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A purine derivative that acts as a potent, reversible and selective inhibitor of p34cdk1/cyclin B and related kinases.
DMSO: soluble
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.
A purine derivative that acts as a potent, reversible, and selective inhibitor of p34cdc2/cyclin B (IC₅₀ = 7 µM) and related kinases, including p33cdk2/cyclin A (IC₅₀ = 7 µM), p33cdk2/cyclin E (IC₅₀ = 7 µM), p33cdk5/p35 (IC₅₀ = 3 µM), and p44MAPK (IC₅₀ = 25 µM). Acts by competing for the ATP binding domain of the kinase. Exhibits reduced sensitivity towards related kinases, p34ᶜᵈᵏ⁴/cyclin D1 (IC₅₀ >1000 µM) and p40cdk6/cyclin D3 (IC₅₀ >250 µM). Does not significantly affect the activity of other protein kinases even at 1 mM concentrations. Known to inhibit DNA synthesis in interleukin-2 stimulated T lymphocytes and triggers G₁ arrest similar to that observed in interleukin-2 deprived cells. Also used to synchronize cells in G₁.
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
Following reconstitution, aliquot and freeze (-20°C). DMSO stock solutions are stable for up to 6 months at -20°C.
Toxicity: Standard Handling (A)
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