Name: Amlexanox
Brand: Selleck Chemicals
SKU: S3648
Availability: InStock
Rating: 5 (17 reviews)

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Quality Control

Batch: Purity: 99.93%

99.93

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Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description
ARPE-19 cells	Function assay	1 μM		Inhibition of TBK1 by Amlx (1 µM) reduces HG-induced mitophagic flux
HCT-116	Function assay	100 μM	48 h	Amlexanox stimulates expression from a NMD reporter vector.
PC3	Function assay	20 nM, 100 nM, 1μM and 5 μM		leads to dosage-dependent downregulation of EMT-inducing transcriptional factors Zeb1 and N-cadherin, and upregulation of epithelial-specific protein E-cadherin
DU145	Function assay	20 nM, 100 nM, 1μM and 5 μM		leads to dosage-dependent downregulation of EMT-inducing transcriptional factors Zeb1 and N-cadherin, and upregulation of epithelial-specific protein E-cadherin
U87	Proliferation assay	0-300 μM	24, 48, 72 and 96 h	The IC50 values for 72 h of amlexanox treatment were approximately 140 μM in U87 cells.
U251	Proliferation assay	0-300 μM	24, 48, 72 and 96 h	The IC50 values for 72 h of amlexanox treatment were approximately 120 μM in U251 cells.
NIH 3T3 cells	Function assay	1 mM or 0.375 mM	24 h	Cells exhibited a dramatic change in their morphology that included a larger and more flattened phenotype and often displayed long processes that are stable for at least 10 days
HUVEC	Function assay	1 mM or 0.375 mM	24 h	modify cell morphology
Swiss 3T3	Function assay	1 mM	10-360 min	Amlexanox was able to stimulate the tyrosine phosphorylation of cortactin in a rapid and sustained manner.
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 59 mg/mL (197.79 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.100mg/ml (7.04mM)	Taking the 1 mL working solution as an example, add 50 μL of 42 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.100mg/ml (7.04mM)	Taking the 1 mL working solution as an example, add 50 μL of 42 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	298.29	Formula	C₁₆H₁₄N₂O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	68302-57-8	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	CHX-3673, Amoxanox, AA-673			Smiles	CC(C)C1=CC2=C(C=C1)OC3=NC(=C(C=C3C2=O)C(=O)O)N

Mechanism of Action

Targets/IC₅₀/Ki	TBK1 IKK-ε
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. This compound 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 this chemical is competitive for its substrate ATP, indicating that it interacts with the enzymes in the ATP-binding site. It 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.
In vivo	Treatment of obese mice with amlexanox elevates energy expenditure through increased thermogenesis, producing weight loss, improves insulin sensitivity and decreases steatosis.
References	[1] https://pubmed.ncbi.nlm.nih.gov/23396211/

Applications

Methods	Biomarkers	Images	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
Growth inhibition assay	Cell viability		29048430

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Amlexanox Immunology & Inflammation related modulator

Chemical Structure

Molecular Weight: 298.29