SYN-1005-M001
SYN-1005-M005
SYN-1005-M010
102991-202EA
292.15
USD
InStock
102991-202
102991-204
102991-294
Akt-I-1 ≥95%
Akt-I-1
The compound (Akt-I-1) inhibits only Akt1 (IC(50) 4.6 µM) and does not inhibit AKT2, or 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 isoform, AKT-I-1 blocked the phosphorylation and activation of AKT1 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.