MT-125-free-base-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEMT-125freebaseCat.No.:HY-174406ACASNo.:2404652-80-6分⼦式:C₂₂H₁₉N₃O₂分⼦量:357.41作⽤靶点:Myosin;PDGFR;ReactiveOxygenSpecies(ROS);Ferroptosis;Akt;mTOR;ERK作⽤通路:Cytoskeleton;ProteinTyrosineKinase/RTK;

Immunology/Inflammation;MetabolicEnzyme/Protease;NF-κ

B;Apoptosis;PI3K/Akt/mTOR;MAPK/ERKPathway;Stem

Cell/Wnt储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)BIOLOGICALACTIVITY⽣物活性MT-125freebase⼀种特异性和耐受性良好的⾮肌⾁肌球蛋⽩myosinIIA(Ki,NMIIA=2.7μM)和IIB(EC50=1.7μM)抑制剂。MT-125freebase可以穿过⾎脑屏障。MT-125freebase通过增加肿瘤细胞内的活性氧(ROS)⽔平诱导铁死亡ferroptosis和DNA损伤。MT-125freebase可以增强PDGFR信号通路。MT-125freebase可⽤于胶质母细胞瘤的研究[1]。IC50&TargetPDGFRα体外研究MT-125freebase(5μM,8h)significantlyinhibitstheinvasiveabilityofonemurine(MES1861)andthreehuman(187,190,andL1)Glioblastoma(GBM)celllines[1].MT-125freebase(5μM,48h)leadsto12%-25%cellmultinucleationin10humanGBMcells[1].MT-125freebase(0.1-10μM;96h)producesover90%cytotoxicityinvariousmouseandhumanGBMcelllines[1].MT-125increasereactiveoxygenspecies(ROS)andlipidperoxidationlevelsinL1cells[1].MT-125freebase(4μM)caninduceferroptosisandferroptosisinhibitorscanreverseitscytotoxicityinTrp53(-/-)cells[1].MT-125freebase(5μM,48h)significantlyincreasePDGFRαexpressionandactivationofdownstreamsignalingpathwaysinTrp53(-/-)cells[1].MT-125freebase(5μM,48h)regulatestheMAPKsignalingpathwaybyinhibitingNMIIAinTrp53(-/-)cells[1].MT-125freebase(5μM,48h)exhibitssynergisticeffectswithcarcinogenickinaseinhibitorsinTrp53(-/-)cells[1].CellViabilityAssay[1]1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECellLine:murine(TRP53(-/-),Pten(-/-),TRP53/Pten(-/-))andhuman(L1,L0,GBM1A,612,QNS120,QNS166,QNS315)GBMcelllinesConcentration:3.3-7.3μMIncubationTime:96hResult:SignificantlyinhibitedtheGBMcelllines.WesternBlotAnalysis[1]CellLine:Trp53(‒/‒)cellsConcentration:5μMIncubationTime:48hResult:EffectivelyenhancedactivationofPDGFRα,AKT,mTOR,ERK1/2,andSRC.体内研究MT-125freebase(10mg/kg;s.c.;oncedaily;for2weeks)demonstrateslowtoxicityinvivofortheC57BL/6mice[1].MT-125freebase(20mg/kg,s.c.;oncedaily;for7days)doesnotcauseanyadverseeffectsrelatedtomedicationanddoesnotaffectage-relatedweightchangesintheC57BL/6mice[1].MT-125freebase(7.5,15,or30mg/kg;s.c.;oncedaily;for28days)maintaingoodtolerabilityinrepeateddosetoxicologystudiesinthefemalerats[1].MT-125freebase(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]2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEDosage:7.5,15,or30mg/kgAdministration:Subcutaneousinjection(s.c.);oncedailyfor28daysResult:Didnotcauseanyobviousorlastingadversehealtheffects.AnimalModel:C57BL/6micewithTrp53(‒/‒)tumors(8-10weeks;25-35g)[1]Dosage:10mg/kg,co-incubationwithPaxalisib(HY-19962)Administration:Intraperitonealinjection(i.p.);oncedailyfor4weeksResult:MarkedlyreducedtumorsizetoanisolatednestofHA-positivecellsandprolongedsurvivalrate.REFERENCES[1].KenchappaRS,etal.MT-125inhibitsnon-musclemyosinIIAandIIBandprolongssurvivalinglioblastoma.Cell.2025Jun3:S0092-8674(25)00569-0.Mce