Tocris Bioscience™ AKT Inhibitor IV

AKT Inhibitor IV promotes hyperphosphorylation of Akt (Protein kinase B), decreases phosphorylation of Akt substrates, and inhibits FOXO1a nuclear export (IC50 = 625 nM in PTEN-null cells). AKT Inhibitor IV inhibits the proliferation of several cells lines (IC50 values are <1.25 μM, 320 - 670 nM and 340 nM for 786-O, HeLa and Jurkat cells, respectively). This compound also displays broad antiviral activity against negative-stranded RNA viruses; inhibits replication of parainfluenza virus 5 (PIV5) in HeLa cells (IC50 = 520 nM). In HeLa cells, AKT Inhibitor IV accumulates in mitochondria, disrupting morphology and increasing ROS production. At high concentrations (10 μM), AKT Inhibitor IV activates the unfolded protein response and apoptosis in HEK293T cells.

AKT Inhibitor IV is weakly fluorescent upon irradiation with UV light (excitation/emission maxima λ ∼ 388/460; quantum yield = 0.0016).