MS023-trihydrochloride-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEMS023trihydrochlorideCat.No.:HY-19615ACASNo.:2108631-19-0分⼦式:C₁₇H₂₈Cl₃N₃O分⼦量:396.78作⽤靶点:HistoneMethyltransferase作⽤通路:Epigenetics储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性MS023trihydrochloride⼀种有效选择性的，具有细胞活性的⼈I型蛋⽩精氨酸甲转移酶(PRMTs)抑制剂，对PRMT1，PRMT3，PRMT4，PRMT6和PRMT8的IC50分别为30，119，83，4和5nM[1]。体外研究MS023(1-1000nM;48hours)inhibitsPRMT1methyltransferaseactivityinMCF7cells[1].MS023(1-1000nM;20hours)inhibitsPRMT6methyltransferaseactivityinHEK293cells[1].WesternBlotAnalysis[1]CellLine:MCF7andHEK293cellsConcentration:1.4,4,12,37,111,333,and1000nMIncubationTime:48hoursforMCF7cells;20hoursforHEK293cellsResult:Treatmentpotentlyandconcentration-dependentlyreducedcellularlevelsofH4R3me2a(IC50=9nM).Treatmentconcentration-dependentlyreducedtheH3R2me2amark(IC50=56nM).体内研究AdministrationofMS023(160mg/kg,i.p)incombinationwithPKC412(100mg/kg,i.g.)blocksMLL-racutelymphoblasticleukemia(ALL)propagationbyinhibitingmaintenanceoffunctionalMLL-rALL-initiatingcells[2].AnimalModel:NOD-scidIL2Rgnull(NSG)micebearingprimaryMLL-rALLcells[2]1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEDosage:160mg/kgAdministration:Intraperitonealinjection;PKC412(100mg/kg,i.g.),MS023(160mg/kg,i.p),oracombinationfor4weeksResult:Combinatorialtreatmentextendedsurvivalofleukemicmicerelativetosingletreatments.户使⽤本产品发表的科研⽂献•ActaPharmSinB.22October2021.•CellRep.2021Sep21;36(12):109731.•ActaPharmacolSin.2021Apr13.•Oncogenesis.2022Aug8;11(1):45.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].EramMS,etal.APotent,Selective,andCell-ActiveInhibitorofHumanTypeIProteinArginineMethyltransferases.ACSChemBiol.2016Mar18;11(3):772-81.[2].YinghuiZhu,etal.TargetingPRMT1-mediatedFLT3methylationdisruptsmaintenanceofMLL-rearrangedacutelymphoblasticleukemia.Blood.2019Oct10;134(15):1257-1268.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly