PQA-18-生命科学试剂-MCE-3779

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPQA-18Cat.No.:HY-171034CASNo.:1604678-82-1分⼦式:C₂₅H₃₁NO₄分⼦量:409.52作⽤靶点:InterleukinRelated;TNFReceptor;PAK作⽤通路:Immunology/Inflammation;Apoptosis;CellCycle/DNADamage;Cytoskeleton储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性PQA-18⼀种独特的PAK2抑制剂(IC50:10nM)。PQA-18具有免疫抑制活性，可抑制IL2、IL4、IL6和TNFα产⽣。PQA-18可抑制⼩⿏中调节性T细胞亚群的数量和针对T细胞依赖性抗原的免疫球蛋⽩(Ig)的产⽣，并可减轻⼩⿏的⽪炎症状[1]。IC50&TargetPAK2IL-6IL4IL-210nM(IC50)体外研究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—您⾝边的抑制剂⼤师www.MedChemEResult:SuppressedIL2mRNAlevelinConA-stimulatedJurkatcells.Affected-50%ofIL2transcriptsatahighdose(10μM).体内研究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