2. Metabolic Enzyme/Protease
  3. E1/E2/E3 Enzyme
  4. NSC232003

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.

For research use only. We do not sell to patients.

CAS No. : 1905453-18-0

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Customer Review

Based on 5 publication(s) in Google Scholar

NSC232003 Related Antibodies

Top Publications Citing Use of Products

    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.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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.

    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.

    NSC232003 Related Antibodies
    Molecular Weight

    169.14

    Formula

    C6H7N3O3
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C1NC(/C(C=N1)=C(NO)/C)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    H2O : 2 mg/mL (11.82 mM; Need ultrasonic)

    DMSO : < 1 mg/mL (insoluble or slightly soluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 5.9123 mL 29.5613 mL 59.1226 mL
    5 mM 1.1825 mL 5.9123 mL 11.8245 mL
    View the 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.

    * 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.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    Volume (start)

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    C2

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    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.

    • Protocol 1

      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

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

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    (per animal)

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
    Purity & Documentation
    References

    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.

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    NSC232003 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    NSC2320031905453-18-0NSC 232003NSC-232003E1/E2/E3 EnzymeE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseInhibitorinhibitorinhibit

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    Product Name:
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    Cat. No.:
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