Suramin-sodium-salt-Suramin-hexasodium-salt-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemESuraminsodiumsaltCat.No.:HY-B0879ACASNo.:129-46-4Synonyms:Suraminhexasodiumsalt分⼦式:C₅₁H₃₄N₆Na₆O₂₃S₆分⼦量:1429.17作⽤靶点:Phosphatase;Sirtuin;ReverseTranscriptase;Topoisomerase;SARS-CoV;Parasite;Apoptosis作⽤通路:MetabolicEnzyme/Protease;CellCycle/DNADamage;Epigenetics;Anti-infection;Apoptosis储存⽅式:4°C,sealedstorage,awayfrommoistureandlight*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoistureandlight)溶解性数据体外实验H2O:≥200mg/mL(139.94mM)DMSO:83.33mg/mL(58.31mM;Needultrasonic)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM0.6997mL3.4985mL6.9971mL5mM0.1399mL0.6997mL1.3994mL10mM0.0700mL0.3499mL0.6997mL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(sealedstorage,awayfrommoistureandlight)。-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。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀1/4MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(1.46mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(1.46mM);Clearsolution3.请依序添加每种溶剂：PBSSolubility:100mg/mL(69.97mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性Suraminsodiumsalt(Suraminhexasodiumsalt)⼀种可逆的竞争性蛋⽩酪氨酸磷酸酶(PTPases)抑制剂。Suraminsodiumsalt有效的sirtuins抑制剂：SirT1(IC50=297nM)，SirT2(IC50=1.15μM)，SirT5(IC50=22μM)。Suraminsodiumsalt竞争性逆转录酶抑制剂(DNAtopoisomeraseII:IC50=5μM)。Suraminsodiumsalt⼀种有效的SARS-CoV-2RNA依赖性RNA聚合酶(RdRp)抑制剂。Suraminsodiumsalt有效抑制IP5K，并且抗寄⽣⾍(antiparasitic)，抗肿瘤和抗⾎管⽣成剂。IC50&TargetSIRT1SIRT2SIRT5297nM(IC50)1.15μM(IC50)22μM(IC50)体外研究Suraminsodiumsalt(Suraminhexasodiumsalt;50-600μg/mL;for24-96hours)inhibitscellsproliferationinadose-dependentandtime-dependentmanneranddecreasesviabilityincancercells[7].Suraminsodiumsalt(300μg/mL;for48hours)inducescellsapoptosisanddown-regulatesmRNAexpressioninHeLacells[7].Suraminsodiumsalt(1mg/mL;1hour)significantlysuppressesthephosphorylatedERK1/2[8].TheIC50valuesofHO-8910PMandHeLaare319μg/mL,476μg/mL,respectively[7].SuraminblocksviralreplicationinVeroE6cells[5].CellProliferationAssay[6]CellLine:HO-8910PMovarianandHelacervicalcancercellsConcentration:50,100,200,300,400,500and600μg/mLIncubationTime:For24,48,72and96hoursResult:Inhibitedcellsproliferationinadose-dependentandtime-dependentmanner.ApoptosisAnalysis[6]CellLine:HeLacellsConcentration:300μg/mLIncubationTime:For48hoursResult:Inducedcellsapoptosis.2/4MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEWesternBlotAnalysis[7]CellLine:PA-SMCscellsConcentration:1mg/mLIncubationTime:For1hourResult:SignificantlysuppressedthephosphorylatedERK1/2.体内研究Suraminsodiumsalt(Suraminhexasodiumsalt;10mg/kg;IV;twiceweeklyfor3weeks)reversesestablishedpulmonaryhypertension(PH),therebynormalizingthepulmonaryarterypressurevaluesandvesselstructure[8].AnimalModel:AdultmaleWistarrats(200-225g)[7]Dosage:10mg/kgAdministration:IV;twiceweeklyfor3weeksResult:ReversedestablishedPH,therebynormalizingthepulmonaryarterypressurevaluesandvesselstructure.户使⽤本产品发表的科研⽂献•NatStructMolBiol.2021Mar;28(3):319-325.•BrJPharmacol.2021Aug6.•ClinTranslMed.2021Jun;11(6):e485.•JBiolChem.2021Sep3;101166.•JBiolChem.2020Jul24;295(30):10281-10292.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].XiaozheZhang,etal.SuraminandNF449AreIP5KInhibitorsThatDisruptIP6-mediatedRegulationofCullinRINGLigaseandSensitizeCancerCellstoMLN4924/pevonedistat.JBiolChem.2020Jun3;jbc.RA120.014375.[2].JindalHK,etal.SuraminaffectsDNAsynthesisinHeLacellsbyinhibitionofDNApolymerases.CancerRes.1990Dec15;50(24):7754-7.[3].IzikkiM,etal.Thebeneficialeffectofsuraminonmonocrotaline-inducedpulmonaryhypertensioninrats.PLoSOne.2013Oct15;8(10):e77073.[4].ZhangYL,etal.Suraminisanactivesite-directed,reversible,andtight-bindinginhibitorofprotein-tyrosinephosphatases.JBiolChem.1998May15;273(20):12281-7.[5].TrappJ,etal.Structure-activitystudiesonsuraminanaloguesasinhibitorsofNAD+-dependenthistonedeacetylases(sirtuins).3/4MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEChemMedChem.2007Oct;2(10):1419-31.[6].SchuetzA,etal.StructuralbasisofinhibitionofthehumanNAD-dependentdeacetylaseSIRT5bysuramin.Structure.2007Mar;15(3):377-89.[7].DeClercqE,etal.Suramin:apotentinhibitorofthereversetranscriptaseofRNAtumorviruses.CancerLett.1979Nov;8(1):9-22.[8].NovaesRD,etal.PurinergicAntagonistSuraminAggravatesMyocarditisandIncreasesMortalitybyEnhancingParasitism,Inflammation,andReactiveTissueDamageinTrypanosomacruzi-InfectedMice.OxidMedCellLongev.2018Sep30;2018:7385639.[9].WanchaoYin,etal.StructuralbasisforinhibitionoftheSARS-CoV-2RNApoly