GSTP1-M2-IN-1-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEGSTP1/M2-IN-1Cat.No.:HY-179217分⼦式:C₁₆H₁₂N₆O₈S₂分⼦量:480.43作⽤靶点:JNK;Apoptosis作⽤通路:MAPK/ERKPathway;Apoptosis储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性GSTP1/M2-IN-1⼀种GSTP1/GSTM2双重抑制剂(IC50=1.56μM/0.09μM)。GSTP1/M2-IN-1可激活JNK通路并诱导细胞凋亡(apoptosis)。GSTP1/M2-IN-1可⽤于乳腺癌和胰腺癌的研究[1]。体外研究GSTP1/M2-IN-1(Compound5b)exhibitspotentanticanceractivity,particularlyeffectiveagainstGSTM2-overexpressingcelllines(suchas67NRand4T1):MDA-MB-231cells(IC50=1.11μM),MiaPaCa-2cells(IC50=1.81μM),4T1cells(IC50=1.90μM),67NRcells(IC50=1.08μM)[1].GSTP1/M2-IN-1co-treatmentwiththeJNKinhibitorSP600125(HY-12041)markedlyincreasesIC50values,confirmingthatJNKactivationisessentialfortheircytotoxicityinMDA-MB-231(2.71to15.42μM)andMiaPaCa-2(1.78to15.23μM)celllines[1].GSTP1/M2-IN-1(24-72h)significantlyincreasesJNK,p-c-Jun,cleavedcaspase-3,andPARPcleavageinMDA-MB-231andMiaPaCa-2celllines[1].GSTP1/M2-IN-1anditscombinationwithGemcitabine(HY-17026)activateapoptoticpathways,asevidencedbyincreasedcleavageofPARP,elevatedP-JNK,andP-c-JUNinMIAPaCa-2cells[1].体内研究GSTP1/M2-IN-1(Compound5b)(5mg/kg,oncedailyfor14days)incombinationwithGemcitabineexhibitspotentsynergisticantitumoractivityintheMiaPaCa-2pancreaticcancerxenograftmicemodelanddownregulatestheproteinexpressionlevelsofGSTP1andGSTM2intumortissues[1].AnimalModel:500,000MiaPaCa-2humanpancreaticcancercellsweremixedwithMatrigelina1:1ratioandinjectedintotheflankofNSGmice[1].Dosage:5mg/kg;Gemcitabine:100mg/kgAdministration:I.p.,oncedailyfor14days1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEResult:Bothtumorvolumeandmassweresignificantlyreduced.ProteinexpressionlevelsofGSTP1andGSTM2intumortissueweredownregulated.REFERENCES[1].GreeshmaP,etal.TargetingtumorantioxidantpathwayswithnovelGSTP1/M2inhibitorsforcancertreatment,bioRxiv.October21,2025.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseon