Dual Akt and PDK1 inhibitor; binds the pleckstrin homology (PH) domain of Akt and PDK1 (Ki
values are 2.7 and 5.2 μ
M, respectively). Inhibits Akt phosphorylation and Akt downstream targets; also induces apoptosis in vitro
. Displays synergistic antitumor effect when combined with chemotherapeutics in breast cancer mouse models.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Molecular pharmacology and antitumor activity of PHT-427, a novel Akt/phosphatidylinositide-dependent protein kinase 1 pleckstrin homology domain inhibitor.
Meuillet EJ, Zuohe S, Lemos R et al.
Mol Cancer Ther.
In vitro and in vivo activity of novel small-molecule inhibitors targeting the pleckstrin homology domain of protein kinase B/AKT.
Moses et al.
Cancer Res., 2009;69:5073