Amoxanox (AA-673) is a high affinity, specific inhibitor of IKKε and TBK1 with IC50 of 1-2 uM for both, without effect on IKKα or IKKβ. Amoxanox (AA-673) reduces leukotriene D4- and platelet-activating factor-induced bronchoconstriction in guinea pigs, strongly suggesting an antagonistic activity against slow reacting substance of anaphylaxis. Amoxanox (AA-673) is an approved small-molecule therapeutic presently used in the clinic to treat aphthous ulcers and asthma. Amoxanox (AA-673) 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. Amoxanox (AA-673) (25 mg/kg, daily gavage) prevents and reverses diet-induced or genetic obesity, improves insulin sensitivity and glucose tolerance in obese mice. Amoxanox (AA-673) reverses hepatic steatosis, reduces chronic adipose tissue inflammation and promotes energy expenditure in adipose tissue in obese mice.
Physicochemical Properties
M.Wt
298.30
Formula
C16H14N2O4
Appearance
Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility
10 mM in DMSO
Chemical Name/SMILES
O=C(C1=C(N)N=C2C(C(C3=CC(C(C)C)=CC=C3O2)=O)=C1)O
References
1. T Saijo, et al. Int Arch Allergy Appl Immunol. 1985;77(3):315-21.
2. Zhang Y, et al. Sci Rep. 2015 Sep 4;5:13575.
3. Reilly SM, et al. Nat Med. 2013 Mar;19(3):313-21.
