2. Cell Cycle/DNA Damage
  3. CDK
  4. NG 52

NG 52 is a potent, cell-permeable, selective, ATP-compatible and orally active Cdc28p and Pho85p kinase inhibitor with IC50s of 7 μM and 2 μM, respectively. NG 52 also inhibits the activity of phosphoglycerate kinase 1 (PGK1) with an IC50 of 2.5 μM. NG 52 is inactive against yeast kinases Kin28p, Srb10, and Cak1p.

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

NG 52 Chemical Structure

NG 52 Chemical Structure

CAS No. : 212779-48-1

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 227 In-stock
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10 mM * 1 mL in DMSO USD 227 In-stock
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5 mg USD 206 In-stock
10 mg USD 370 In-stock
50 mg USD 1115 In-stock
100 mg USD 1452 In-stock
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Customer Review

Based on 5 publication(s) in Google Scholar

NG 52 Related Antibodies

Top Publications Citing Use of Products

    NG 52 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2020 Jul 31.  [Abstract]

    Inhibition of NG52 on the phosphorylation of PDHK1 and PDH in glioma cells is examined by Western blot after glioma cells are treated with NG52 for 12 h under hypoxic conditions.

    View All CDK Isoform Specific Products:

    View All Isoforms
    CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    NG 52 is a potent, cell-permeable, selective, ATP-compatible and orally active Cdc28p and Pho85p kinase inhibitor with IC50s of 7 μM and 2 μM, respectively. NG 52 also inhibits the activity of phosphoglycerate kinase 1 (PGK1) with an IC50 of 2.5 μM. NG 52 is inactive against yeast kinases Kin28p, Srb10, and Cak1p[1][2].

    IC50 & Target[1][2]

    cdc2-cyclin B

    0.34 μM (IC50)

    Pho85p

    2 nM (IC50)

    Cdc28p

    7 μM (IC50)

    Phosphoglycerate kinase 1 (PGK1)

    2.5 μM (IC50)

    In Vitro

    NG 52 (Compound 52) inhibits growth in a drug-sensitized yeast strain (S. cerevisiae) with a GI50 of 30 μM. NG 52 is active against cdc2-cyclin B with an IC50 value of 340 nM[1].
    NG 52 dose-dependently inhibits the proliferation of glioma U87 and U251 cell lines with GI50 values of 7.8 μM and 5.2 μM, respectively, meanwhile it potently inhibits the proliferation of primary glioma cells[2].
    NG 52 (12.5-50 μM) effectively inhibits the phosphorylation of PDHK1 at Thr338 site and the phosphorylation of PDH at Ser293 site in U87 and U251 cells, resulting in more pyruvic acid entering the Krebs cycle with increased production of ATP and ROS[2].
    NG 52 can reverse the Warburg effect by enhancing the activity of pyruvate dehydrogenase (PDH) through inhibiting the activity of PGK1, and switched cellular glucose metabolism from anaerobic mode to aerobic mode[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    NG 52 Related Antibodies

    Cell Proliferation Assay[2]

    Cell Line: Glioma U87 and U251 cells
    Concentration: 0 μM, 12.5 μM, 25 μM, 50 μM
    Incubation Time: 6 days
    Result: Potently inhibited the proliferation of primary glioma cells.

    Western Blot Analysis[2]

    Cell Line: Glioma U87 and U251 cells
    Concentration: 0 μM, 12.5 μM, 25 μM, 50 μM
    Incubation Time: 12 hours or 24 hours
    Result: Potently inhibited the proliferation of primary glioma cells.
    In Vivo

    NG 52 (50-150 mg/kg; oral administration; daily; for 13 days) treatment dose-dependently suppresses the growth of glioma xenograft[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Female nu/nu mice (5-week-old) injected with glioma cells[2]
    Dosage: 50 mg/kg, 100 mg/kg, 150 mg/kg
    Administration: Oral administration; daily; for 13 days
    Result: Dose-dependently suppressed the growth of glioma xenograft.
    Molecular Weight

    346.81

    Formula

    C16H19ClN6O
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    ClC1=CC(NC2=NC(NCCO)=NC3=C2N=CN3C(C)C)=CC=C1
    Shipping

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

    DMSO : 75 mg/mL (216.26 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.8834 mL 14.4171 mL 28.8342 mL
    5 mM 0.5767 mL 2.8834 mL 5.7668 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    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:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (7.21 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (7.21 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock 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).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.97%

    COA (250 KB) LCMS (111 KB)

    Handling Instructions (2659 KB)
    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.8834 mL 14.4171 mL 28.8342 mL 72.0856 mL
    5 mM 0.5767 mL 2.8834 mL 5.7668 mL 14.4171 mL
    10 mM 0.2883 mL 1.4417 mL 2.8834 mL 7.2086 mL
    15 mM 0.1922 mL 0.9611 mL 1.9223 mL 4.8057 mL
    20 mM 0.1442 mL 0.7209 mL 1.4417 mL 3.6043 mL
    25 mM 0.1153 mL 0.5767 mL 1.1534 mL 2.8834 mL
    30 mM 0.0961 mL 0.4806 mL 0.9611 mL 2.4029 mL
    40 mM 0.0721 mL 0.3604 mL 0.7209 mL 1.8021 mL
    50 mM 0.0577 mL 0.2883 mL 0.5767 mL 1.4417 mL
    60 mM 0.0481 mL 0.2403 mL 0.4806 mL 1.2014 mL
    80 mM 0.0360 mL 0.1802 mL 0.3604 mL 0.9011 mL
    100 mM 0.0288 mL 0.1442 mL 0.2883 mL 0.7209 mL
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    NG 52 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:

    NG 52212779-48-1Compound 52NG52NG-52Compound52Compound-52CDKCyclin dependent kinaseCDK2Cdc28pPho85pATP-compatiblecdc2-cyclin ByeastPGK1anti-proliferationPDHK1ATPROSWarburggliomaInhibitorinhibitorinhibit

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