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PDK

In the field of biochemistry, PDPK1 refers to the protein 3-phosphoinositide-dependent protein kinase-1, an enzyme which is encoded by the PDPK1 gene in humans. It is implicated in the development and progression of melanomas.PDPK1 is a master kinase, which is crucial for the activation of AKT/PKB and many other AGC kinases including PKC, S6K, SGK. An important role for PDPK1 is in the signalling pathways activated by several growth factors and hormones including insulin signaling.
Cat No. product name
T3163 PS 48 PS 48 has been shown to be a PKB Kinase (PDK1) activator (Kd: 10.3 μM). This compound selectively binds to the PIF-binding pocket of PKB Kinase (PDK1).
T1830 BX795 BX795 is an effective and selective PDK1 inhibitor (IC50: 6 nM), and its selectivity is 140- and 1600-fold for PDK1 over PKA and PKC in cell-free assays, respect...
T22350 JX06 JX06, a potent, selective and covalent PDK inhibitor, inhibits PDK1, PDK2 and PDK3 with IC50 of 49 nM, 101 nM and 313 nM respectively.
T17224 VER-246608 VER-246608 is an effective and ATP-competitive inhibitor of pyruvate dehydrogenase kinase (IC50s: 35 nM, 40 nM, 84 nM, and 91 nM for PDK-1, PDK-3, PDK-2, and PDK...
T12412L PDK4-IN-1 hydrochloride PDK4-IN-1 hydrochloride is an anthraquinone derivative and a potent and orally active inhibitor of pyruvate dehydrogenase kinase 4 (PDK4)(IC50 value of 84 nM)
T6084 Rabusertib Rabusertib is an inhibitor of the cell cycle checkpoint kinase 2 (chk2) with potential chemopotentiating activity. Rabusertib has been used in trials studying th...
T3895 Polyphyllin I Polyphyllin D induces apoptosis via the mitochondrial apoptotic pathway as evidenced by decreased Bcl-2 expression levels, disruption of MMP and increased Bax, c...
T1837 BX-912 BX-912 is a specific inhibitor of 3-Phosphoinositide-dependent Kinase-1 (PDK1, IC50: 12 nM). The selectivity of BX-912 is more 10 fold than C-Kit, EGFR, PKA, PKC...
T24677 PS47 PS-47 is an inactive E-isomer of PS48. PS48 is an activator of PDK1.
T2420 PHT-427 PHT-427 is a dual Akt (Ki: 2.7 μM) and PDPK1 (Ki: 5.2 μM) inhibitor (high-affinity binding for the PH domains of Akt and PDPK1).
T11765 KPLH1130 KPLH1130 improves glucose tolerance in HFD-fed mice. KPLH1130 is a specific pyruvate dehydrogenase kinase (PDK) inhibitor, blocks macrophage polarization and att...
T0809 Dicoumarol Dicumarol is a hydroxycoumarin originally isolated from molding sweet-clover hay, with anticoagulant and vitamin K depletion activities. Dicumarol is a competiti...
T3604 Sodium dichloroacetate Dichloroacetate, a specific inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50 values of 183 and 80 μM for PDK2 and PDK4 respectively, has been shown to ...
T2348 GSK2334470 GSK2334470 is a novel PDK1 inhibitor (IC50: ~10 nM, in a cell-free assay), with no inhibitory at other close related AGC-kinases.
T2466 Osu03012 AR-12 is an orally bioavailable, small-molecule, celecoxib-derived inhibitor of phosphoinositide-dependent kinase-1 (PDK1) with potential antineoplastic activity...
TMA2474 δ-Tocotrienol Delta-tocotrienol is a potential angiogenic inhibitor, it (2.5-5 microM) can significantly suppress human colorectal adenocarcinoma cells (DLD-1-CM) -induced tub...
T12566 PS10 PS10 is a ATP-competitive inhibitor of pan-PDK(PDK2, PDK4, PDK1, and PDK3 with IC50 of 0.8 μM, 0.76 μM, 2.1 μM and 21.3 μM , respectively).
T12398 MP7 MP7 is a inhibitor of phosphoinositide-dependent kinase-1 (PDK1).
T4046 BX517 BX-517 is a potent and selective inhibitor of PDK1.
T16450 PDK1-IN-RS2 PDK1-IN-RS2 inhibits the activation of the downstream kinases S6K1 by PDK1. PDK1-IN-RS2 is a mimic of the peptide docking motif (PIFtide) and is a substrate-sele...
