Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemERAGEantagonistpeptideCat.No.:HY-P2268CASNo.:1092460-91-7分?式:C??H???N??O??S分?量:1272.56SequenceShortening:Ac-ELKVLMEKEL-NH2作?靶點(diǎn):Amyloid-β作?通路:NeuronalSignaling儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性RAGEantagonistpeptide?種晚期糖化終產(chǎn)物(RAGE)拮抗劑。RAGEantagonistpeptide(RAP)可阻斷RAGE和?個(gè)重配體HMGB-1、S100P、S100A4的結(jié)合。RAGEantagonistpeptide(RAP)具有抗腫瘤和抗炎活性。體外研究RAGEantagonistpeptide(RAP)reducestheabilityoftheligandstostimulateRAGEactivationofNFκBincancercellsinvitro[1].體內(nèi)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?邊的抑制劑?師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