NSC232003-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemENSC232003Cat.No.:HY-103236CASNo.:1905453-18-0分?式:C?H?N?O?分?量:169.14作?靶點:E1/E2/E3Enzyme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H2O:2mg/mL(11.82mM;Needultrasonic)DMSO:<1mg/mL(insolubleorslightlysoluble)MassSolvent1mg5mg10mgConcentration制備儲備液1mM5.9123mL29.5613mL59.1226mL5mM1.1825mL5.9123mL11.8245mL10mM0.5912mL2.9561mL5.9123mL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?。BIOLOGICALACTIVITY?物活性NSC232003?種?效的可滲透細胞的UHRF1抑制劑，可抑制DNA甲化，并破壞DNMT1/UHRF1相互作?。IC50&TargetUHRF1[1]1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE體外研究NSC232003,auracilderivativefreelyavailablebytheNCI/DTPrepository,providesaversatileleadfordevelopinghighlypotentandcell-permeableUHRF1inhibitorsthatwillenabledissectionofDNAmethylationinheritance.NSC232003isindeedaneffectiveDNAmethylationinhibitorandindicatethatthisparticularnucleotidescaffoldcouldprovideaversatilebasisforthedesignofpotentUHRF1inhibitors.NSC232003ispredictedtobepartiallydeprotonatedatpH7,asthepKaofthemoreacidicimidenitrogenofthepyrimidineringisavalueof7.6inNSC232003.TheDNMT1/UHRF1interactionsaresignificantlyreducedafter4hofincubationofU251gliomacellswiththemostpotentcompoundNSC232003,showinga50%interactioninhibitionat15μMaswellasinductionofglobalDNAcytosinedemethylationasmeasuredbyELISA[1].戶使?本產(chǎn)品發(fā)表的科研?獻?EBioMedicine.2022May;79:103985.?JCIInsight.2022Sep27;e162831.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].MyrianthopoulosV,etal.TandemvirtualscreeningtargetingtheSRAdomainofUHRF1identifiesanovelchemicaltoolmodulatingDNAmethylation.EurJMedChem.2016May23;114:390-6.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel: