BX-912 is a 3-Phosphoinositide-dependent Kinase-1 (PDK-1) inhibitor. BX 912 suppresses growth in a number of cell lines and also induces apoptosis. Cell lines with elevated levels of AKT are >30-fold more sensitive to PDK1 inhibition by BX-912. This compound is a competitive inhibitor of PDK1, indicating that it binds to the ATP-binding pocket to inhibit phosphorylation. BX-912 accomplishes this due to the fact that the aminopyrimidine backbone, which adopts a similar conformation to ATP in the active site of PDK1. BX-912 potently inhibits the growth of PC-3 cells in soft agar, displaying an IC50 of 320 nM.
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