JPC0661-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEJPC0661Cat.No.:HY-W471288CASNo.:30479-81-3分⼦式:C₁₅H₁₃N₃O₅S分⼦量:347.35作⽤靶点:AP-1作⽤通路:Immunology/Inflammation储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性JPC0661⼀种直接且变构的ΔFOSB抑制剂。JPC0661以微尔级IC50值(9-52μM)抑制ΔFOSB/JUND和ΔFOSB与DNA的结合,在体外可直接抑制ΔFOSB介导的转录，其IC50值为0.82μM。JPC0661在体内能显著降低ΔFOSB在因组AP1位点的占据。JPC0661通过结合于ΔFOSBDNA结合裂隙外的⼀个全新沟槽，破坏ΔFOSB/JUND-DNA复合物的形成。JPC0661可⽤于阿尔茨海默病的研究[1]。IC50&TargetFosB体外研究JPC0661(0-100μM)regulateΔFOSB-drivengeneexpressionwithIC50of0.82μMandaccumulatesΔFOSBproteininHEK293cells[1].JPC0661(0-100μM,24or72h)hasgoodtoleranceinneuronalprogenitorcells,AP1-lucHEK293cellsanddNeuro2Acells(NPC)[1].CellViabilityAssay[1]CellLine:Neuronalprogenitorcells(NPC)Concentration:0.16,0.31,0.63,1.25,2.5,5.00,10.00and20μM,IncubationTime:24,72hResult:Observednodiscernabledecreaseafter24handonlyminimallossesafter72h.体内研究JPC0661(50μM,16.7ng/h,intra-hippocampalinfusion,for3days)causesarobust,broadreductioninΔFOSBbindingacrossmostthistranscriptionfactor’snormalgenomiclocationsinheterozygoustransgenic1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEmaleandfemalemiceexpressinghumanamyloidprecursorprotein(APP)carryingSwedish(K670N,M671L)andIndiana(V717F)mutations[1].AnimalModel:Heterozygoustransgenicmaleandfemalemice(2-3months)[1]Dosage:50μMin0.2%DMSO/0.9%salinewith0.96μL/hAdministration:intra-hippocampalinfusionfor3daysResult:Exhibitedanapproximately60%reductionintotalbindingsites.Decreasedaveragepeakwidth.DirectlydisruptedΔFOSB–DNAinteractions.Causedamodestdeclineinpromoterproximalpeaks(≤1kb)andarelativeenrichmentindistalintergenicpeaks.REFERENCES[1].McNemeS,etal.DiscoveryofSmallMoleculesandaDruggableGrooveThatRegulateDNABindingandReleaseoftheAP-1TranscriptionFactorΔFOSB.JBiolChem.2025Dec22:111080.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.