| Bioactivity | Amlexanox (AA673; Amoxanox; CHX3673) is a specific inhibitor of IKKε and TBK1, and inhibits the IKKε and TBK1 activity determined by MBP phosphorylation with an IC50 of approximately 1-2 μM. | ||||||||||||
| Invitro | Amlexanox increases phosphorylation of TBK1 on 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 IKKε and TBK1[1]. Amlexanox potently inhibits the release of histamine and leukotrienes from mast cells, basophils and neutrophils in in vitro settings, possibly through increasing intracellular cyclic AMP content in inflammatory cells, a mem-brane-stabilising effect or inhibition of calcium influx[2]. In primary bone marrow derived macrophages (BMMs), amlexanox inhibits osteoclast formation and bone resorption. At the molecular level, amlexanox suppresses RANKL-induced activation of nuclear factor-κB (NF-κB), mitogen-activated protein kinase (MAPKs), c-Fos and NFATc1. Amlexanox decreases the expression of osteoclast-specific genes, including TRAP, MMP9, Cathepsin K and NFATc1[3]. | ||||||||||||
| In Vivo | Amlexanox (100 mg/kg, p.o.) prevents and reverses diet-induced or genetic obesity, and produces reversible weight loss in obese mice. Amlexanox also causes a significant decrease in adipose tissue mass in these mice, and an increase in circulating adiponectin. Amlexanox (25 mg/kg) significantly improves insulin sensitivity in mice with established DIO, and after four weeks of treatment, amlexanox produces marked improvements in glucose[1]. Amlexanox before the first application of the paste and at each has been shown to suppress both immediate and evaluation thereafter. A categorical scale is also delayed-type hypersensitivity reactions[2]. Amlexanox (20 mg/kg) enhances osteoblast differentiation of BMSCs. In ovariectomized (OVX) mouse model, amlexanox prevents OVX-induced bone loss by suppressing osteoclast activity[3]. | ||||||||||||
| Name | Amlexanox | ||||||||||||
| CAS | 68302-57-8 | ||||||||||||
| Formula | C16H14N2O4 | ||||||||||||
| Molar Mass | 298.29 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Reilly SM, et al. An inhibitor of the protein kinases TBK1 and IKK-e improves obesity-related metabolic dysfunctions in mice. Nat Med. 2013 Mar;19(3):313-21. [2]. Bell, J. AmLexanox for the treatment of recurrent aphthous ulcers. Clin Drug Investig, 2005. 25(9): p. 555-66. [3]. Zhang Y, et al. AmLexanox Suppresses Osteoclastogenesis and Prevents Ovariectomy-Induced Bone Loss. Sci Rep. 2015 Sep 4;5:13575. |