WS-383-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEWS-383Cat.No.:HY-126075ACASNo.:2247544-02-9分?式:C??H??Cl?N?S?分?量:498.46作?靶點:E1/E2/E3Enzyme作?通路:MetabolicEnzyme/Protease儲存?式:4°C,sealedstorage,awayfrommoistureandlight*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoistureandlight)溶解性數(shù)據(jù)體外實驗DMSO:7.35mg/mL(14.75mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.0062mL10.0309mL20.0618mL5mM0.4012mL2.0062mL4.0124mL10mM0.2006mL1.0031mL2.0062mL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(sealedstorage,awayfrommoistureandlight)。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。BIOLOGICALACTIVITY?物活性WS-383?種有效、選擇性、可逆的DCN1-UBC12相互作?抑制劑，IC50值為11nM。WS-383抑制Cul3/1的類泛素化修飾，引起p21，p27和NRF2的積累[1]。IC50&TargetIC50:11nM(DCN1-UBC12interaction)[1]體外研究WS-383(10μM)isagainstapanelofkinasessuchasBTK,CDKs,andEGFR[L858R]usingstaurosporine1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEandBIBW2992asthepositivecontrols.WS-383showedweakinhibitoryactivityat10.0μM,itisselectivetotheDCN1-UBC12interactionovertheselectedkinasesr[1].WS-383(0.03-3μM;24hours)blocksCul3neddylationat3μMandalsohascertaininhibitionofCul1neddylationat10μMbutwasnoteffectiveininhibitingneddylationofothercullinmembers[1].WS-383(0.03-3μM;24hours)increasesCul1,Skp1(adaptorprotein),F-boxprotein,andRBX1/RBX2RINGproteinformSCFE3complex.Cyclindependentkinaseinhibitor1A(p21)andcyclindependentkinaseinhibitor1B(p27)expressioninadose-dependentmannerinMGC-803andKYSE70manner[1].WesternBlotAnalysis[1]CellLine:MGC-803cellsConcentration:0.03μM;0.3μM;3μM;10μMIncubationTime:24hoursResult:DecreasedN8-Cul1andN8-Cul2proteinexpression.WesternBlotAnalysis[1]CellLine:MGC-803andKYSE70cellsConcentration:0.03μM;0.3μM;3μM;10μMIncubationTime:24hoursResult:Inducedaccumulationofp21,p27,andNRF2inMGC-803cells.REFERENCES[1].WangS,etal.DevelopmentofHighlyPotent,Selective,andCellularActiveTriazolo[1,5-a]pyrimidine-BasedInhibitorsTargetingtheDCN1-UBC12Protein-ProteinInteraction.JMedChem.2019Mar14;62(5):2772-2797.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearc