PQA-18-生命科學(xué)試劑-MCE-3779

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPQA-18Cat.No.:HY-171034CASNo.:1604678-82-1分?式:C??H??NO?分?量:409.52作?靶點(diǎn):InterleukinRelated;TNFReceptor;PAK作?通路:Immunology/Inflammation;Apoptosis;CellCycle/DNADamage;Cytoskeleton儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性PQA-18?種獨(dú)特的PAK2抑制劑(IC50:10nM)。PQA-18具有免疫抑制活性，可抑制IL2、IL4、IL6和TNFα產(chǎn)?。PQA-18可抑制??中調(diào)節(jié)性T細(xì)胞亞群的數(shù)量和針對T細(xì)胞依賴性抗原的免疫球蛋?(Ig)的產(chǎn)?，并可減輕??的?炎癥狀[1]。IC50&TargetPAK2IL-6IL4IL-210nM(IC50)體外研究PQA-18(0.1-20μM,6-24h)markedlyinhibitsConA(HY-P2149)-inducedproductionofIL2,IL4,IL6andTNFαinhumanperipherallymphocytes(IC50:450,650,580and460nM,respectively)andIL2productionatprotein(IC50:400nM)andmRNAlevelsinJurkatcells[1].PQA-18(10μM)attenuatesthephosphorylationofcofilin-1andhistoneH4byinhibitingthecorrespondingkinases[1].PQA-18(0.1nM-1μM)inhibitsPAK2kinaseactivityinanon-competitiveandconcentration-dependentmannerbyitsautophosphorylationatSer141(IC50of10nM,Kmof2.1μM)[1].RealTimeqPCR[1]CellLine:JurkatcellsculturedwithConAConcentration:1,10,20μMIncubationTime:6h1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEResult:SuppressedIL2mRNAlevelinConA-stimulatedJurkatcells.Affected-50%ofIL2transcriptsatahighdose(10μM).體內(nèi)研究PQA-18(0.5mg/kg,i.p.,threetimesaweek)displaysimmunosuppressingactivityinC57BL/6JmiceimmunizedwithNP-CGG,withinhibitingthepopulationofasubsetofregulatoryTcellsandtheimmunoglobulin(Ig)productionagainstTcell-dependentantigens[1].PQA-18ointment(100mg/mouse,contains0.05%-0.1%PQA-18,threetimesaweek,17weeks)improvesdermatitisandIgElevelsinNc/Ngamice[1].AnimalModel:MaleC57BL/6Jmice(10weeksold)immunizedbyintraperitonealinjectionof50μgNP-CGG[1]Dosage:0.5mg/kgAdministration:Intraperitonealinjection(i.p.);threetimesaweekResult:SuppressedtheNP-specificresponses(IgM,IgG1,andIgG3)inperipheralblood.SignificantlysuppressedthenumberofFoxp3+CD4+CD25+cellsinspleens.REFERENCES[1].OguraM,etal.PrenylatedquinolinecarboxylicacidderivativesuppressesimmuneresponsethroughinhibitionofPAK2.BiochemPharmacol.2016Apr1;105:55-65.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresear