfHmyZTDhcoQhd2[2ZX6g[Il{eGyjeXXkJIxwdmdicILvZ4V{e2W|IIToZZQh[XKnIIP0ZYJt\SCob4KgZZQhdGWjc4SgNVAh\GG7cx?= MnTxNVA6OjF7MUO=
HUVEC MmjkSpVv[3Srb36gZZN{[Xl? M4PGTFEhdU1ib4KgNE4{PzVibV2= MlHJNlQhcA>? MoHycY9lcW[7IHPlcIwhdW:{cHjvcI9ogQ>? MoLTNVA6OjF7MUO=
Swiss 3T3 MofoSpVv[3Srb36gZZN{[Xl? MkPINUBuVQ>? MX[xNE0{PjBibXnu M1rI[2FudGW6YX7vfEB4[XNiYXLs[UB1dyC|dHnteYxifGVidHjlJJR6em:|aX7lJJBpd3OyaH;yfYxifGmxbjDv[kBkd3K2YXP0bY4hcW5iYTDyZZBq\CCjbnSgd5V{fGGrbnXkJI1idm6ncj6= MVuxNFkzOTlzMx?=
Assay
Methods Test Index PMID
Western blot IKKε / TBK1 / IKKβ ; MMP2 / MMP9 ; IKBKE / MST1 / MST2 / p-MST / LAST1 / LAST2 / p-YAP1 / YAP1 / Axl / c-Myc / Cyr61 ; p-p65 / p-IκBα / S100A13 23396211 29048430 30670674
Growth inhibition assay Cell viability 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 (from reference)

Cell Research:[1]
  • 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]
  • 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
Formula

C16H14N2O4

CAS No. 68302-57-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)C1=CC2=C(C=C1)OC3=NC(=C(C=C3C2=O)C(=O)O)N

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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