Home PI3K/Akt/mTOR PDPK1

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.

Other PI3K/Akt/mTOR Related Inhibitors

PI3K mTOR Akt GSK-3 DNA-PK ATM/ATR PDK AMPK PTEN MELK
Cat.No. Product Name Information Product Use Citations Product Validations
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
Verified customer review of OSU-03012 (AR-12)
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
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
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
Verified customer review of BX-795
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
Verified customer review of GSK2334470
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 Ki 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
Verified customer review of PHT-427

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.