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PDPK1 Products

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Catalog No. Product Name Information Product Use Citations Product Validations
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.
EMBO J, 2024, 10.1038/s44318-024-00244-9
Vet Microbiol, 2024, 290:109973
Cell Rep, 2023, 10.1016/j.celrep.2023.113352
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 and 2-fold increase in potency over OSU-02067.
J Med Virol, 2023, 95(7):e28957
Gut Microbes, 2023, 15(1):2180315
Aging (Albany NY), 2022, 14(20):8221-8242
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.
Nat Commun, 2024, 15(1):7181
Cell Commun Signal, 2024, 22(1):473
J Cancer, 2024, 15(5):1429-1441
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
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).
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. Indoprofen prevents muscle wasting in aged mice through activation of PDK1/AKT pathway.Indoprofen selectively increases 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.
EMBO J, 2024, 10.1038/s44318-024-00244-9
Vet Microbiol, 2024, 290:109973
Cell Rep, 2023, 10.1016/j.celrep.2023.113352
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 and 2-fold increase in potency over OSU-02067.
J Med Virol, 2023, 95(7):e28957
Gut Microbes, 2023, 15(1):2180315
Aging (Albany NY), 2022, 14(20):8221-8242
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.
Nat Commun, 2024, 15(1):7181
Cell Commun Signal, 2024, 22(1):473
J Cancer, 2024, 15(5):1429-1441
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
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).
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. Indoprofen prevents muscle wasting in aged mice through activation of PDK1/AKT pathway.Indoprofen selectively increases SMN2-luciferase reporter protein and endogenous SMN protein.

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