Marizomib-Salinosporamide-A-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEMarizomibCat.No.:HY-10985CASNo.:437742-34-2Synonyms:SalinosporamideA;NPI-0052分?式:C??H??ClNO?分?量:313.78作?靶點:Proteasome作?通路:MetabolicEnzyme/Protease儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:≥100mg/mL(318.69mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.1869mL15.9347mL31.8695mL5mM0.6374mL3.1869mL6.3739mL10mM0.3187mL1.5935mL3.1869mL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。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?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：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(6.63mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(6.63mM);ClearsolutionBIOLOGICALACTIVITY?物活性Marizomib(SalinosporamideA)第?代不可逆的腦滲透性泛蛋?酶體(proteasome)抑制劑。Marizomib抑制20S蛋?酶體的CT-L(β5)、CT-T-laspase樣(C-L,β1)和胰蛋?酶樣(T-L,β2)活性(IC50分別為3.5,28,430nM)。IC50&TargetIC50:3.5nM(CT-L),28nM(CT-T-laspase-like),430nM(trypsin-like)[1]體外研究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?邊的抑制劑?師www.MedChemE體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻?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