2-(2-Hydroxyethylamino)-6-benzylamino-9-methylpurine

White solid. A purine derivative that acts as a potent 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. Purity: ≥98% by TLC. CAS 101622-51-9.

Ref.: 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.