NSC232003-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemENSC232003Cat.No.:HY-103236CASNo.:1905453-18-0分⼦式:C₆H₇N₃O₃分⼦量:169.14作⽤靶点:E1/E2/E3Enzyme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H2O:2mg/mL(11.82mM;Needultrasonic)DMSO:<1mg/mL(insolubleorslightlysoluble)MassSolvent1mg5mg10mgConcentration制备储备液1mM5.9123mL29.5613mL59.1226mL5mM1.1825mL5.9123mL11.8245mL10mM0.5912mL2.9561mL5.9123mL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。BIOLOGICALACTIVITY⽣物活性NSC232003⼀种⾼效的可渗透细胞的UHRF1抑制剂，可抑制DNA甲化，并破坏DNMT1/UHRF1相互作⽤。IC50&TargetUHRF1[1]1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE体外研究NSC232003,auracilderivativefreelyavailablebytheNCI/DTPrepository,providesaversatileleadfordevelopinghighlypotentandcell-permeableUHRF1inhibitorsthatwillenabledissectionofDNAmethylationinheritance.NSC232003isindeedaneffectiveDNAmethylationinhibitorandindicatethatthisparticularnucleotidescaffoldcouldprovideaversatilebasisforthedesignofpotentUHRF1inhibitors.NSC232003ispredictedtobepartiallydeprotonatedatpH7,asthepKaofthemoreacidicimidenitrogenofthepyrimidineringisavalueof7.6inNSC232003.TheDNMT1/UHRF1interactionsaresignificantlyreducedafter4hofincubationofU251gliomacellswiththemostpotentcompoundNSC232003,showinga50%interactioninhibitionat15μMaswellasinductionofglobalDNAcytosinedemethylationasmeasuredbyELISA[1].户使⽤本产品发表的科研⽂献•EBioMedicine.2022May;79:103985.•JCIInsight.2022Sep27;e162831.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].MyrianthopoulosV,etal.TandemvirtualscreeningtargetingtheSRAdomainofUHRF1identifiesanovelchemicaltoolmodulatingDNAmethylation.EurJMedChem.2016May23;114:390-6.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel: