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- Amlexanox 68302-57-8

- Amlexanox 68302-57-8
Amlexanox 68302-57-8
产品描述 描述 Amlexanox (AA673; CHX3673) is a specific inhibitor of IKKε and TBK1; inhibition of IKKε and TBK1 activity as determined by MBP phosphorylation showing an IC50 of approximately 1–2 μM.
纯度 >98%储存/保存方法 Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.基本信息 别名 氨lai呫诺;AA673;Amoxanox;CHX3673外观 white to beige powder可溶性/溶解性 DMSO : 100 mg/mL(335.24 mM)生物活性 靶点 TBK1 ,IKK-εIn vitro(体外研究) Dose-response relationship of amlexanox inhibition of IKK-ɛ and TBK1 activity as determined by MBP phosphorylation showing an IC50 of approximately 1-2 μM. Amlexanox also blocks the activity of TBK1 at approximately the same concentrations but has no effect on IKK-α or IKK-β and at these concentrations do not block any other kinases from a broad panel representing most kinase families. Inhibition of IKK-ɛ or TBK1 by amlexanox is competitive for its substrate ATP, indicating that it interacts with the enzymes in the ATP-binding site. Amlexanox increases the phosphorylation of TBK1 at 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 IKK-ɛ and TBK1.In vivo(体内研究) Treatment of obese mice with amlexanox elevates energy expenditure through increased thermogenesis, producing weight loss, improves insulin sensitivity and decreases steatosis.研究领域 研究领域 CancerOncoproteins/suppressorsOncoproteinsSignal transducersCancerSignal transductionProtein phosphorylationSerine/threonine kinasesOtherEpigeneticsCell cycleKinases/PhosphatasesOtherImmunologyInnate ImmunityTLR SignalingSignal TransductionProtein PhosphorylationSer / Thr KinasesOther KinasesDrug DiscoverySmall Molecule DrugLead Compound DiscoveryAmlexanox 68302-57-8温馨提示:本产品仅作科研实验使用,不支持临床等研究
