MS023-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEMS023Cat.No.:HY-19615CASNo.:1831110-54-3分⼦式:C₁₇H₂₅N₃O分⼦量:287.4作⽤靶点:HistoneMethyltransferase作⽤通路:Epigenetics储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验H2O:66.67mg/mL(231.98mM;Needultrasonic)DMSO:≥30mg/mL(104.38mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM3.4795mL17.3974mL34.7947mL5mM0.6959mL3.4795mL6.9589mL10mM0.3479mL1.7397mL3.4795mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。BIOLOGICALACTIVITY⽣物活性MS023⼀种有效选择性的，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]。1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEIC50&TargetIC50:30nM(PRMT1),119nM(PRMT3),83nM(PRMT4),4nM(PRMT6),5nM(PRMT8)[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=9±0.2nM).Treatmentconcentration-dependentlyreducedtheH3R2me2amark(IC50=56±7nM).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]Dosage: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):1257-1268.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplica