Olomoucine

貨號 Cat. No.
O-300
規格 Size
10 x 0.1 mg 1mg 5x1mg

Description

Olomoucine


A Cyclin Dependent Kinase (CDK) Inhibitor











Product#: O-300

























Sizes:
10 x 0.1 mg
1 mg
5 x 1 mg
 
 
 





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 mM).1








M.W.: 298.35










CAS No.: [1-1622-51-9]












Structure:
 








 










Purity: >99%












Bioassay:
Olomoucine (#O-300) prevents NGF-mediated survival of PC12 cells.










PC12 cells were grown in the absence of serum.  The cells were not protected (fragmented line) or protected from apoptosis with 100 ng/ml mNGF 2.5S (#N-240, continuous line) and treated with different concentrations of Olomoucine.  The survival of the cells after 4 days was measured using XTT method, calculated as a relative percentage of the control without Olomoucine and plotted against Olomoucine concentrations. 







 









References:


























































1.



Vesely, J. et al. (1994) Eur. J. Biochem. 224, 771.



2.


Glab, N. et al. (1994) FEBS Lett. 353, 207.

3.


Abraham, R.T. (1995) Biol. Cell  83, 105.

4.


Schutte, B. et al. (1997) Exp. Cell Res. 236, 4.

5.


Meijer, L. et al. (1997) Eur. J. Biochem. 243, 527.

6.


Flament, S. (2000) Zygote 8, 3.

7.


Rossi, L.A. et al. (1998) Exp. Cell. Res. 245, 8.

8.


Yakisich, J.S. et al. (1998) Biochem. Biophys. Res. Commun. 243, 674.

9.


Wesierska-Gadek, J. et al. (2004) Pol. J. Pharmacol. 56, 635.

10.



Dobashi, Y. et al. (2000) J. Biol. Chem. 275, 12572.



11.


Iseki, H. et al. (1997) Surgery 122, 187.

12.



Monaco, E.A. et al. (2004) Biochem. Pharmacol. 67, 1947.



13.



Ohnuma, S. et al. (2001) Curr. Opin. Neurobiol. 11, 66.




OlomoucineOlomoucine 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=40-90mM). Olomoucine, at 1-100 mM, 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


 


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