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  3. NG 52

NG 52 (Synonyms: Compound 52)

Cat. No.: HY-15154 Purity: 99.97%
Handling Instructions

NG 52 (Compound 52) is a potent, cell-permeable, selective, ATP-compatible and orally activeCdc28p 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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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 206 In-stock
Estimated Time of Arrival: December 31
5 mg USD 187 In-stock
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10 mg USD 336 In-stock
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50 mg USD 1014 In-stock
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100 mg USD 1320 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products

Publications Citing Use of MCE NG 52

    NG 52 purchased from MCE. Usage Cited in: Acta Pharmacol Sin. 2020 Jul 31.

    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.
    • Biological Activity

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    Description

    NG 52 (Compound 52) is a potent, cell-permeable, selective, ATP-compatible and orally activeCdc28p 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].

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

    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].

    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.

    212779-48-1

    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 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (288.34 mM; Need ultrasonic)

    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
    10 mM 0.2883 mL 1.4417 mL 2.8834 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

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

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

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

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.97%

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    Keywords:

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

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    Product Name:
    NG 52
    Cat. No.:
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