PDPK1

This gene encodes a serine/threonine protein kinase called phosphoinositide-dependent kinase 1 (PDPK1) which is integral to the function of the PI3-K/Akt signaling pathway. PDPK1 plays a central role in the transduction of signals from insulin by providing the activating phosphorylation to PKB/AKT1, thus propagating the signal to downstream targets controlling cell proliferation and survival, as well as glucose and amino acid uptake and storage. It also negatively regulates the TGF-β-induced signaling by: modulating the association of SMAD3 and SMAD7 with TGF-beta receptor, phosphorylating SMAD2, SMAD3, SMAD4 and SMAD7, preventing the nuclear translocation of SMAD3 and SMAD4 and the translocation of SMAD7 from the nucleus to the cytoplasm in response to TGF-beta. Activates the NF-κB pathway via phosphorylation of IKKB.

PI3K/Akt/mTOR

Aurora Kinase CDK Chk ROCK Antimetabolites APC Wee1 MPS1 Rho Myc DYRK BMI-1 eIF LIM kinase PFKFB RUNX Nur77 FOXM1 Choline kinase Haspin Kinase Mad2 p21 Cyclin CDK4/6 Cell Cycle Arrest

All (9)
PDPK1 Inhibitors (5)
PDPK1 Activators (4)
New PDPK1 Products

Cat.No.	Product Name	Information	Product Use Citations
S1106	OSU-03012 (AR-12)	OSU-03012 (AR-12) is a potent inhibitor of recombinant PDK-1(phosphoinositide-dependent kinase 1) with IC50 of 5 μM in a cell-free assay, showing a 2-fold increase in potency over OSU-02067.	Autophagy, 2025, 1-17. J Med Virol, 2023, 95(7):e28957 Gut Microbes, 2023, 15(1):2180315
S7087	GSK2334470	GSK2334470 is a novel PDK1 inhibitor with IC50 of ~10 nM in a cell-free assay, with no activity at other close related AGC-kinases.	Am J Physiol Renal Physiol, 2025, 328(3):F344-F359 Nat Commun, 2024, 15(1):7181 Cell Commun Signal, 2024, 22(1):473
S6504	BX517	BX517 is a potent and selective inhibitor of PDK1 that binds to the ATP binding pocket of the protein (IC50 = 6 nM).	Cancer Cell, 2022, S1535-6108(21)00662-0
S7586	PS-48	PS-48 is an allosteric activator of phosphoinositide-dependent protein kinase-1 (PDK1).	iScience, 2025, 28(8):113117 Cell Stem Cell, 2022, 29(8):1229-1245.e7
S3462	PS210	PS210 is a potent activator of PDK1 that binds to the PIF-pocket and allosterically modulates the active site of PDK1.
E2816	PS47	PS47 is an inactive E isomer of PS48, an activator of 3-Phosphoinositide-dependent protein kinase 1 (PDPK1).
S2272	Indoprofen	Indoprofen is a nonsteroidal anti-inflammatory drug (NSAID) and cyclooxygenase (COX) inhibitor. This compound prevents muscle wasting in aged mice through activation of the PDK1/AKT pathway. It selectively increases the SMN2-luciferase reporter protein and endogenous SMN protein.
S1274	BX-795	BX-795 is a potent and specific PDK1 inhibitor with IC50 of 6 nM, 140- and 1600-fold more selective for PDK1 than PKA and PKC in cell-free assays, respectively. Meanwhile, in comparison to GSK3β more than 100-fold selectivity observed for PDK1. BX-795 modulates autophagy via inhibiting ULK1. BX-795 also is a potent TBK1 inhibitor that blocks both TBK1 and IKKε with IC 50 values of 6 nM and 41 nM, respectively.	Cancer Res, 2025, 10.1158/0008-5472.CAN-25-1791 Cell Rep, 2025, 44(7):115972 EMBO J, 2024, 10.1038/s44318-024-00244-9
S1556	PHT-427	PHT-427 (CS-0223) is a dual Akt and PDPK1 inhibitor (high affinity binding for the PH domains of Akt and PDPK1) with K_i of 2.7 μM and 5.2 μM, respectively.	Exp Gerontol, 2023, 173:112091 Cancer Cell, 2022, S1535-6108(22)00312-9 Nucleic Acids Res, 2022, gkac179
S1106	OSU-03012 (AR-12)	OSU-03012 (AR-12) is a potent inhibitor of recombinant PDK-1(phosphoinositide-dependent kinase 1) with IC50 of 5 μM in a cell-free assay, showing a 2-fold increase in potency over OSU-02067.	Autophagy, 2025, 1-17. J Med Virol, 2023, 95(7):e28957 Gut Microbes, 2023, 15(1):2180315
S7087	GSK2334470	GSK2334470 is a novel PDK1 inhibitor with IC50 of ~10 nM in a cell-free assay, with no activity at other close related AGC-kinases.	Am J Physiol Renal Physiol, 2025, 328(3):F344-F359 Nat Commun, 2024, 15(1):7181 Cell Commun Signal, 2024, 22(1):473
S6504	BX517	BX517 is a potent and selective inhibitor of PDK1 that binds to the ATP binding pocket of the protein (IC50 = 6 nM).	Cancer Cell, 2022, S1535-6108(21)00662-0
S1274	BX-795	BX-795 is a potent and specific PDK1 inhibitor with IC50 of 6 nM, 140- and 1600-fold more selective for PDK1 than PKA and PKC in cell-free assays, respectively. Meanwhile, in comparison to GSK3β more than 100-fold selectivity observed for PDK1. BX-795 modulates autophagy via inhibiting ULK1. BX-795 also is a potent TBK1 inhibitor that blocks both TBK1 and IKKε with IC 50 values of 6 nM and 41 nM, respectively.	Cancer Res, 2025, 10.1158/0008-5472.CAN-25-1791 Cell Rep, 2025, 44(7):115972 EMBO J, 2024, 10.1038/s44318-024-00244-9
S1556	PHT-427	PHT-427 (CS-0223) is a dual Akt and PDPK1 inhibitor (high affinity binding for the PH domains of Akt and PDPK1) with K_i of 2.7 μM and 5.2 μM, respectively.	Exp Gerontol, 2023, 173:112091 Cancer Cell, 2022, S1535-6108(22)00312-9 Nucleic Acids Res, 2022, gkac179
S7586	PS-48	PS-48 is an allosteric activator of phosphoinositide-dependent protein kinase-1 (PDK1).	iScience, 2025, 28(8):113117 Cell Stem Cell, 2022, 29(8):1229-1245.e7
S3462	PS210	PS210 is a potent activator of PDK1 that binds to the PIF-pocket and allosterically modulates the active site of PDK1.
E2816	PS47	PS47 is an inactive E isomer of PS48, an activator of 3-Phosphoinositide-dependent protein kinase 1 (PDPK1).
S2272	Indoprofen	Indoprofen is a nonsteroidal anti-inflammatory drug (NSAID) and cyclooxygenase (COX) inhibitor. This compound prevents muscle wasting in aged mice through activation of the PDK1/AKT pathway. It selectively increases the SMN2-luciferase reporter protein and endogenous SMN protein.