PARP1-IN-49-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPARP1-IN-49Cat.No.:HY-179406分⼦式:C₁₅H₁₁FN₂O₃分⼦量:286.26作⽤靶点:PARP;DNA/RNASynthesis;ReactiveOxygenSpecies(ROS);Apoptosis作⽤通路:CellCycle/DNADamage;Epigenetics;Immunology/Inflammation;MetabolicEnzyme/Protease;NF-κB;Apoptosis储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性PARP1-IN-49⼀种选择性的PARP1抑制剂，其IC50值为23.56nM，Kd为17.78nM。PARP1-IN-49对PARP1的选择性⾼于PARP2。PARP1-IN-49通过抑制PARP1导致DNA损伤、细胞周期阻滞和凋亡(apoptosis)的诱导。PARP1-IN-49还可增加细胞内活性氧(ROS)的⽔平，并抑制细胞迁移。PARP1-IN-49可⽤于乳腺癌和巢癌的研究[1]。IC50&TargetPARP1PARP1PARP223.56nM(IC50)17.78nM(Kd)285.39nM(IC50)体外研究PARP1-IN-49(compound9a)(0.5-2μM;48h)inhibitsMDA-MB-231cellproliferationandmigration[1].PARP1-IN-49(0.5-2μM;48h)increasesapoptosis-relatedproteinexpressionanddecreasesBcl-2levelsinMDA-MB-231cells[1].PARP1-IN-49(0.5-2μM;48h)inducesDNAdamageanddouble-strandbreaksMDA-MB-231cells[1].PARP1-IN-49(0.5-2μM;48h)increasesapoptosisandcausesSphasecellcyclearrestMDA-MB-231cells[1].PARP1-IN-49(0.5-4μM;48h)inducesapoptosisviaROSgenerationandalteredmitochondrialmembranepotentialMDA-MB-231cells[1].PARP1-IN-49(2μM;48h)enhancesPARP1thermalstability,indicatingdirectinteraction[1].CellProliferationAssay[1]CellLine:MDA-MB-231cellsConcentration:0.5μM,1μM,2μM1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEIncubationTime:48hResult:Inhibitedcellproliferationandmigrationinadose-dependentmanner.WesternBlotAnalysis[1]CellLine:MDA-MB-231cellsConcentration:0.5μM,1μM,2μMIncubationTime:48hResult:Inducedapoptosisinadose-dependentmanner,increasingtheexpressionofapoptosis-relatedproteins,suchasCleavedPARP,Cleavedcaspase3andBax,anddecreasingBcl-2proteinlevels.Immunofluorescence[1]CellLine:MDA-MB-231cellsConcentration:0.5μM,1μM,2μMIncubationTime:48hResult:InducedDNAdamageandtheaccumulationofdouble-strandbreaks,asindicatedbyincreasedγH2AXandcomettaillength.CellCycleAnalysis[1]CellLine:MDA-MB-231cellsConcentration:0.5μM,1μM,2μMIncubationTime:48hResult:TheproportionofcellsintheSphaseincreasedfrom20.09%to47.56%,whiletheproportionofcellsintheG2/Mphasedecreasedfrom19.11%to6.58%.ApoptosisAnalysis[1]CellLine:MDA-MB-231cellsConcentration:0.5μM,1μM,2μMIncubationTime:48hResult:Theproportionofcellsundergoingearlyandlateapoptosisincreasedfrom0.49%to53.8%.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE体内研究PARP1-IN-49(compound9a)(20,40mg/kg;Intraperitoneal;22days)significantlyinhibitstumorgrowthinMDA-MB-231cellssubcutaneouslyinoculatedintoBALB/cmice[1].AnimalModel:MDA-MB-231cells(1×107cells)weresubcutaneouslyinoculatedintotherightflankofBALB/cnudemice(4-week-old)[1]Dosage:20mg/kg,40mg/kgAdministration:Intraperitoneal;22daysResult:Tumorgrowthwassignificantlyinhibited.REFERENCES[1].ZhengY,etal.CoixolderivativesinduceDNAdamagebytargetingPARP1.EurJMedChem.2026;302(Pt2):118307.McePdfHeightCaution:Producthasnotbeenfullyv