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Catalog No. Product Name Information Product Use Citations Product Validations
S0983 JX06 JX06 as a selective covalent inhibitor of PDK1 in cells. JX06 dose-dependently inhibits PDK1, PDK2 and PDK3 with IC50 0.049 μM, 0.101 μM and 0.313 μM, respectively.
Biochem Biophys Res Commun, 2021, 587:153-159
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.
Nat Commun, 2021, 12(1):4566
Aging (Albany NY), 2021, 13(13):17097-17117
Eur J Med Chem, 2021, 226:113895
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.
Cell Rep, 2022, 38(7):110373
Microbiol Spectr, 2022, e0219321
FASEB J, 2022, 36(2):e22171
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.
Nucleic Acids Res, 2022, gkac179
J Agric Food Chem, 2021, 10.1021/acs.jafc.1c02738
Mol Syst Biol, 2020, 16(2):e8664
S3233 Emetine hydrochloride Emetine hydrochloride (NSC 33669), a principal alkaloid extracted from the root of ipecac clinically used as an emetic and antiprotozoal drug, reduces HIFs (hypoxia-inducible factors; HIF-1α and HIF-2α), PDK1, RhoA, Rho-kinases (ROCK1 and ROCK2) and BRD4. Emetine hydrochloride inhibits cellular autophagy and has anti-malarial, anti-viral, anti-bacterial and anti-amoebic effect.
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
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.
Cell Rep, 2022, 38(11):110522
Nat Commun, 2021, 12(1):4566
PLoS Biol, 2021, 19(12):e3001483
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.
S3462 PS210 PS210 is a potent activator of PDK1 that binds to the PIF-pocket and allosterically modulates the active site of PDK1.
S7586 PS-48 PS-48 is an allosteric activator of phosphoinositide-dependent protein kinase-1 (PDK1).
S0983 JX06 JX06 as a selective covalent inhibitor of PDK1 in cells. JX06 dose-dependently inhibits PDK1, PDK2 and PDK3 with IC50 0.049 μM, 0.101 μM and 0.313 μM, respectively.
Biochem Biophys Res Commun, 2021, 587:153-159
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.
Nat Commun, 2021, 12(1):4566
Aging (Albany NY), 2021, 13(13):17097-17117
Eur J Med Chem, 2021, 226:113895
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.
Cell Rep, 2022, 38(7):110373
Microbiol Spectr, 2022, e0219321
FASEB J, 2022, 36(2):e22171
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.
Nucleic Acids Res, 2022, gkac179
J Agric Food Chem, 2021, 10.1021/acs.jafc.1c02738
Mol Syst Biol, 2020, 16(2):e8664
S3233 Emetine hydrochloride Emetine hydrochloride (NSC 33669), a principal alkaloid extracted from the root of ipecac clinically used as an emetic and antiprotozoal drug, reduces HIFs (hypoxia-inducible factors; HIF-1α and HIF-2α), PDK1, RhoA, Rho-kinases (ROCK1 and ROCK2) and BRD4. Emetine hydrochloride inhibits cellular autophagy and has anti-malarial, anti-viral, anti-bacterial and anti-amoebic effect.
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
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.
Cell Rep, 2022, 38(11):110522
Nat Commun, 2021, 12(1):4566
PLoS Biol, 2021, 19(12):e3001483
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.
S3462 PS210 PS210 is a potent activator of PDK1 that binds to the PIF-pocket and allosterically modulates the active site of PDK1.
S7586 PS-48 PS-48 is an allosteric activator of phosphoinositide-dependent protein kinase-1 (PDK1).
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