Manzamine-A-Keramamine-A-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEManzamineACat.No.:HY-117025CASNo.:104196-68-1Synonyms:KeramamineA分⼦式:C₃₆H₄₄N₄O分⼦量:548.76作⽤靶点:GSK-3;CDK;Parasite;ProtonPump;HSV;Autophagy作⽤通路:PI3K/Akt/mTOR;StemCell/Wnt;CellCycle/DNADamage;Anti-infection;MembraneTransporter/IonChannel;Autophagy储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.溶解性数据体外实验DMSO:10mg/mL(18.22mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.8223mL9.1115mL18.2229mL5mM0.3645mL1.8223mL3.6446mL10mM0.1822mL0.9111mL1.8223mLBIOLOGICALACTIVITY⽣物活性ManzamineA⼀种⼝服活性β-carboline⽣物碱，抑制GSK-3β和CDK-5的IC50值为10.2μM和1.5μM。ManzamineA靶向胰腺癌细胞的vacuolarATPases并抑制⾃噬(autophagy)。ManzamineA具有抗疟和抗癌活性。ManzamineA对HSV-1具有较强的活性。IC50&TargetPlasmodiumGSK-3βCDK5vacuolarATPases10.2μM(IC50)1.5μM(IC50)MalariaHSV-11/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE体外研究ManzamineA(5-50µM,18h)decreasestauphosphorylation,measuredwithELISA[1].ManzamineA(10µM)inhibitsyeastS.cerevisiaegrowthby30%[2].ManzamineAdisplaysafewenlargedvacuolesinyeast[2].ManzamineA(2.5-10µM,24h)increasesacidityinpancreaticcancercellsandnon-malignantVerocells[2].ManzamineA(1µM,24h)inhibitsHSV-1infectioninSIRCcells[4].ManzamineAshowsantimalarialactivitywithanIC50of8.0nM(D6clone)and11nM(W2clone)[5].CellViabilityAssay[4]CellLine:SIRCcellConcentration:0.1,0.5,1,2,3,5,and10µMIncubationTime:72hResult:InhibitedSIRCcellviabilitywithanIC50of5.6µM.体内研究ManzamineA(50and100mol/kg,p.o.ori.p.)inhibitsthegrowthoftherodentmalariaparasitePlasmodiumbergheiininfectedmice[6].ManzamineA(8mg/kg,i.p.,dailyfor8consecutivedays)prolongsthesurvivalofSWmiceto20days[7].AnimalModel:Plasmodiumbergheiininfectedmice[6]Dosage:50or100mol/kgAdministration:Intraperitonealinjection(i.p.)ororaladministration(p.o.)Result:InhibitedthegrowthoftherodentmalariaparasitePlasmodiumberghei.Prolongedthesurvivalofhighlyparasitaemicmice.户使⽤本产品发表的科研⽂献•MarDrugs.2023,21(3),151.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].HamannM,etal.Glycogensynthasekinase-3(GSK-3)inhibitoryactivityandstructure-activityrelationship(SAR)studiesofthemanzaminealkaloids.PotentialforAlzheimer'sdisease.JNatProd.2007;70(9):1397-1405.[2].KallifatidisG,etal.ThemarinenaturalproductmanzamineAtargetsvacuolarATPasesandinhibitsautophagyinpancreaticcancercells[publishedcorrectionappearsinMarDrugs.2014;12(4):2305-7].MarDrugs.2013;11(9):3500-3516.Published2013Sep17.[3].WinklerJD,etal.AntimalarialactivityofanewfamilyofanaloguesofmanzamineA.OrgLett.2006;8(12):2591-2594.[4].PalemJR,etal.ManzamineAasanovelinhibitorofherpessimplexvirustype-1replicationinculturedcornealcells.PlantaMed.2011;77(1):46-51.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[5].WahbaAE,etal.Structure-activityrelationshipstudiesofmanzamineA:amidationofpositions6and8ofthebeta-carbolinemoiety.BioorgMedChem.2009Nov15;17(22):7775-82.[6].DoniaM,etal.Marinenaturalproductsandtheirpotentialapplicationsasanti-infectiveagents.LancetInfectDis.2003Jun;3(6):338-48.[7].ElSayedKA,etal.Newmanzaminealkaloidswithpotentactivityagainstinfectiousdiseases.JAmChemSoc.2001Mar7;123(9):1804-8.McePdfHeightCaution:Productha