| References: |
The compound (Akt-I-1,2) inhibited both Akt1 and Akt2 with IC50 values of 2.7 and 21 μM respectively. It does not inhibit AKT3. The compound is a reversible inhibitor, and exhibits a linear mixed-type inhibition against ATP and peptide substrate. In addition to inhibiting kinase activity of AKT1 and AKT2 isoforms, AKT-I-1,2 blocked the phosphorylation and activation of AKT1 and AKT2 by PDK1 (phosphoinositide-dependent kinase 1). The inhibitor was found to be cell-active and to block phosphorylation of Akt at Thr308 and Ser473, reduce the levels of active Akt in cells, block the phosphorylation of known Akt substrates and promote TRAIL (tumour-necrosis-factor-related apoptosis-inducing ligand)-induced apoptosis in LNCap prostate cancer cells. |
