AMPK-mTOR-modulator-1-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAMPK/mTORmodulator-1Cat.No.:HY-181059CASNo.:1190602-80-2分⼦式:C₃₁H₅₆O₄分⼦量:492.77作⽤靶点:DrugDerivative;mTOR;AMPK作⽤通路:Others;PI3K/Akt/mTOR;Epigenetics储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性AMPK/mTORmodulator-1，⼈参皂苷衍⽣物，⼀种具有⼝服活性的mTOR抑制剂和AMPK激活剂。AMPK/mTORmodulator-1激活AMPK信号通路的Kd值为4.759μM。AMPK/mTORmodulator-1促进M1型肿瘤相关巨噬细胞极化，同时抑制M2型极化。AMPK/mTORmodulator-1可增强糖酵解。AMPK/mTORmodulator-1显著抑制肿瘤进展并表现出抗炎活性。AMPK/mTORmodulator-1可⽤于结直肠癌研究[1]。IC50&TargetAMPK4.759μM(Kd)体外研究AMPK/mTORmodulator-1(CompoundAD-1)directlybindstorecombinantAMPKproteinwithaKdof4.759×10−6M[1].AMPK/mTORmodulator-1(2.5-10μM;24h)promotesM1-likepolarizationandsuppressesM2-likepolarizationinRAW264.7-derivedTAMsinadose-dependentmanner[1].AMPK/mTORmodulator-1(2.5-10μM;24h)activatesAMPKandinhibitsmTORsignalinginRAW264.7-derivedTAMsinadose-dependentmanner[1].AMPK/mTORmodulator-1(2.5-10μM;24h)enhancesglycolyticactivityinRAW264.7-derivedTAMsinadose-dependentmanner[1].RT-PCR[1]CellLine:RAW264.7-derivedTAMsinTCSofmousecoloncancercells(CT26)Concentration:2.5,5,and10μMIncubationTime:24h1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEResult:DownregulatedM2-associatedmarkers(Arg-1,IL-10,andTGF-β)andupregulatedM1-associatedmarkers(iNOS,TNF-α,andIL-1β).WesternBlotAnalysis[1]CellLine:RAW264.7-derivedTAMsinTCSofmousecoloncancercells(CT26)Concentration:2.5,5,and10μMIncubationTime:24hResult:IncreasedproteinlevelsofiNOSandreducedArg-1levels.IncreasedP-AMPKAMPKratioandreducedp-mTOR/mTORratio.Upregulatedtheexpressionofkeyglycolyticen-zymes,includingGLUT1,LDHA,PKM2,andHK2.ELISAAssay[1]CellLine:RAW264.7-derivedTAMsinTCSofmousecoloncancercells(CT26)Concentration:2.5,5,and10μMIncubationTime:24hResult:ReducedTGF-β,IL-10levlesandincreasedIL-1β,TNF-αlevels.体内研究AMPK/mTORmodulator-1(CompoundAD-1)(10mg/kg;i.g.;daily;64days)inhibitsthedevelopmentandprogressionofcolitis-associatedtumorsbypromotingM1-likepolarizationandsuppressingM2-likepolarizationinAOM(HY-111375)/DSS(HY-116282C)-inducedCACmice[1].AMPK/mTORmodulator-1(10mg/kg;oralgavage;daily;15days)suppressestumorgrowthandreprogramsTAMpolarizationinHT-29cellsxenograftmice[1].AnimalModel:CACmiceinducedbyAOM/DSS(male,BALB/c，6–8weeksold,20–22g)[1]Dosage:10mg/kgAdministration:oralgavage;daily;64daysResult:Restoredcolonlengthandreducedtumornumber.Alleviatedcryptdestruction,epithelialdamage,andinflammatoryinfiltration.DecreasedKi-67-positiveproliferatingcellsandreducedproportionofF4/80+CD206+(M2-like)TAMs.IncreasedlevelsofTNF-αandIL-1βanddecreasedIL-10levels.IncreasediNOSproteinlevelsanddecreasedArg-1proteinlevels.IncreasedinfiltrationofF4/80+CD86+(M1-like)TAMsanddecreasedF4/80+CD206+TAMsincolonictissues.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAnimalModel:CRCmicewithHT-29cellsxenograft(female,BALB/cnude,6–8weeksold,20–22g)[1]Dosage:10mg/kgAdministration:oralgavage;daily;15daysResult:Reducedtumorvolumeandweight,inflammatorycellinfiltrationandimprovedtissuearchitectureintumorsections.Decreasedtumorcellproliferation(lowerKi-67expression).ElevatediNOSexpressionanddecreasedArg-1expression.IncreasedabundanceofF4/80+CD86+(M1-like)TAMs;reducednumberofF4/80+CD206+(M2-like)TAMsintumortissue.REFERENCES[1].FuY,etal.GinsenosidederivativeAD-1suppressescolitis-associatedcolorectalcancerprogressionbyreprogrammingtumor-associatedmacrophagepolarizationviatheAMPK/mTOR-glycolysispathway.BioorgChem.2026;169:109458.McePdfHeightCa