3-Phosphoinositide-dependent protein kinase 1 (PDK1) is a serine-threonine kinase that phosphorylates and activates a range of other kinases, including protein kinase (PK)B, PKA, and certain isoforms of PKC. BX-912 is a potent, ATP-competitive inhibitor of PDK1 (IC50 = 26 nM). It less effectively inhibits a panel of related serine-threonine kinases. BX-912 has been used to evaluate the role of PDK1 in kinase activation and cell survival.