Chemical Name: 1,3-Dihydro-1-[1-[[4-(6-phenyl-1H-imidazo[4,5-g]quinoxalin-7-yl)phenyl]methyl]-4-piperidinyl]-2H-benzimidazol-2-one
Biological ActivityPotent and selective dual Akt1 and 2 inhibitor (IC50 values are 50 and 210 nM, respectively). Selective for Akt1 and 2 over a panel of other tyrosine and serine/threonine kinases. Sensitizes LnCaP cells to TRAIL (TNF-related apoptosis-inducing ligand) induced apoptosis. Active in vivo.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
The selectivity of protein kinase inhibitors: a further update.
Bain et al.
Tumor cell sensitization to apoptotic stimuli by selective inhibition of specific Akt/PKB family members.
DeFeo-Jones D et al.
Mol.Cancer Ther., 2005;4:271
Identification and characterization of pleckstrin-homology-domain-dependent and isoenzyme-specific Akt inhibitors.
Barnett et al.
Biochem. J., 2005;385:399
Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors.
Lindsley et al.
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Human osteosarcoma cells were incubated with 10 μM Akti-1/2 for 30 min prior to treatment with 10 μM LPA to estimate COX-2 expression using Western blot analysis. Akti-1/2 abolished LPA-induced COX-2 expression.
MG-63 cells were incubated with PD169316 (25 μM), LY294002 (10 μM) or Akt-1/2 (5 μM Akt-I) for 30 min prior to 15d-PGJ2 treatment (20 μM) for 1 h to follow pAkt expression using Western blot. Akt-1/2 completely blocked 15d-PGJ2-induced Akt phosphorylation in MG-63 cells.