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Chemical Structure| 68302-57-8 Chemical Structure| 68302-57-8
Chemical Structure| 68302-57-8

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CAS No.: 68302-57-8

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Amlexanox (AA673; Amoxanox; CHX3673) is a specific inhibitor of IKKε and TBK1, inhibiting IKKε and TBK1 activity determined by MBP phosphorylation with an IC50 of approximately 1-2 μM.

Synonyms: AA673; Amoxanox; Elics

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Product Details of Amlexanox

CAS No. :68302-57-8
Formula : C16H14N2O4
M.W : 298.29
SMILES Code : CC(C)C1=CC=C2OC3=C(C=C(C(O)=O)C(N)=N3)C(=O)C2=C1
Synonyms :
AA673; Amoxanox; Elics
MDL No. :MFCD00864790
InChI Key :SGRYPYWGNKJSDL-UHFFFAOYSA-N
Pubchem ID :2161

Safety of Amlexanox

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of Amlexanox

pyroptosis
TLR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description Reference
Human bone marrow mesenchymal stem cells (hBMSCs) 1.5 μM 24 h To assess AM’s potential for improving osteogenesis, leading to increased osteogenic marker gene expression and β-catenin activity. PMC11489180
THP-1 cells 100-200 μM 4 hours To evaluate the inhibitory effect of Amlexanox on the cGAS/STING signaling pathway. Results showed that Amlexanox significantly inhibited the levels of p-p65 and p-IRF3 but enhanced TBK1 phosphorylation. PMC10916235
NSC-34 cells 200 μM To evaluate the inhibitory effect of Amlexanox on ALS-related toxic protein-mediated cGAS/STING signaling. Results showed that Amlexanox inhibited the levels of p-p65 and p-IRF3 but had no significant effect on TBK1 phosphorylation. PMC10916235
HEC-1A cells 50, 100, 200 μM 24 hours To evaluate the effect of Amlexanox on the proliferation of endometrial cancer cells, results showed that Amlexanox significantly inhibited the proliferation of HEC-1A cells. PMC11667804
Ishikawa cells 50, 100, 200 μM 24 hours To evaluate the effect of Amlexanox on the proliferation of endometrial cancer cells, results showed that Amlexanox significantly inhibited the proliferation of Ishikawa cells. PMC11667804
bone marrow-derived dendritic cells (BMDCs) 2 to 200 μM 12 hours ALX significantly inhibited the proliferation and maturation of BMDCs, characterized by the reduced MHCII, a co-stimulatory molecule, IL12, and IL-23 expression, along with morphological alterations. PMC6396467

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description Reference
BALB/c nude mice NSCLC xenografted tumor models Intraperitoneal injection 25 mg/kg twice per week to inhibit the progression of Gefitinib-resistant NSCLC PMC11022703
C57BL/6J mice ovariectomized (OVX) mice Intragastric administration 50 mg/kg and 100 mg/kg daily for eight weeks To evaluate the ability of AM to enhance bone formation, suppress fat accumulation, and improve bone microarchitecture. PMC11489180
BALB/c Nude mice Endometrial cancer xenograft model Intraperitoneal injection 5 mg/kg Once daily for two weeks To evaluate the effect of Amlexanox on tumor growth in an endometrial cancer xenograft model, results showed that Amlexanox significantly inhibited tumor growth. PMC11667804
C57BL/6 mice experimental autoimmune encephalomyelitis (EAE) Oral 50 mg/kg twice daily, starting on the immunization day ALX significantly attenuated the EAE development by decreasing inflammatory infiltration and demyelination in the spinal cords, accompanied by reduced frequency of splenic pathogenic Th1 and Th17 cells and increased Tregs. PMC6396467
BKS-DB/Nju (db/db) mice Type 2 diabetes painful diabetic neuropathy (PDN) model Oral gavage 5, 25, or 100 mg/kg Once daily for four weeks Amlexanox, as a TBK1 inhibitor, could effectively improve neuropathic pain in PDN mice, suppress spinal cord inflammation, and improve peripheral nerve injury. PMC11264750
C57BL/6J mice Diet-induced obese (DIO) mice Oral gavage 25 mg/kg Daily for 8 days Amlexanox treatment resulted in a 17% loss of body weight, 26% reduction in blood glucose levels, 41% reduction in liver weight, and 76% reduction in hepatic lipid accumulation. PMC7710607
C57Bl/6 mice High-fat diet-induced obese mice Oral gavage 25 or 100 mg/kg Daily for 12 weeks Amlexanox treatment prevented the weight gain produced by HFD; drug-treated mice maintained weights equivalent to those of vehicle-treated control diet mice throughout 12 weeks. PMC3594079

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT03237533 Oral Lichen Planus Early Phase 1 Recruiting December 31, 2017 Pakistan ... More >> The university of Faisalabad Recruiting Faisalābād, Punjab, Pakistan, 38000 Contact: Sadaf Rashid, BDS ?? +923237791689 ?? durr_e_sadaf@hotmail.com ?? Contact: Arsalan Wahid, M. Phil ?? +923216685228 ?? dr.arsalanmalik@gmail.com Less <<
NCT01975935 Diabetes Mellitus Type 2 ... More >> Non-alcoholic Fatty Liver Disease Obesity Less << Phase 2 Completed - United States, Michigan ... More >> University of Michigan Ann Arbor, Michigan, United States, 48109 Less <<
NCT01975935 - Completed - -
NCT01083875 Oral Mucositis Phase 2 Completed - United States, Alabama ... More >> Mobile Infirmary Medical Center Mobile, Alabama, United States, 36607 United States, Arkansas University of Arkansas Medical School Little Rock, Arkansas, United States, 72205 United States, California Florence Wheeler Cancer Center Bakersfield, California, United States, 93301 United States, Connecticut University of Connecticut Health Center Farmington, Connecticut, United States, 06030 United States, Florida ICSL Clinical Studies Melbourne, Florida, United States, 32935 United States, Illinois Loyola University Medical Center Maywood, Illinois, United States, 60115 United States, Massachusetts Beth Israel Deaconess Medical Center Boston, Massachusetts, United States, 02215 United States, Michigan Wayne State University School of Medicine Detroit, Michigan, United States, 48201 United States, Tennessee University of Tennessee Memphis, Tennessee, United States, 38163 St. Thomas Hospital Nashville, Tennessee, United States, 37202 United States, Texas Arlington Cancer Center Arlington, Texas, United States, 76012 Corpus Christi Cancer Center Corpus Christi, Texas, United States, 78412 Less <<
NCT01842282 Diabetes Mellitus Type 2|Non A... More >>lcoholic Fatty Liver Disease|Obesity Less << PHASE2 TERMINATED 2014-02-25 University of Michigan, Ann Ar... More >>bor, Michigan, 48109, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.35mL

0.67mL

0.34mL

16.76mL

3.35mL

1.68mL

33.52mL

6.70mL

3.35mL

References

 

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