Stemcell, 72942, AKT Inhibitor VIII

AKT Inhibitor VIII is a cell-permeable, allosteric inhibitor of all three forms of the kinase AKT (AKT1, AKT2, and AKT3) with IC₅₀ values of 58, 210, and 2,200 nM, respectively (Lindsley et al.; Calleja et al.). It displays good selectivity against a panel of 70 other kinases with micromolar inhibition against some kinases, such as calcium/calmodulin-dependent protein kinase 1 and smooth muscle myosin light-chain kinase (Logie et al.).

CANCER RESEARCH

· Sensitizes prostate tumor and cervical carcinoma cells to apoptotic stimuli (DeFeo-Jones et al.).

· Blocks mitosis and inhibits migration of HeLa cells (Jo et al.).

METABOLISM

· Reduces insulin-dependent gene repression in liver cells leading to reduced insulin sensitivity (Logie et al.).