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Olomoucine

A Cyclin-Dependent Kinase (CDK) Inhibitor

Cat #: O-300
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 298.35
    Purity: >99%
    Effective concentration 20-200 µM.
    Structure
    Chemical name 6-(Benzylamino)-2-(2-hydroxyethylamino)-9-methylpurine.
    Molecular formula C15H18N6O.
    CAS No.: 101622-51-9
    Activity Olomoucine selectively inhibits cdc2/cyclin B (IC50 = 7 μM), cdk2/cyclin A (IC50 = 7 μM), cdk2/cyclin E (IC50 = 7 μM), cdk/p35 kinase (IC50 = 3 μM) and ERK1/MAP kinase at higher concentrations (IC50 = 25 μM)1. It also prevents NGF-mediated survival of neuronal cells2.
    References-Activity
    1. Veseley, J. et al. (1994) Eur. J. Biochem. 224, 771.
    2. Monaco, E.A. et al. (2004) Biochem. Pharmacol67, 1947.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to two weeks at 4°C or six months at -20°C.
    Our bioassay
    • Alomone Labs Olomoucine prevents NGF-mediated survival of PC-12 cells.
      Alomone Labs Olomoucine prevents NGF-mediated survival of PC-12 cells.
      Cells were grown in the absence of serum. The cells were not protected (dotted line) or protected (continuous line) from apoptosis with 100 ng/ml Native mouse NGF 2.5S protein (99%) (#N-240) and treated with different concentrations of Olomoucine (#O-300). Cell survival was measured after 4 days using the XTT method, calculated as a relative percentage of the control without Olomoucine and plotted against Olomoucine concentrations.
    References - Scientific background
    1. Vesely, J. et al. (1994) Eur. J. Biochem224, 771.
    2. Glab, N. et al. (1994) FEBS Lett353, 207.
    3. Abraham, R.T. (1995) Biol. Cell  83, 105.
    4. Schutte, B. et al. (1997) Exp. Cell Res236, 4.
    5. Meijer, L. et al. (1997) Eur. J. Biochem243, 527.
    6. Flament, S. (2000) Zygote 8, 3.
    7. Rossi, L.A. et al. (1998) Exp. Cell. Res245, 8.
    8. Yakisich, J.S. et al. (1998) Biochem. Biophys. Res. Commun243, 674.
    9. Wesierska-Gadek, J. et al. (2004) Pol. J. Pharmacol56, 635.
    10. Dobashi, Y. et al. (2000) J. Biol. Chem275, 12572.
    11. Iseki, H. et al. (1997) Surgery 122, 187.
    12. Monaco, E.A. et al. (2004) Biochem. Pharmacol67, 1947.
    13. Ohnuma, S. et al. (2001) Curr. Opin. Neurobiol11, 66.
    Scientific background

    Olomoucine is a cell-permeable purine protein kinase inhibitor, found to be highly specific for the cell-cycle regulating p34cdc2/cyclin B, p33cdk2/cyclin A and p33cdk2/cyclin E kinases, the brain p33cdk5/p35 kinase and the ERK1/2 MAP- kinase (IC50=7-25 µM).1 Olomoucine behaves as a competitive inhibitor for ATP and as a non-competitive inhibitor for histone H1 binding in CDKs kinases.1-5

    Olomoucine induces a dose-dependent inhibition of proliferation rate and the cell cycle progression in many human cancer cells in culture (EC50 = 40-90 µM). Olomoucine, at 1-100 µM, slowdown or arrest KB 3-1 cells in G1/S and G2/M phase and decreased the DNA synthesis of rat brain cortex.6-11

    Olomoucine also induces apoptosis in maturing cerebellar granule neurons,11 NGF induced neuronal differentiation of PC12 cells in vitro12 and in NE cells in vivo.13

    Last update: 11/04/2021

    Olomoucine (#O-300) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use

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    Scientific Background

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