| Description |
A cell-permeable aminopyrimidine compound that acts as a potent, ATP-competitive and reversible multi-kinase inhibitor (IC 50 = 11 nM for PDK1 at ≤ 10 µM of ATP; IC 50 = 5 , 6, 19, 31, 41 and 111 nM for NUAK1, TBK1, MARK4, Aurora B, IKKε and PDK1 at 100 µM of ATP, respectively) and displays 50-fold greater selectivity over Cdk2/E, EGFR, GSK-3β, IR, c-Kit, PKA, PKC, TAK1 and VEGFR. Shown to block PDK1/Akt signaling, induce growth arrest and apoptosis in PC-3 and MDA-468 cells (IC 50 = 0.25 and 0.75 µM, respectively); further, inhibit phosphorylation (pSer 396 ), nuclear translocation and transcriptional activity of IRF3 and reduce IFN-β production in stimulated macrophages.
|
