Olomoucine

A purine derivative that acts as a potent, reversible and selective inhibitor of p34^cdk1/cyclin B (IC₅₀ = 7 µM) and related kinases including p33^cdk2/cyclin A (IC₅₀ = 7 µM), p33^cdk2/cyclin E (IC₅₀ = 7 µM), p33^cdk5/p35 (IC₅₀ = 3 µM), and p44 MAP kinase (IC₅₀ = 25 µM). Acts by competing for the ATP binding domain of the kinase. Exhibits reduced sensitivity towards related kinases, p34^cdk4/cyclin D (IC₅₀ >1 mM), and p40^cdk6/cyclin D3 (IC₅₀ >250 µM). Does not significantly affect the activity of other protein kinases at 1 mM. Known to inhibit DNA synthesis in interleukin-2-stimulated T lymphocytes and trigger G₁ arrest similar to that observed in interleukin-2-deprived cells. Also used to synchronize cells in G₁. A 50 mM (5 mg/336 µl) solution of Olomoucine (Cat. No. 495624) in DMSOis also available.

Cell permeable: yes

Primary Target
p34^cdk1/cyclin B

Product competes with ATP.

Reversible: yes

Target IC₅₀: 7 µM, 7 µM, 7 µM, 3 µM, 25 µM against p34cdk1/cyclin B, p33cdk2/cyclin A, p33cdk2/cyclin E, p33cdk5/p35, and p44 MAP kinase, respectively

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). DMSO stock solutions are stable for up to 6 months at -20°C.

Abraham, R.T., et al. 1995. Biol. Cell 83, 105.
Mistelli, T., and Warren, G. 1995. J. Cell Sci. 108, 2715.
Glab, N., et al. 1994. FEBS Lett. 353, 207.
Veselý, J., et al. 1994. Eur. J. Biochem.224, 771.

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