RA-9-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemERA-9Cat.No.:HY-136528CASNo.:919091-63-7分?式:C??H??N?O?分?量:365.34作?靶點(diǎn):Deubiquitinase;Apoptosis作?通路:CellCycle/DNADamage;Apoptosis儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:4.17mg/mL(11.41mM;ultrasonicandwarmingandheatto80°C)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.7372mL13.6859mL27.3718mL5mM0.5474mL2.7372mL5.4744mL10mM0.2737mL1.3686mL2.7372mL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(chǔ)備液，并請注意儲(chǔ)備液的保存?式和期限。BIOLOGICALACTIVITY?物活性RA-9?種?效選擇性蛋?酶體相關(guān)DUBs抑制劑，具有良好的毒性和抗癌活性。RA-9阻斷泛素依賴性蛋?降解?不響20S蛋?酶體蛋??解活性。RA-9選擇性誘導(dǎo)巢癌細(xì)胞株和供體原代培養(yǎng)細(xì)胞凋亡。RA-9誘導(dǎo)巢癌細(xì)胞內(nèi)質(zhì)?應(yīng)激反應(yīng)。體外研究RA-9(10-30μM;48hours)inhibitsgrowthofovariancancercelllinesandprimarycultures[1].RA-9(1.25-5μM;18hours)causescellcyclearrestandcaspase-mediatedapoptosisinovariancancercells[1].1/3MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemERA-9(5μM;0-24hours)inducesER-stressresponsesinovariancancercells[1].RA-9(5μM;over24hours)treatmentresultswithtime-dependentaccumulationofthecleavedformedofPARPnoticeableasearlyas8hours[1].CellViabilityAssay[1]CellLine:Cisplatin-sensitiveovariancancercelllinesTOV-21GandES-2,Cisplatin-resistantovariancancercelllinesHEYandOVCAR-3,primaryovariancancercellsConcentration:10,20,30μMIncubationTime:48hoursResult:Compromisedtheviabilityofovariancancercellsinadose-dependentfashion.CellCycleAnalysis[1]CellLine:ES-2cellsConcentration:1.25,5μMIncubationTime:18hoursResult:Resultedinadose-dependentincreaseinthefractionofES-2cellsintheG2-Mcellcyclephase.WesternBlotAnalysis[1]CellLine:ES-2,SKOV-3andTOV-21GovariancancercellsConcentration:5μMIncubationTime:0-24hResult:Causedatime-dependentincreaseinthesteadylevelsoftheearlyER-stressmarkerGRP-78,aswellasthelateER-stressmarkersIRE1-αandEro1L-α.體內(nèi)研究RA-9(5mg/kg;i.p;one-dayon,two-daysoff)inhibitshumanovariancancercellgrowthinvivoandprolongssurvivalinamousemodelforovariancancer[1].AnimalModel:Six-week-oldfemaleimmunodeficient(NCrnu/nu)mice[1]Dosage:5mg/kgAdministration:I.p;one-dayon,two-daysoffResult:Significantreductionintumorburdenatday12.REFERENCES2/3MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemE[1].CoughlinK,etal.Small-moleculeRA-9inhibitsproteasome-associatedDUBsandovariancancerinvitroandinvivoviaexacerbatingunfoldedproteinresponses.ClinCancerRes.2014;20(12):3174-3186.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplic