BX-912 is a potent inhibitor of PDK1 (3-Phosphoinositide dependent protein kinase-1). The IC50 values for direct inhibition of kinase activity or inhibition in a cell based assay are 26 nM and 12 nM, respectively. BX-912 inhibits the growth of PC-3 tumor cells grown on soft agar more potently than cells grown on plastic (IC50 = 320 nM vs. 5.5 mM, respectively).