Description General description A cell-permeable 2,6,9-trisubstituted purine analog that displays anti-mitotic as well as anti-tumor properties (GI50 = ~ 1.8 µM in the NCI 60-cell panel in vitro activity screen; potently inhibits the growth of KM12 colon cancer cells with a GI50 of 30 nM). Acts as a reversible and ATP-competitive inhibitor of Cdks (IC50 = 33 nM for Cdk1/cyclin B and Cdk2/cyclin A, 28 nM for Cdk2/cyclin E, and 20 nM for Cdk5/p35), and displays ~ 100-fold greater selectivity over a panel of kinases tested (IC50 ≥ 2.4 µM). Shown to induce cell differentiation by preferentially targeting the G2/M-phase and act intracellularly by inhibiting both Cdks and MAPKs. A cell-permeable 2,6,9-trisubstituted purine analog that displays anti-mitotic as well as anti-tumor properties (GI50 ~1.8 µM in the NCI 60-cell panel in vitro activity screen; potently inhibits the growth of KM12 colon cancer cells with a GI50 of 30 nM). Acts as a reversible and ATP-competitive inhibitor of Cdks (IC50 = 33 nM for Cdk1/cyclin B and Cdk2/cyclin A, 28 nM for Cdk2/cyclin E, and 20 nM for Cdk5/p35), and displays ~100-fold greater selectivity over a panel of kinases tested (IC50 ≥2.4 µM). Shown to induce cell differentiation by preferentially targeting the G2/M-phase and act intracellularly by inhibiting both Cdks and MAPKs. Packaging 5 mg in Plastic ampoule Biochem/physiol Actions Cell permeable: yes Primary Target Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, and Cdk5/p35 Product competes with ATP. Reversible: yes Target IC50: 33 nM for Cdk1/cyclin B and Cdk2/cyclin A, 28 nM for Cdk2/cyclin E, and 20 nM for Cdk5/p35 Packaging Packaged under inert gas Warning Toxicity: Irritant (B) Reconstitution Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C. Other Notes Breton, M.L., et al. 2003. Biochem. Biophys. Res. Commun.306, 880. Knockaert, M., et al. 2002.Oncogene21, 6413. Adachi, S., et al. 2001. Mol. Cell. Biol.21, 4929. Knockaert, M., et al. 2000. Chem. Biol.7, 411. Rosiana, G.R., et al. 1999. Proc. Natl. Acad. Sci. USA96, 4797. Chang, Y.T., et al. 1999. Chem. Biol.6, 361. Legal Information Sold under license of U.S. Patent 6,255,485 and 6,617,331.