RAGE-antagonist-peptide-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemERAGEantagonistpeptideCat.No.:HY-P2268CASNo.:1092460-91-7分⼦式:C₅₇H₁₀₁N₁₃O₁₇S分⼦量:1272.56SequenceShortening:Ac-ELKVLMEKEL-NH2作⽤靶点:Amyloid-β作⽤通路:NeuronalSignaling储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性RAGEantagonistpeptide⼀种晚期糖化终产物(RAGE)拮抗剂。RAGEantagonistpeptide(RAP)可阻断RAGE和⼏个重配体HMGB-1、S100P、S100A4的结合。RAGEantagonistpeptide(RAP)具有抗肿瘤和抗炎活性。体外研究RAGEantagonistpeptide(RAP)reducestheabilityoftheligandstostimulateRAGEactivationofNFκBincancercellsinvitro[1].体内研究RAGEantagonistpeptide(RAP,100µg)inhibitsRAGE-mediatedBasalNFκBActivityinPDACcellsinvivo[1].RAGEantagonistpeptide(RAP)reducesthegrowthandmetastasisofpancreatictumorsandalsoinhibitedgliomatumorgrowth[1].Inmicebearingasthma,RAGEantagonistpeptide(RAP;4mg/kg;i.p.)bluntsairwayreactivity,airwayinflammationandgobletcellmetaplasia,anddecreasesreleaseofTh2cytokines.RAGEantagonistpeptidealsoreducestotal,cytoplasmicandnuclearlevelsofβ-catenin,enhancedβ-cateninphosphorylationatSer33/37/Thr41,whichtriggersubiquitination,down-regulatedexpressionofβ-catenintargetedgenes,andtendstokeepβ-cateninatthecytomembrane,shiftingβ-cateninfromasignallingactivepatterntoanadhesivefunction[2].AnimalModel:CancercellsexpressingtheNFκB-lucreporterimplantedintoimmune-deficientmice[1].Dosage:100µg.1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAdministration:Intratumoraldelivery(orintraperitoneally).Result:Systemicadministrationcausedasubstantialreduction(p<0.05)intheNFκBsignal5hafterinjection.REFERENCES[1].ThiruvengadamArumugam,etal.S100P-derivedRAGEantagonisticpeptidereducestumorgrowthandmetastasis.ClinCancerRes.2012Aug15;18(16):4356-64.[2].LihongYao,etal.Thereceptorforadvancedglycationendproductsisrequiredforβ-cateninstabilizationinachemical-inducedasthmamodel.BrJPharmacol.2016Sep;173(17):2600-13.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly