PS47是PS48的非活性异构体，PS48作为PDK1激活剂，PS47用作PS48的阴性对照，用于验证药理学研究中的结果。

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 是一种有效、选择性高的共价 PDK 抑制剂，抑制 PDK1、PDK2 和 PDK3 的 IC50 值分别为 49 nM、101 nM 和 313 nM，JX06 通过与半胱氨酸残基共价结合抑制 PDK1 活性，具有抗肿瘤活性。

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

PS48是一种PDK1激活剂，其AC50为8 μM。

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。

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.

PDK4-IN-1 is an anthraquinone derivative and a potent and orally active pyruvate dehydrogenase kinase 4 (PDK4) inhibitor with an IC50 value of 84 nM. PDK4-IN-1 potently represses cellular transformation and cellular proliferation and induces apoptosis. PDK4-IN-1 has antidiabetic, anticancer and anti-allergic activity[1].

PDK1 inhibitor is a potent and selective inhibitor of PDK1 with potential as anticancer agent.