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Beschreibung

A cell-permeable purine analog that displays anti-proliferative properties and acts as a potent and ATP-competitive inhibitor of Cdk1/cyclin B and Cdk2/cyclin A3 (IC50 = 9.5 nM and 5.4 nM, respectively). Displays greater selectivity for Cdk's over other kinases tested (IC50 = 30 nM, 600 nM, 800 nM, 900 nM, and 1.6 µ,M for Cdk2/A, ROCKII, PDK1, DYRK1A, and Cdk4/D1, respectively). Shown to inhibit human MCF-7 breast carcinoma cell growth (GI50 of 8 µ,M)., A cell-permeable 2,6-disubstituted purine compound that displays antiproliferative properties. Acts as a potent and ATP-competitive inhibitor of Cdk1/cyclin B and Cdk2/cyclin A3 (IC50 = 9.5 nM and 5.4 nM). Displays greater selectivity for Cdk1/2 over other kinases tested (IC50 = 600 nM, 800 nM, 900 nM and 1.6 µ,M for ROCKII, PDK1, DYRK1A and Cdk4/D1, respectively). Shown to inhibit human MCF-7 breast carcinoma cell growth with a GI50 of 8 µ,M.