PRMT1-IN-3-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEPRMT1-IN-3Cat.No.:HY-175821CASNo.:892570-48-8分子式:C₁₈H₂₃FN₂O分子量:302.39作用靶点:HistoneMethyltransferase;Apoptosis作用通路:Epigenetics;Apoptosis储存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性PRMT1-IN-3是一种强效的蛋白精氨酸甲基转移酶1(PRMT1)抑制剂，其IC50为4.11μM。PRMT1-IN-3能够抑制PRMT6和PRMT8，其IC50值分别为23.3和30.1μM。PRMT1-IN-3可抑制三阴性乳腺癌(TNBC)细胞中的不对称二甲基精氨酸(ADMA)水平和组蛋白H4R3me2a修饰。PRMT1-IN-3可诱导MDA-MB-231细胞周期停滞、凋亡(apoptosis)，并抑制细胞的迁移和集落形成。PRMT1-IN-3可作为Paclitaxel(HY-B0015)的化疗增敏剂。PRMT1-IN-3可用于TNBC的研究[1]。IC50&TargetPRMT1PRMT3PRMT4PRMT64.11μM(IC50)>100μM(IC50)>100μM(IC50)23.3μM(IC50)PRMT5PRMT8PRMT7>100μM(IC50)30.1μM(IC50)>100μM(IC50)体外研究PRMT1-IN-3(CompoundYH-4)(10μM,37-65°C)significantlyenhancesthethermalstabilityofPRMT1(ΔTm=+5.2°C)andhasnosignificanteffectonotherPRMTsubtypes[1].PRMT1-IN-3(0.01-100μM,48h)inhibitsMDA-MB-231,HCT116,HeLa,andA549cellsgrowthwithIC50sof6.38μM,15.29μM,12.97μM,and9.187μM,respectively[1].PRMT1-IN-3(1.25-10μM,48h)dose-dependentlyinhibitsADMAlevelsandH4R3me2amodificationinMDA-MB-231cells[1].PRMT1-IN-3(0-20μM,72h)(resistanceratio:9.0)showssynergisticeffectwithPaclitaxel(PTX)(resistanceratio:92.7)inMDA-MB-231cellsandMDA-MB-231/Taxolcells[1].PRMT1-IN-3(0-40μM,0-48h)inducesG0/G1phasearrestandcellapoptosis,andinhibitscellmigrationinMDA-MB-231cells[1].PRMT1-IN-3(0-20μM,10days)almostcompletelyinhibitsMDA-MB-231cellscolonyformationat20μM[1].1/3 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEApoptosisAnalysis[1]CellLine:MDA-MB-231cellsConcentration:0,5,20and40μMIncubationTime:48hResult:Resultedinanincreaseinearlyapoptosisfrom2.34%to34.3%from2.5μMto40μM.CellCycleAnalysis[1]CellLine:MDA-MB-231cellsConcentration:0,2.5,5,10,20μMIncubationTime:48hResult:ObservedthattheproportionofcellsintheG0/G1phaseincreasedinadose-dependentmannerfrom41.8%to60.9%,whiletheproportionsofcellsintheSphaseandG2/Mphasedecreasedinadose-dependentmannerfrom33.2%to23.6%andfrom24.9%to15.2%,respectively.CellMigrationAssay[1]CellLine:MDA-MB-231cellsConcentration:1.25,2.5,5,10and20μMIncubationTime:0,12,36,and48hResult:Decreasedthehealingrateto18.52%after48hat20μM.体内研究PRMT1-IN-3(CompoundYH-4)(30mg/kg,i.p.,foroneweek,thendiscontinueforthreedays,foratotalof21days)isachemotherapeuticsensitizerforPTX,enhancingitstherapeuticefficacywhilesignificantlyreducingtherequireddosageandmitigatingittoxicsideeffectsinTNBCmicemodel[1].AnimalModel:MDA-MB-23-YFP-Luccellsinducedxenograftmodelestablishedinfemalenudemice4-5weeksoldweighing16-18g[1]Dosage:30mg/kgwithorwithoutPTXAdministration:Intraperitonealinjection(i.p.),foroneweek,thendiscontinueforthreedays,foratotalof21daysResult:Demonstratedsignificantinhibitoryeffectsontumorvolume,withthecombinationofPTXshowingamarkedlysuperiorantitumorefficacycomparedtothemonotherapies.2/3 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEREFERENCESSuY,etal.Discoveryofproteinargininemethyltransferase1inhibitorbystructure-basedpharmacophoremodeling,virtualscreening,moleculardynamicssimulations,andtheenhancementofpaclitaxel'santitumoractivity.EurJMedChem.2025Dec5;299:118066.McePdfHeightCaution:Producthas