Marizomib-Salinosporamide-A-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEMarizomibCat.No.:HY-10985CASNo.:437742-34-2Synonyms:SalinosporamideA;NPI-0052分⼦式:C₁₅H₂₀ClNO₄分⼦量:313.78作⽤靶点:Proteasome作⽤通路:MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥100mg/mL(318.69mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM3.1869mL15.9347mL31.8695mL5mM0.6374mL3.1869mL6.3739mL10mM0.3187mL1.5935mL3.1869mL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、析出现象，可以通过加热和/或超声的⽅式助溶)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(6.63mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(6.63mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Marizomib(SalinosporamideA)第⼆代不可逆的脑渗透性泛蛋⽩酶体(proteasome)抑制剂。Marizomib抑制20S蛋⽩酶体的CT-L(β5)、CT-T-laspase样(C-L,β1)和胰蛋⽩酶样(T-L,β2)活性(IC50分别为3.5,28,430nM)。IC50&TargetIC50:3.5nM(CT-L),28nM(CT-T-laspase-like),430nM(trypsin-like)[1]体外研究Marizomib(SalinosporamideA)(0.1-10000nM;72hours)effectivelyreducessurvivalofD-54andU-251cellsinadose-dependentmanner.TheIC50sare-52nMforU-251and-20nMforD-54[1].Marizomib(24hours;60nM)inducesapoptosisandcaspase-3activationingliomacells[1].CellProliferationAssay[1]CellLine:U-251andD-54cellsConcentration:0.1,1,10,100,1000,10000nMIncubationTime:72hoursResult:EffectivelyreducedsurvivalofD-54andU-251cellsinadose-dependentmanner.ApoptosisAnalysis[1]CellLine:D-54cellsConcentration:60nMIncubationTime:24hoursResult:InducesD-54cellsapoptosis.WesternBlotAnalysis[1]CellLine:D-54cellsConcentration:60nMIncubationTime:24hoursResult:Ledtoincreasedactivityofcaspase-3inadose-dependentmanner.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE体内研究Marizomib(SalinosporamideA)(0.15mg/kg;i.v;twiceaweekforthreeweeks)significantlydecreasestumorgrowth,andisnotassociatedwithanytoxicity[3].AnimalModel:CB-17SCID-malemice(4-6weeksold)[3]Dosage:0.15mg/kgAdministration:i.v;twiceaweekforthreeweeksResult:Significantlydecreasedtumorgrowth,andwasnotassociatedwithanytoxicity.户使⽤本产品发表的科研⽂献•ACSCatal.September8,2021.•JExpClinCancerRes.2022Oct22;41(1):311.•CellDeathDis.2022Oct8;13(10):860.•IntJMolSci.2022,23(5),2655.•BiochemPharmacol.2022Oct29;206:115326.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].DiK,etal.Marizomibactivityasasingleagentinmalignantgliomas:abilitytocrosstheblood-brainbarrier.NeuroOncol.2016Jun;18(6):840-8.[2].KaleAJ,etal.Molecularmechanismsofacquiredproteasomeinhibitorresistance.JMedChem.2012Dec13;55(23):10317-27.[3].SinghAV,etal.PharmacodynamicandefficacystudiesofthenovelproteasomeinhibitorNPI-0052(marizomib)inahumanplasmacytomaxenograftmurinemodel.BrJHaematol.2010May;149(4):550-9.McePdfHeightCaution:Producthasnotbeen