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Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEMAPK-IN-5Cat.No.:HY-175175CASNo.:2579683-39-7分子式:C₃₀H₂₉F₃N₆O₄分子量:594.58作用靶点:p38MAPK;Bcl-2Family;Caspase;ReactiveOxygenSpecies(ROS);PARP;Apoptosis作用通路:MAPK/ERKPathway;Apoptosis;Immunology/Inflammation;MetabolicEnzyme/Protease;NF-κB;CellCycle/DNADamage;Epigenetics储存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性MAPK-IN-5是一种强效的MAPK抑制剂。MAPK-IN-5对Hela细胞的IC50值为1.35μM。MAPK-IN-5可通过MAPK途径诱导ROS介导的DNA损伤和线粒体细胞凋亡(apoptosis)。MAPK-IN-5显著抑制HeLa细胞集落形成,减少活细胞数量,抑制细胞迁移,阻滞周期于G2/M期。MAPK-IN-5可用于宫颈癌的研究[1]。IC50&Targetp38Caspase-3Caspase-9Bcl-2PARP-1体外研究MAPK-IN-5(Compound3h)(5-10μM,48h)significantlyinhibitsthecolonyformationofHeLacellsandincreasesthenumberofdeadcells[1].MAPK-IN-5(5-10μM,0-48h)hasapronouncedinhibitoryeffectonthemigrationofHeLacells[1].MAPK-IN-5(5-10μM,24h)inducesG2/MphasearrestinHeLacells[1].MAPK-IN-5(5-10μM,48h)inducesapoptosisinHeLacells,andtheactivationofthemitochondrialapoptosispathwayisinvolved[1].MAPK-IN-5(5-10μM,48h)promotesROSgeneration,triggersDNAdamageandmodulatestheMAPKsignalingpathwayinHeLacells[1].Immunofluorescence[1]CellLine:HeLacells1/3 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEConcentration:5and10μMIncubationTime:48hResult:Thenumberoflivecellsgraduallydecreased,whilethenumberofdeadcellsincreased.Dose-dependentlyincreasedtheintracellularROSlevel.Increasedthefluorescenceintensityofγ-H2AXinthenucleiofHeLacells.CellMigrationAssay[1]CellLine:HeLacellsConcentration:5and10μMIncubationTime:0,24,48hResult:ThemigrationrateofHeLacellswasreducedto20.75%at10μM.CellCycleAnalysis[1]CellLine:HeLacellsConcentration:5and10μMIncubationTime:24hResult:TheproportionofcellsintheG1phasegraduallydecreased,whiletheproportionofcellsintheG2/Mphasesignificantlyaccumulated.ApoptosisAnalysis[1]CellLine:HeLacellsConcentration:5and10μMIncubationTime:48hResult:ThetotalapoptosisrateofHeLacellswas37.63%at10μM.Cellshrinkage,intensifiednuclearstaining,andevenapoptoticfeaturessuchasnuclearcondensationandfragmentationwereobserved.WesternBlotAnalysis[1]CellLine:HeLacellsConcentration:5and10μMIncubationTime:48h2/3 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEResult:DecreasedthelevelsofBcl-2,Caspase-3,Caspase-9,andPARP-1.IncreasedthelevelofBaxandCleavedPARP-1.Dose-dependentlyinhibitedthelevelsofphosphorylatedERK1/2(p-ERK1/2)andphosphorylatedJNK(p-JNK),whileupregulatingthephosphorylationofp38.HadnoeffectonthetotalproteinlevelsofERK1/2,JNK,andp38.REFERENCESWangL,etal.Design,synthesisandanti-canceractivityofnovel1,2,3-triazolehybridsoferlotinibagainstcervicalcancerviaMAPKsignalingpathway.SciRep.2025Jul9;15(1):24582.McePdfHeightCaution:Producthasnotbeenfullyvalidatedfo

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