Puromycin-aminonucleoside-NSC-3056-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPuromycinaminonucleosideCat.No.:HY-15695CASNo.:58-60-6Synonyms:NSC3056分⼦式:C₁₂H₁₈N₆O₃分⼦量:294.31作⽤靶点:Bacterial;Apoptosis;DipeptidylPeptidase;Aminopeptidase;Antibiotic作⽤通路:Anti-infection;Apoptosis;MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验H2O:40mg/mL(135.91mM;ultrasonicandwarmingandheatto50°C)DMSO:25mg/mL(84.94mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.3978mL16.9889mL33.9778mL5mM0.6796mL3.3978mL6.7956mL10mM0.3398mL1.6989mL3.3978mL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。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(7.07mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(7.07mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(7.07mM);Clearsolution4.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(7.07mM);Clearsolution5.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(7.07mM);Clearsolution6.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(7.07mM);Clearsolution7.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(7.07mM);Clearsolution8.请依序添加每种溶剂：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥2.5mg/mL(8.49mM);Clearsolution9.请依序添加每种溶剂：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(8.49mM);Clearsolution请依序添加每种溶剂：PBSSolubility:12.5mg/mL(42.47mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性Puromycinaminonucleoside(NSC3056)⼀种氨核苷类抗⽣素，为嘌呤霉素类似物[1]。Puromycinaminonucleoside诱导细胞凋亡(apoptosis)[2]。Puromycinaminonucleoside可逆抑制⼆肽肽酶(dipeptidylpeptidaseII)和胞浆丙氨酸氨肽酶[3]。Puromycinaminonucleoside诱导细胞迁移⼩体的分泌。IC50&TargetDPP-2体外研究Puromycinaminonucleoside(NSC3056)(30μg/mL)markedlyincreasesp53proteinlevelsinpodocytes.Puromycinaminonucleoside(NSC3056)-inducedpodocyteapoptosisisp53dependent.Puromycinaminonucleoside(NSC3056)inducespodocyteapoptosisinatime-dependentmanner[2].TheIC50valuesforPMAT-expressingandvector-transfectedcellsare48.9and122.1μM,respectively,suggestingexpressionofPMAT-enhancedcellsensitivitytoPuromycinaminonucleoside.Puromycinaminonucleoside(NSC3056)(250μM)istoxictobothPMAT-expressingandvector-transfectedcells.Puromycinaminonucleoside(NSC3056)uptakeinPMAT-expressingcellsisfourfoldhigheratpH6.6thanthatatpH7.4[5].体内研究Thenumberofpodocytesperglomerulusis95.5±17.6inthecontrolrats,90.7onDay4inPuromycinaminonucleoside(NSC3056)(8mg/100g,i.v.)-treatednephrosisrats.Theamountofnephrinperglomerulusincontrolratsis1.02±0.11fmolandthoseinPuromycinaminonucleoside(NSC3056)nephrosisratsarereducedto0.46±0.06fmoland0.35±0.04fmolonDay4andDay7.Thenephrinamountper2/4MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEpodocyteissignificantlydecreasedassociationwiththedevelopmentofproteinuriainPuromycinaminonucleoside(NSC3056)nephrosisrats[5].RatsgivenPuromycinaminonucleoside(NSC3056)(100mg/kg,s.c.)gainlessweightandtheirserumcreatininelevelsarehigherthanthecontrolrats[7].PROTOCOLCellAssay[4]CellsareseededinMEMwith10%FBSon96-wellplatesatadensityof5,000cells/well.Afterappr48-hincubation(appr40-50%confluence),cellsarechangedtofreshgrowthmediumcontainingPuromycinaminonucleoside(NSC3056)atvariousconcentrations.Fortheprotectionexperiment,cellsareincubatedinmediumcontaining250μMPuromycinaminonucleoside(NSC3056)withorwithoutthePMATinhibitordecynium-22(2μM).Afteratotalof72-hincubationina95%O2incubatorat37°C,cellsarewashedandtheplates.TheIC50valuesaredeterminedbyfittingthecellgrowthdatatothefollowingmodelusingnonlinearregression(WinNonLinversion3.2):S=Smax−[Smax−S0]×[Cγ/(Cγ+IC50γ)],whereSisthecellsurvivalexpressedaspercentageoftheopticaldensitytountreatedcontrolcells,Smaxisthemaximalcellsurvival,S0isthelowestresidualcellsurvivalatthehighdrugconcentration,CisPuromycinaminonucleosideconcentration,γistheHillcoefficient,andIC50isthePuromycinaminonucleosideconcentrationleadingtohalf-maximalcellsurvival.Fivetosixdeterminationsarecarriedoutwithineachexperiment,andfourindependentexperimentsareperformed.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMaleF344ratsat11weeksofagearepurchasedfromJaPuromycinaminonucleosideSLC.NormalratsandAdministration[5]aPuromycinaminonucleosidenephrosismodelareusedinthepresentstudy.Puromycinaminonucleoside(NSC3056)nephrosisisinducedinratsbyasingleintravenousinjectionofPuromycinaminonucleosideatadoseof8mg/100gbodyweightinsaline.Controlanimalsreceiveanidenticalvolumeofsaline.Nephroticrats(n=6pergroup)arestudiedatDays4and7afterthePuromycinaminonucleosideinjection.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•AdvSci(Weinh).2021Jan6;8(5):2002738.•PharmacolRes.2022Aug;182:106285.•FrontPharmacol.2021Mar8;12:603453.•JEthnopharmacol.2022Mar5;115171.•AmJTranslRes.2020Jul15;12(7):3512-3521.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].YingLiu,etal.Podocyte-ReleasedMigrasomesinUrineServeasanIndicatorforEarlyPodocyteInjury.KidneyDis(Basel).2020Nov;6(6):422-433.[2].WadaT,etal.Preventspodocyteapoptosisinducedbypuromycinaminonucleoside:roleofp53andBcl-2-relatedfamilyproteins.JAm3/4MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESocNephrol.2005Sep;16(9):2615-25.[3].XiaL,etal.Podocyte-specificexpressionoforganiccationtransporterPMAT:implicationinpuromycinaminonucleosidenephrotoxicity.AmJPhysiolRenalPhysiol.2009Jun;296(6):F1307-13.[4].KawakamiH,etal.Dynamicsofabsoluteamountofnephrininasinglepodocyteinpuromycinaminonucleosidenephrosisratscalculatedbyquantitativeglomerularproteomicsapproachwithselectedreactionmonitoringmode.NephrolDialTransplant.2012Apr;[5]