Dihydrotanshinone-I-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEDihydrotanshinoneICat.No.:HY-N0360CASNo.:87205-99-0分⼦式:C₁₈H₁₄O₃分⼦量:278.3作⽤靶点:SARS-CoV作⽤通路:Anti-infection储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:2mg/mL(7.19mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.5932mL17.9662mL35.9324mL5mM0.7186mL3.5932mL7.1865mL10mM---------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DihydrotanshinoneI从丹参中分离到的天然产物，⼴泛⽤于⼼⾎管疾病的研究。DihydrotanshinoneI可抑制MERS-CoV。体外研究Inlipopolysaccharide(LPS)-stimulatedhumanumbilicalveinendothelialcells(HUVECs),DHT(10nM)decreaseslectin-likeox-LDLreceptor-1(LOX-1)andNADPHoxidase4(NOX4)expression,reactiveoxygen1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEspecies(ROS)production,NF-κBnucleartranslocation,ox-LDLendocytosisandmonocytesadhesion[1].DihydrotanshinoneIinducescaspasedependentapoptosisinducedinHCT116cells.DihydrotanshinoneIinducesconcentrationandROSdependentcaspaseactivation.ApoptosisinducedbyDihydrotanshinoneIiscompletelypreventedbyZ-VAD-fmk.ApoptosisinducedbyDihydrotanshinoneIissignificantlyinhibitedbypretreatmentofZ-LEHD-fmkbutonlyispartiallyinhibitedbyZ-IETD-fmk.ApoptosisinducedbyDihydrotanshinoneIissignificantlyincreasedbycaspase-2knockdown[3].体内研究DHT(10and25mg/kg)significantlyattenuatesatheroscleroticplaqueformation,alteresserumlipidprofile,decreasesoxidativestressandshrinksnecroticcoreareasinApoE-/-mice.DHTdramaticallyinhibitstheenhancedexpressionofLOX-1,NOX4,andNF-κBinaorta[1].DihydrotanshinoneI(1,2,4mg/kg)treatmentcanimprovecardiacfunction,reduceinfarctsize,amelioratethevariationsinmyocardialzymogramandhistopathologicaldisorders,decrease20-HETEgeneration,andregulateapoptosis-relatedproteininmyocardialischemia-reperfusionrats[2].PROTOCOLKinaseAssay[3]CellsaretreatedwithvariousconcentrationsofDihydrotanshinoneI(3.13-20µM)for48h.Fortheactivityassay,Ac-DEVD-AMC(1µg/µL),Ac-IETD-AMC(1µg/µL)orAc-LEDH-AMC(1µg/µL)andcelllysateareaddedintoProteaseAssayBufferin96-wellplate.Reactionmixtureswithlysisbufferareusedasnegativecontrols.CellstreatedwithDMSO(0.1%)aretreatedasvehiclecontrol.Thereactionmixturesareincubatedfor1hat37°C.TheAMCliberatedfromthesubstratesismeasuredusingspectrofluorometerofVictor2platereaderwithanexcitationwavelengthof380nmandanemissionwavelengthof430nm.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMaleApoE-/-mice(6-8weeksold)onC57BL/6Jbackgroundandage-matchedwild-typeC57BL/6JcontrolsAdministration[1]housedinSPF-gradeanimalfacilitieswitha12hlight/darkcycle,at23°C(±2°C).Startingfrom6weeks,themicearefedwithaHCD(54.35%rawgrain,20%lard,0.15%cholesterol,15%sucrose,0.5%SodiumCholate,10%yolkpowder)for12weeks.AllApoE-/-micearedoseddailyviaintragastricgavagewith10and25mg/kgDihydrotanshinoneIdissolvedin0.5%CMC-Naoradministered0.5%CMC-Naalone(vehiclecontrol)(n=8pergroup).MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•NucleicAcidsRes.2021Jan8;49(D1):D1113-D1121.•CellMolLifeSci.2020Aug13.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].ZhaoW,etal.DihydrotanshinoneIAttenuatesAtherosclerosisinApoE-DeficientMice:RoleofNOX4/NF-κBMediatedLectin-Like2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEOxidizedLDLReceptor-1(LOX-1)oftheEndothelium.FrontPharmacol.2016Nov8;7:418.eCollection2016.[2].WeiY,etal.ThecardioprotectionofdihydrotanshinoneIagainstmyocardialischemia-reperfusioninjuryviainhibitionofarachidonicacidω-hydroxylase.CanJPhysiolPharmacol.2016Dec;94(12):1267-1275.Epub2016Jun24.[3].WangL,etal.DihydrotanshinoneIinducedapoptosisandautophagythroughcaspasedependentpathwayincoloncancer.Phytomedicine.2015Nov15;22(12):1079-87[4].JiYeunKim,etal.Safe,High-ThroughputScreeningofNaturalCompoundsofMERS-CoVEntryInhibitorsUsingaPseudovirusExpressingMERS-CoVSpikeProtein.IntJAntimicrobAgents.2018N