T16670 PS210 PS210 is inactive against other protein kinases, including PDK1 downstream signaling components such as S6K, PKB/Akt, or GSK3. PS210 is a potent and selective PD...
PS 48
T3163
PS 48 has been shown to be a PKB Kinase (PDK1) activator (Kd: 10.3 μM). This compound selectively binds to the PIF-binding pocket of PKB Kinase (PDK1).
BX795
T1830
BX795 is an effective and selective PDK1 inhibitor (IC50: 6 nM), and its selectivity is 140- and 1600-fold for PDK1 over PKA and PKC in cell-free assays, respect...
JX06
T22350
JX06, a potent, selective and covalent PDK inhibitor, inhibits PDK1, PDK2 and PDK3 with IC50 of 49 nM, 101 nM and 313 nM respectively.
VER-246608
T17224
VER-246608 is an effective and ATP-competitive inhibitor of pyruvate dehydrogenase kinase (IC50s: 35 nM, 40 nM, 84 nM, and 91 nM for PDK-1, PDK-3, PDK-2, and PDK...
PDK4-IN-1 hydrochloride
T12412L
PDK4-IN-1 hydrochloride is an anthraquinone derivative and a potent and orally active inhibitor of pyruvate dehydrogenase kinase 4 (PDK4)(IC50 value of 84 nM)
Rabusertib
T6084
Rabusertib is an inhibitor of the cell cycle checkpoint kinase 2 (chk2) with potential chemopotentiating activity. Rabusertib has been used in trials studying th...
Polyphyllin I
T3895
Polyphyllin D induces apoptosis via the mitochondrial apoptotic pathway as evidenced by decreased Bcl-2 expression levels, disruption of MMP and increased Bax, c...
BX-912
T1837
BX-912 is a specific inhibitor of 3-Phosphoinositide-dependent Kinase-1 (PDK1, IC50: 12 nM). The selectivity of BX-912 is more 10 fold than C-Kit, EGFR, PKA, PKC...
PS47
T24677
PS-47 is an inactive E-isomer of PS48. PS48 is an activator of PDK1.
PHT-427
T2420
PHT-427 is a dual Akt (Ki: 2.7 μM) and PDPK1 (Ki: 5.2 μM) inhibitor (high-affinity binding for the PH domains of Akt and PDPK1).
KPLH1130
T11765
KPLH1130 improves glucose tolerance in HFD-fed mice. KPLH1130 is a specific pyruvate dehydrogenase kinase (PDK) inhibitor, blocks macrophage polarization and att...
Dicoumarol
T0809
Dicumarol is a hydroxycoumarin originally isolated from molding sweet-clover hay, with anticoagulant and vitamin K depletion activities. Dicumarol is a competiti...
Sodium dichloroacetate
T3604
Dichloroacetate, a specific inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50 values of 183 and 80 μM for PDK2 and PDK4 respectively, has been shown to...
GSK2334470
T2348
GSK2334470 is a novel PDK1 inhibitor (IC50: ~10 nM, in a cell-free assay), with no inhibitory at other close related AGC-kinases.
Osu03012
T2466
AR-12 is an orally bioavailable, small-molecule, celecoxib-derived inhibitor of phosphoinositide-dependent kinase-1 (PDK1) with potential antineoplastic activity...
δ-Tocotrienol
TMA2474
Delta-tocotrienol is a potential angiogenic inhibitor, it (2.5-5 microM) can significantly suppress human colorectal adenocarcinoma cells (DLD-1-CM) -induced tub...
PS10
T12566
PS10 is a ATP-competitive inhibitor of pan-PDK(PDK2, PDK4, PDK1, and PDK3 with IC50 of 0.8 μM, 0.76 μM, 2.1 μM and 21.3 μM , respectively).
MP7
T12398
MP7 is a inhibitor of phosphoinositide-dependent kinase-1 (PDK1).
BX517
T4046
BX-517 is a potent and selective inhibitor of PDK1.
PDK1-IN-RS2
T16450
PDK1-IN-RS2 inhibits the activation of the downstream kinases S6K1 by PDK1. PDK1-IN-RS2 is a mimic of the peptide docking motif (PIFtide) and is a substrate-sele...
PS210
T16670
PS210 is inactive against other protein kinases, including PDK1 downstream signaling components such as S6K, PKB/Akt, or GSK3. PS210 is a potent and selective PD...