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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 ≥ 60 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 |
|---|
| BAY 11-7082
BAY 11-7082 is an inhibitor of cytokine-induced IκB-α phosphorylation (IC50 ~ 10 μM). BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 (IC50=0.19, 0.96 μM, respectively). |
| SC-514
SC-514 is a selective and reversible inhibitor of IκB kinase 2 (IKK2) with IC50 of 3-12 μM. |
| TPCA-1
TPCA-1 is an inhibitor of IKK-2 with IC50 of 17.9 nM. |
| BMS-345541 hydrochloride
BMS-345541 hydrochloride is a selective inhibitor of the catalytic subunits of IKK (IC50 values of 0.3 μM and 4 μM for IKK-2 and IKK-1 respectively). BMS-345541 binds at an allosteric site of IKK. |
| Bardoxolone Methyl
Bardoxolone Methyl is an IKK inhibitor with potent pro-apoptotic and anti-inflammatory activities, as well as an activator of the Nrf2 pathway and an inhibitor of the NF-κB pathway. |
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