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

JX06 is a selective covalent PDK1 inhibitor with IC50 values of 49, 101 and 313nM for PDK-1, PDK-2 and PDK-3, respectively.

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.

PS-210 is a selective activator of PDK1 activator. It acts by binding to the PIF-pocket allosteric docking site.

PDK-4 Inhibitor compound 8c HCl is an allosteric PDK-4 inhibitor with IC50 value of 84nM.

PS48 is a phosphoinositide-dependent protein kinase-1 (PDK1) activator with Kd value of 10.3 μM and binds exclusively to the PIF-binding pocket of PDK1, distinct from the ATP binding site.

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

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.

BX795 is a potent and selective dual inhibitor of TBK1/PDK1 with IC50s of 2 nM/6 nM respectively, also inhibit Aurora B and IκB kinase ε (IKKε).