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PI3K/Akt/mTOR signaling PDK

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
TMA2474 Delta-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...
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...
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.
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...
T0809 Dicumarol Dicumarol is a hydroxycoumarin originally isolated from molding sweet-clover hay, with anticoagulant and vitamin K depletion activities. Dicumarol is a comp...
T1837 BX912 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...
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...
T2466 Osu03012 AR-12 is an orally bioavailable, small-molecule, celecoxib-derived inhibitor of phosphoinositide-dependent kinase-1 (PDK1) with potential antineoplastic activity...
T4046 BX517 BX-517 is a potent and selective inhibitor of PDK1.
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.
T12398 MP7 MP7 is a inhibitor of phosphoinositide-dependent kinase-1 (PDK1).
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).
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...
T11765 KPLH1130 KPLH1130 improves glucose tolerance in HFD-fed mice. KPLH1130 is a specific pyruvate dehydrogenase kinase (PDK) inhibitor, blocks macrophage polarization and at...
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...
T2420 PHT427 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).
Delta-Tocotrienol
TMA2474CAS 25612-59-3
Delta-tocotrienol is a potential angiogenic inhibitor, it (2.5-5 microM) can significantly suppress human colorectal adenocarcinoma cells (DLD-1-CM) -induced tub...
Rabusertib
T6084CAS 911222-45-2
Rabusertib is an inhibitor of the cell cycle checkpoint kinase 2 (chk2) with potential chemopotentiating activity. Rabusertib has been used in trials studying th...
GSK2334470
T2348CAS 1227911-45-6
GSK2334470 is a novel PDK1 inhibitor (IC50: ~10 nM, in a cell-free assay), with no inhibitory at other close related AGC-kinases.
Sodium Dichloroacetate
T3604CAS 2156-56-1
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...
Dicumarol
T0809CAS 66-76-2
Dicumarol is a hydroxycoumarin originally isolated from molding sweet-clover hay, with anticoagulant and vitamin K depletion activities. Dicumarol is a comp...
BX912
T1837CAS 702674-56-4
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...
BX795
T1830CAS 702675-74-9
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...
Osu03012
T2466CAS 742112-33-0
AR-12 is an orally bioavailable, small-molecule, celecoxib-derived inhibitor of phosphoinositide-dependent kinase-1 (PDK1) with potential antineoplastic activity...
BX517
T4046CAS 850717-64-5
BX-517 is a potent and selective inhibitor of PDK1.
JX06
T22350CAS 729-46-4
JX06, a potent, selective and covalent PDK inhibitor, inhibits PDK1, PDK2 and PDK3 with IC50 of 49 nM, 101 nM and 313 nM respectively.
MP7
T12398CAS 1001409-50-2
MP7 is a inhibitor of phosphoinositide-dependent kinase-1 (PDK1).
PS10
T12566CAS 1564265-82-2
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).
PDK1-IN-RS2
T16450CAS 1643958-89-7
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
T16670CAS 1221962-86-2
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...
KPLH1130
T11765CAS 906669-07-6
KPLH1130 improves glucose tolerance in HFD-fed mice. KPLH1130 is a specific pyruvate dehydrogenase kinase (PDK) inhibitor, blocks macrophage polarization and at...
VER-246608
T17224CAS 1684386-71-7
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...
PHT427
T2420CAS 1191951-57-1
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).