Auranofin-SKF-39162-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAuranofinCat.No.:HY-B1123CASNo.:34031-32-8Synonyms:SKF-39162分⼦式:C₂₀H₃₆AuO₉PS分⼦量:680.5作⽤靶点:Bacterial;SARS-CoV作⽤通路:Anti-infection储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:50mg/mL(73.48mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.4695mL7.3475mL14.6951mL5mM0.2939mL1.4695mL2.9390mL10mM0.1470mL0.7348mL1.4695mL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,awayfrommoisture)。-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、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:≥2.5mg/mL(3.67mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.08mg/mL(3.06mM);Suspendedsolution;Needultrasonicandwarming3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.06mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Auranofin(SKF-39162)硫氧还蛋⽩还原酶(TrxR)的抑制剂，IC50为0.2μM。Auranofin表现出抗SARS-CoV21的抗病毒活性，对猴肾VeroE6细胞的CC50为4.2μM。IC50&TargetIC50:0.2μM(TrxR)[1]体外研究Auranofinisadrugthatisapprovedforthetreatmentofrheumatoidarthritisbutisbeinginvestigatedforpotentialtherapeuticapplicationinanumberofotherdiseasesincludingcancer,neurodegenerativedisorders.AuranofininducesapoptosisincellsthroughaBax/Bak-dependentmechanismassociatedwithselectivedisruptionofmitochondrialredoxhomeostasisinconjunctionwithoxidationofPrx3[1].AuranofininhibitsproliferationandsurvivalofSKOV3cellsinadose-andtime-dependentmanner.Auranofintreatmentactivatesthepro-apoptoticcaspase-3,increasesproteinlevelsofapoptosis-inducingproteinsBaxandBimandreducestheexpressionoftheanti-apoptoticmediatorBcl-2inSKOV3cells[2].Auranofinisalipophilicgoldcompoundwithanti-inflammatoryandimmunosuppressiveproperties.AuranofininhibitsthecellgrowthandinductionofmitochondrialapoptosisinPC3humanprostatecancercells.TreatmentwithauranofinsignificantlyinhibitscellviabilitywithanIC50valueof2.5μMafter24h[3].体内研究Prophylactictreatmentofadjuvant-inducedarthritisratswithauranofinresultsinaslightreductioninpawedema,acompletenormalizationofthedepressedIL-2production,andareductionoftheelevatedIL-1production,buthasnoeffectonthedepressedIL-3production[4].PROTOCOLCellAssay[2]AuranofinisdissolvedinDMSO.Cellsaretreatedwithauranofin(0,50,100,200and400nM)for72hforthedose-dependentresponseassayand100nMofauranofinisaddedintothewellsfor0,24,72and120hforthetime-dependentresponseassay.ControlculturesaretreatedwithDMSO.CellviabilityismeasuredbytheMTTassay[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalRats:Prophylactically,auranofin(6.7to15mgofgold/kg),indomethacin(2mg/kg)ortragacanthvehicleAdministration[4]controlwereadministeredorallyatdailyintervalsbeginningonthedayofadjuvantinjection.Ondays16to17peritonealexudatecellsorspleencellsfromnormaloradjuvant-injectedratswereisolatedandtested[4].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•NatMicrobiol.2020Nov;5(11):1439-1448.•NucleicAcidsRes.2021Jan8;49(D1):D1113-D1121.•NatCommun.2020Oct16;11(1):5263.•CellDeathDiffer.2020Mar;27(3):1086-1104.•RedoxBiol.2020Sep;36:101652.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].CoxAG,etal.ThethioredoxinreductaseinhibitorauranofintriggersapoptosisthroughaBax/Bak-dependentprocessthatinvolvesperoxiredoxin3oxidation.BiochemPharmacol.2008Oct30;76(9):1097-109.[2].ParkSH,etal.AuranofindisplaysanticanceractivityagainstovariancancercellsthroughFOXO3activationindependentofp53.IntJOncol.2014Oct;45(4):1691-8.[3].ParkN,etal.AuranofinpromotesmitochondrialapoptosisbyinducingannexinA5expressionandtranslocationinhumanprostatecancercells.JToxicolEnvironHealthA.2014;77(22-24):1467-76.[4].LeeJC,etal.Effectofauranofintreatmentonaberrantsplenicinterleukinproductioninadjuvantarthriticrats.JImmunol.1987Nov15;139(10):3268-74.[5].ShuofengYuan,etal.MetallodrugranitidinebismuthcitratesuppressesSARS-CoV-2replicationandrelievesvirus-associatedpneumoniainSyria