NSC232003
Based on 5 publication(s) in Google Scholar
NSC232003 is a highly potent and cell-permeable UHRF1 inhibitor, which inhibits DNA methylation in vitro and disrupts DNMT1/UHRF1 interactions at a cellular level.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.94%
- No. CAS: 1905453-18-0
- Fòrmula: C6H7N3O3
- Peso molecular:169.14
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) NSC232003
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Customer Validation & Images
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IF
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Apoptosis Analysis
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Cell Imaging/Staining
Actividad biológica
Descripciòn
IC50 & Target
UHRF1[1]
In Vitro
NSC232003, a uracil derivative freely available by the NCI/DTP repository, provides a versatile lead for developing highly potent and cell-permeable UHRF1 inhibitors that will enable dissection of DNA methylation inheritance. NSC232003 is indeed an effective DNA methylation inhibitor and indicate that this particular nucleotide scaffold could provide a versatile basis for the design of potent UHRF1 inhibitors. NSC232003 is predicted to be partially deprotonated at pH 7, as the pKa of the more acidic imide nitrogen of the pyrimidine ring is a value of 7.6 in NSC232003. The DNMT1/UHRF1 interactions are significantly reduced after 4 h of incubation of U251 glioma cells with the most potent compound NSC232003, showing a 50% interaction inhibition at 15 μM as well as induction of global DNA cytosine demethylation as measured by ELISA[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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No. CAS 1905453-18-0
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Appearance Solid
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Peso molecular 169.14
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Fòrmula C6H7N3O3
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Color White to off-white
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SMILES
O=C1NC(/C(C=N1)=C(NO)/C)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (5)
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Journal Impact Factor
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Most Recent
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EBioMedicine
2022 May;79:103985. PMID: 35429693 -
JCI Insight
Liposomal UHRF1 siRNA shows lung fibrosis treatment potential by regulating fibroblast activation. [Abstract]2022 Sep 27;e162831. PMID: 36166308 -
J Biol Chem
UHRF1-mediated ubiquitination of nonhomologous end joining factor XLF promotes DNA repair in human tumor cells. [Abstract]2024 Nov;300(11):107823. PMID: 39341501
NSC232003 purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2024 Nov;300(11):107823. [Abstract]
HeLa WT cells were transfected with GFP-UHRF1, after 4 h of treatment with 20 μM NSC232003, dynamic recruitment of UHRF1 to DNA damage tracks were monitored using laser micro-irradiation–coupled live-cell imaging.
NSC232003 purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2024 Nov;300(11):107823. [Abstract]
HeLa cells were irradiated with 5 Gy IR for 1 h, treated with 20 μM VP16 for 2 h, and then released for 2 h before being treated with 20 μM NSC232003 for 4 h. Apoptosis was assessed using the Annexin V-FITC apoptosis detection kit.
NSC232003 purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2024 Nov;300(11):107823. [Abstract]
HeLa cells were irradiated with IR for 6 h and then reseeded in 6-well plates. Twenty micromolars of NSC232003 was added, and cell clones were analyzed for relative viability by crystal violet staining.
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J Appl Toxicol
2025 Jun 12. PMID: 40509639 -
Cytoskeleton (Hoboken)
Analyses of Off-Target Effects on Cardiac and Skeletal Muscles by Berberine, a Drug Used to Treat Cancers and Induce Weight Loss. [Abstract]2025 Jun;82(6):344-359. PMID: 39526308
Solvente y solubilidad
In Vitro:
H2O : 2 mg/mL (11.82 mM; Need ultrasonic)
DMSO : < 1 mg/mL (insoluble or slightly soluble)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 4.76 mg/mL (28.14 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
Protocolo
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Research Protocol for Epigenomic Data Analysis
Epigenomic data analysis identifies genome-wide regulatory features that influence gene expression, chromatin state, and phenotype without changing the underlying DNA sequence. In this strategy, the core regulatory layer includes chromatin accessibility, transcription-factor or histone-mark occupancy, DNA methylation, and chromatin-state patterns; these features are measured by sequencing-based assays and interpreted as regulatory elements, promoters, enhancers, repressive domains, methylated cytosines, or candidate phenotype-associated chromatin programs. The literature links epigenomic features to phenotype by showing that functional genomic elements can be mapped across human cell types and tissues, and that integrated epigenomic maps reveal cell-type-specific regulatory programs. ENCODE integrated transcription, chromatin accessibility, transcription-factor occupancy, and histone modification data to annotate functional elements in the human genome, while the Roadmap Epigenomics Co
Pureza y Documentación
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Ficha de datos (273 KB)
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SDS (604 KB)
- English - EN (604 KB)
- Français - FR (604 KB)
- Deutsch - DE (604 KB)
- Norwegian - NO (604 KB)
- Español - ES (604 KB)
- Swedish - SV (604 KB)
- Italian - IT (604 KB)
- Korean - KR (604 KB)
- Portuguese - PT (604 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 5.9123 mL | 29.5613 mL | 59.1226 mL | 147.8066 mL |
| 5 mM | 1.1825 mL | 5.9123 mL | 11.8245 mL | 29.5613 mL | |
| 10 mM | 0.5912 mL | 2.9561 mL | 5.9123 mL | 14.7807 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
NSC232003 Related Classifications
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