NSC232003-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENSC232003Cat. No.: HY-103236CAS No.: 1905453-18-0分式: CHNO分量: 169.14作靶点: E1/E2/E3 Enzyme作通路: Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 H2O : 17 mg/mL (100.51 mM; Need

2、 ultrasonic and warming)DMSO : 1 mg/mL (insoluble or slightly soluble)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 5.9123 mL 29.5613 mL 59.1226 mL5 mM 1.1825 mL 5.9123 mL 11.8245 mL10 mM 0.5912 mL 2.9561 mL 5.9123 mL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，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 NSC232003种效

3、的可渗透细胞的 UHRF1 抑制剂，可抑制 DNA 甲基化，并破坏 DNMT1/UHRF1 相互作。IC50 & Target UHRF1 1体外研究NSC232003, a uracil derivative freely available by the NCI/DTP repository, provides a versatile lead for1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEdeveloping highly potent and cell-permeable UHRF1 inhibitors that will e

4、nable dissection of DNA methylationinheritance. NSC232003 is indeed an effective DNA methylation inhibitor and indicate that this particularnucleotide scaffold could provide a versatile basis for the design of potent UHRF1 inhibitors. NSC232003 ispredicted to be partially deprotonated at pH 7, as th

5、e pKa of the more acidic imide nitrogen of the pyrimidinering is a value of 7.6 in NSC232003. The DNMT1/UHRF1 interactions are significantly reduced after 4 h ofincubation of U251 glioma cells with the most potent compound NSC232003, showing a 50% interactioninhibition at 15 M as well as induction o

6、f global DNA cytosine demethylation as measured by ELISA 1.REFERENCES1. Myrianthopoulos V, et al. Tandem virtual screening targeting the SRA domain of UHRF1 identifies a novel chemical tool modulating DNAmethylation. Eur J Med Chem. 2016 May 23;114:390-6.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-