Keap1-Nrf2-ARE-activator-2-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEKeap1/Nrf2/AREactivator2Cat.No.:HY-180155CASNo.:3105470-83-2分⼦式:C₁₅H₉BrO₄分⼦量:333.13作⽤靶点:Keap1-Nrf2;Cholinesterase(ChE);InterleukinRelated;TNF

Receptor;ReactiveOxygenSpecies(ROS);HemeOxygenase

(HO);QuinoneReductase作⽤通路:NF-κB;NeuronalSignaling;Immunology/Inflammation;Apoptosis;MetabolicEnzyme/Protease储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Keap1/Nrf2/AREactivator2⼀种Keap1/Nrf2/ARE通路激活剂，以⾮竞争性⽅式抑制AChE，IC50值为14.79μM，Ki值为1.35μM。Keap1/Nrf2/AREactivator2可促进Nrf2核转位，从⽽上调抗氧化因表达，增强细胞对氧化应激的防御能⼒。Keap1/Nrf2/AREactivator2对PC12细胞中由H2O2和Scopolamine(SCA)(HY-N0296)诱导的损伤均表现出显著的神经保护作⽤。在斑马鱼模型中，Keap1/Nrf2/AREactivator2可改SCA诱导的认知功能障碍相关的记忆障碍和神经炎症。Keap1/Nrf2/AREactivator2可⽤于阿尔茨海默病的研究[1]。IC50&TargetIL-6IL-1βAChEAChE14.79μM(IC50)1.35μM(Ki)HO-1NQO1体外研究Keap1/Nrf2/AREactivator2(compound32)(5-100µM,24h)demonstratesnosignificanttoxiceffectonPC12cellsupto20μM[1].Keap1/Nrf2/AREactivator2(5-20µM,12-24h)demonstratessignificantcytoprotectionagainstH2O2-andSCA-inducedPC12cellinjury,asevidencedbyimprovedcellviability,reducedLDHandROSrelease,andsuppressionofapoptosis[1].Keap1/Nrf2/AREactivator2(20µM,2-8h)inducesNrf2accumulationandnucleartranslocationinPC12cellsinatime-dependentmanner[1].Keap1/Nrf2/AREactivator2(20µM,6-24h)upregulatesmultipleantioxidantsystemsinPC12cells,suchasHO-1,NQO1,Trx,TrxR,andGCLCmRNA[1].1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECellViabilityAssay[1]CellLine:PC12,PC12-siNrf2andPC12-siNTcellsConcentration:5,10,20,50,100µMIncubationTime:24hResult:DisplayednosignificanttoxiceffectonPC12cellsupto20μMfollowing24hexposure.RescuedPC12cellsfromtheH2O2-inducedoxidativedamages.DemonstratedrobustprotectionagainstSCA-inducedcytotoxicity.SignificantlyprotectedthecontrolcellsfromtheH2O2-inducedinjury,whileshowingnoprotectiveeffectintheNrf2-deficientcells.ShowedaprotectiveeffectinPC12-siNrf2cells.WesternBlotAnalysis[1]CellLine:PC12cellsConcentration:5,10,20µMIncubationTime:2,4,8hResult:SignificantlyactivatedtheNrf2/AREsignalingpathway.ShowedamarkedincreaseintotalandnuclearNrf2levelsasearlyas2haftertreatment.RealTimeqPCR[1]CellLine:PC12cellsConcentration:20µMIncubationTime:6,12,24hResult:SignificantlyupregulatedHO-1,NQO1,Trx,TrxR,andGCLCmRNAafter6h.体内研究Keap1/Nrf2/AREactivator2(5μM,48h)amelioratesSCA-inducedcognitiveimpairmentinzebrafishbyreducingneuroinflammation,restoringcholinergicfunction,andactivatingtheNrf2/AREantioxidantpathway[1].AnimalModel:AdultAB-strainzebrafish(6-monthsold)challengedwithSCA(200μMinwater)[1]Dosage:5μMAdministration:48hResult:Significantlyimprovedspatialmemoryperformanceinzebrafishchallengedwith2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEscopolamine,asevidencedbyincreasedpreferenceforthetargetarmintheT-mazetestandenhancedorientation.Restoredswimmingvelocities,suggestingimprovedmotorfunction.ReducedneuroinflammationbyattenuatingtheexpressionofIL-1β,IL-6,TNF-αandupregulatedtheexpressionofantioxidantgenes(Nrf2,Gpx4,Trx).RestoredAChEactivitytonear-physiologicallevels.REFERENCES[1].SongZL,etal.EmergingofanewneuroprotectiveisoflavonoidwithpotentKeap1/Nrf2/AREpathwayactivationandAChEinhibition.BioorgChem.PublishedonlineDecember4,2025.McePdfHeightCaution:Produc