All AbMole products are for research use only, cannot be used for human consumption.
Amlexanox is a specific inhibitor of IKKε and TBK1. Amlexanox blocked IKKε activity with a half maximal inhibitory concentration of approximately 1–2 μM. Amlexanox increased phosphorylation of TBK1 on Ser172 in 3T3-L1 adipocytes. Mice treated with amlexanox concurrently with HFD had improved glucose tolerance, with an approximate 30–40% reduction in the area under the curve for glucose. After a 100mg dose of 5% amlexanox topical paste, applied directly to the lesion, the maximum serum concentration of the drug was 120 ng/mL, which was achieved 2.4 hours after application.
| Molecular Weight | 298.29 |
| Formula | C16H14N2O4 |
| CAS Number | 68302-57-8 |
| Solubility (25°C) | DMSO ≥ 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[3] Bell J. Clin Drug Investig. Amlexanox for the treatment of recurrent aphthous ulcers.
| Related IκB/IKK Products |
|---|
| ACHP
ACHP is a selective and orally active IκB kinase inhibitor with IC50 values of 8.5 nM and 250 nM for IKKβ and IKKα, respectively. |
| BMS-066
BMS-066 is an IKKβ/Tyk2 pseudokinase inhibitor, with IC50s of 9 nM and 72 nM, respectively. |
| Ainsliadimer A
Ainsliadimer A is a novel guaiacolide sesquiterpene dimer isolated from Ainsliaea macrocephala.Ainsliadimer A can block the NF-κB signaling pathway by binding to IKK α/β, and possesses anti-tumor and anti-inflammatory activities.Meanwhile, Ainsliadimer A can also Ainsliadimer A can also directly target peroxidase 1 and 2 (PRDX1 and PRDX2) and significantly inhibit their enzymatic activities. In addition, Ainsliadimer A can cause mitochondrial dysfunction by altering the permeability of mitochondrial membrane potential, inhibiting mitochondrial respiration and ATP production, inhibiting cell proliferation, promoting cell cycle arrest in G2/M phase, and inducing apoptosis. |
| IKK2-IN-4
IKK2-IN-4 is a potent IKK-2 inhibitor, with an IC50 of 25 nM. |
| MRT67307 dihydrochloride
MRT67307 dihydrochloride is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively. |
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