Potent 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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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.