OSU-03012 is a potent inhibitor of recombinant PDK-1 with IC50 of 5 μM and 2-fold increase in potency over OSU-02067.

BX795是一种高效、选择性的PDK1抑制剂，IC50为6 nM。它还有效抑制TBK1和IKKε，IC50值分别为6 nM和41 nM。BX795阻止S6K1、Akt、PKCδ和GSK3β的磷酸化，但对酶如PKA、PKC、c-Kit和GSK3β的选择性较低。此外，BX795调节自噬。

PHT-427 is dual inhibitor of Akt and PDPK1 with Ki of 2.7 μM and 5.2 μM, respectively, targeting PH domains of Akt and PDPK1.

GSK2334470 is a PDK1 inhibitor with IC50 of ~10 nM, with no activity at other close related AGC-kinases.

BX-912 is a selective inhibitor of 3-Phosphoinositide-dependent Kinase-1 (PDK1) with IC50 of 12 nM, showing > 10 fold selectivity over PKA, PKC, C-Kit, EGFR etc.