Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemEMT-125Cat.No.:HY-174406分子式:C??H??ClN?O?分子量:393.87作用靶點:Myosin;PDGFR;ReactiveOxygenSpecies(ROS);Ferroptosis;Akt;mTOR;ERK作用通路:Cytoskeleton;ProteinTyrosineKinase/RTK;Immunology/Inflammation;MetabolicEnzyme/Protease;NF-κB;Apoptosis;PI3K/Akt/mTOR;MAPK/ERKPathway;StemCell/Wnt儲存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性 MT-125是一種特異性和耐受性良好的非肌肉肌球蛋白myosinIIA(Ki,NMIIA=2.7μM)和IIB(EC50=1.7μ抑制劑。MT-125可以穿過血腦屏障。MT-125通過增加腫瘤細(xì)胞內(nèi)的活性氧(ROS)水平誘導(dǎo)鐵死亡ferroptosis和DNA損傷。MT-125可以增強PDGFR信號通路。MT-125可用于膠質(zhì)母細(xì)胞瘤的研究[1]。IC50&TargetPDGFRα體外研究MT-125(5μM,8h)significantlyinhibitstheinvasiveabilityofonemurine(MES1861)andthreehuman(187,190,andL1)Glioblastoma(GBM)celllines[1].MT-125(5μM,48h)leadsto12%-25%cellmultinucleationin10humanGBMcells[1].MT-125(0.1-10μM;96h)producesover90%cytotoxicityinvariousmouseandhumanGBMcelllines[1].MT-125increasereactiveoxygenspecies(ROS)andlipidperoxidationlevelsinL1cells[1].MT-125(4μM)caninduceferroptosisandferroptosisinhibitorscanreverseitscytotoxicityinTrp53(?/?)cells[1].MT-125(5μM,48h)significantlyincreasePDGFRαexpressionandactivationofdownstreamsignalingpathwaysinTrp53(?/?)cells[1].MT-125(5μM,48h)regulatestheMAPKsignalingpathwaybyinhibitingNMIIAinTrp53(?/?)cells[1].MT-125(5μM,48h)exhibitssynergisticeffectswithcarcinogenickinaseinhibitorsinTrp53(?/?)cells[1].CellViabilityAssay[1]CellLine:murine(TRP53(-/-),Pten(-/-),TRP53/Pten(-/-))andhuman(L1,L0,GBM1A,612,QNS120,QNS166,QNS315)GBMcelllinesConcentration:3.3-7.3μM1/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEIncubationTime:96hResult:SignificantlyinhibitedtheGBMcelllines.WesternBlotAnalysis[1]CellLine:Trp53(?/?)cellsConcentration:5μMIncubationTime:48hResult:EffectivelyenhancedactivationofPDGFRα,AKT,mTOR,ERK1/2,andSRC.體內(nèi)研究MT-125(10mg/kg;s.c.;oncedaily;for2weeks)demonstrateslowtoxicityinvivofortheC57BL/6mice[1].MT-125(20mg/kg,s.c.;oncedaily;for7days)doesnotcauseanyadverseeffectsrelatedtomedicationanddoesnotaffectage-relatedweightchangesintheC57BL/6mice[1].MT-125(7.5,15,or30mg/kg;s.c.;oncedaily;for28days)maintaingoodtolerabilityinrepeateddosetoxicologystudiesinthefemalerats[1].MT-125(10mg/kg;i.p.;oncedaily;for4weeks)synergizeswithoncogenickinaseinhibitorsandcansignificantlyinhibitthegrowthoftumorcellsintheC57BL/6micewithTrp53(?/?)tumors[1].AnimalModel:C57BL/6mice(8-10weeks;25-35g)[1]Dosage:10mg/kgAdministration:Subcutaneousinjection(s.c.);oncedailyfor2weeksResult:Hadgoodtoleranceandtheweightandhematologicalindicatorsofmicewerewithinnormalrange.AnimalModel:C57BL/6mice(8-10weeks;25-35g)[1]Dosage:20mg/kgAdministration:Subcutaneousinjection(s.c.);oncedailyfor7daysResult:Maintainednormalbodyweightandhematologicalparameterswithinthenormalrangeinmice.AnimalModel:femalerats(8-10weeks;25-35g)[1]Dosage:7.5,15,or30mg/kgAdministration:Subcutaneousinjection(s.c.);oncedailyfor28daysResult:Didnotcauseanyobviousorlastingadversehealtheffects.2/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEAnimalModel:C57BL/6micewithTrp53(?/?)tumors(8-10weeks;25-35g)[1]Dosage:10mg/kg,co-incubationwithPaxalisib(HY-19962)Administration:Intraperitonealinjection(i.p.);oncedailyfor4weeksResult:MarkedlyreducedtumorsizetoanisolatednestofHA-positivecellsandprolongedsurvivalrate.REFERENCESKenchappaRS,etal.MT-125inhibitsnon-musclemyosinIIAandIIBandprolongssurvivalinglioblastoma.Cell.2025Jun3:S0092-8674(25)00569-0.McePdfHeightCauti