Aminopurvalanol A is 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) Aminopurvalanol A acts as a reversible and ATP-competitive inhibitor of Cdks (IC50 = 33 nM for cdc2 (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). Aminopurvalanol A has been shown to induce cell differentiation by preferentially targeting the G2/M-phase and act intracellularly by inhibiting both Cdks and MAPKs.
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