Suramin-sodium-salt-Suramin-hexasodium-salt-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemESuraminsodiumsaltCat.No.:HY-B0879ACASNo.:129-46-4Synonyms:Suraminhexasodiumsalt分?式:C??H??N?Na?O??S?分?量:1429.17作?靶點(diǎn):Phosphatase;Sirtuin;ReverseTranscriptase;Topoisomerase;SARS-CoV;Parasite;Apoptosis作?通路:MetabolicEnzyme/Protease;CellCycle/DNADamage;Epigenetics;Anti-infection;Apoptosis儲存?式:4°C,sealedstorage,awayfrommoistureandlight*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoistureandlight)溶解性數(shù)據(jù)體外實(shí)驗(yàn)H2O:≥200mg/mL(139.94mM)DMSO:83.33mg/mL(58.31mM;Needultrasonic)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM0.6997mL3.4985mL6.9971mL5mM0.1399mL0.6997mL1.3994mL10mM0.0700mL0.3499mL0.6997mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoistureandlight)。-80°C儲存時，請?jiān)?個?內(nèi)使?，-20°C儲存時，請?jiān)?個?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀1/4MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(1.46mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(1.46mM);Clearsolution3.請依序添加每種溶劑：PBSSolubility:100mg/mL(69.97mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性Suraminsodiumsalt(Suraminhexasodiumsalt)?種可逆的競爭性蛋?酪氨酸磷酸酶(PTPases)抑制劑。Suraminsodiumsalt有效的sirtuins抑制劑：SirT1(IC50=297nM)，SirT2(IC50=1.15μM)，SirT5(IC50=22μM)。Suraminsodiumsalt競爭性逆轉(zhuǎn)錄酶抑制劑(DNAtopoisomeraseII:IC50=5μM)。Suraminsodiumsalt?種有效的SARS-CoV-2RNA依賴性RNA聚合酶(RdRp)抑制劑。Suraminsodiumsalt有效抑制IP5K，并且抗寄??(antiparasitic)，抗腫瘤和抗?管?成劑。IC50&TargetSIRT1SIRT2SIRT5297nM(IC50)1.15μM(IC50)22μM(IC50)體外研究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?邊的抑制劑?師www.MedChemEWesternBlotAnalysis[7]CellLine:PA-SMCscellsConcentration:1mg/mLIncubationTime:For1hourResult:SignificantlysuppressedthephosphorylatedERK1/2.體內(nèi)研究Suraminsodiumsalt(Suraminhexasodiumsalt;10mg/kg;IV;twiceweeklyfor3weeks)reversesestablishedpulmonaryhypertension(PH),therebynormalizingthepulmonaryarterypressurevaluesandvesselstructure[8].AnimalModel:AdultmaleWistarrats(200-225g)[7]Dosage:10mg/kgAdministration:IV;twiceweeklyfor3weeksResult:ReversedestablishedPH,therebynormalizingthepulmonaryarterypressurevaluesandvesselstructure.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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?邊的抑制劑?師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