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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.
Signaling Pathways | Target | TargetMol
Cat. No. Product name CAS No. Purity Chemical Structure
T16450 PDK1-IN-RS2 1643958-89-7 98%
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...
T12566 PS10 1564265-82-2 98%
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).
T15944 M77976 394237-61-7 99.80%
M77976
M77976 is a selective ATP-competitive inhibitor of pyruvate dehydrogenase kinase 4 (PDK4) with an inhibitory effect on PDK4, having an IC50 value of 648 μM. It i...
T22350 JX06 729-46-4 99.66%
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.
T16670 PS210 1221962-86-2 99.65%
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...
T12398 MP7 1001409-50-2 99.45%
MP7
MP7 (PDK1 inhibitor) is a inhibitor of phosphoinositide-dependent kinase-1 (PDK1).
T3895 Polyphyllin I 50773-41-6 99.36%
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 702674-56-4 99.34%
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...
T2466 Osu03012 742112-33-0 99.22%
Osu03012
Osu03012 (AR-12) is an orally bioavailable, small-molecule, celecoxib-derived inhibitor of phosphoinositide-dependent kinase-1 (PDK1) with potential antineoplast...
T17224 VER-246608 1684386-71-7 98.88%
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...
T6084 Rabusertib 911222-45-2 98.86%
Rabusertib
Rabusertib (IC-83) is an inhibitor of the cell cycle checkpoint kinase 1 (chk1) with potential chemopotentiating activity. Rabusertib has been used in trials stu...
T77685 6-Bromo-4-methoxypyrazolo[1,5-a]pyridine-3-carbonitrile 1207836-10-9 98.81%
6-Bromo-4-methoxypyrazolo[1,5-a]pyridine-3-carbonitrile
6-Bromo-4-methoxypyrazolo[1,5-a]pyridine-3-carbonitrile is a PDK1 inhibitor with anticancer and antiproliferative activity that can be used to study angiosarcoma...
T2348 GSK2334470 1227911-45-6 98.65%
GSK2334470
GSK2334470 is a novel PDK1 inhibitor (IC50: ~10 nM, in a cell-free assay), with no inhibitory at other close related AGC-kinases.
T24677 PS47 1180676-33-8 98.61%
PS47
PS-47(PS 47) is an inactive E-isomer of PS48. PS48 is an activator of PDK1.
T11765 KPLH1130 906669-07-6 98.43%
KPLH1130
KPLH1130, a specific pyruvate dehydrogenase kinase (PDK) inhibitor, enhances glucose tolerance in mice fed a high-fat diet (HFD). It effectively hinders macropha...
T1830 BX795 702675-74-9 98.32%
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...
T24741 RS1-PDK1 inhibitor 1643958-85-3 98.25%
RS1-PDK1 inhibitor
RS1-PDK1 inhibitor (RS 1) is a selective inhibitor of the protein kinase PDK1 that can be used to treat and prevent disease or disorders.
T3604 Sodium dichloroacetate 2156-56-1 98.17%
Sodium dichloroacetate
Sodium dichloroacetate (BCA) , a specific inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50 values of 183 and 80 μM for PDK2 and PDK4 respectively, has ...
T2420 PHT-427 1191951-57-1 98%
PHT-427
PHT-427 (CS-0223) 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).
T3163 PS 48 1180676-32-7 98%
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).
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...
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).
M77976
T15944
M77976 is a selective ATP-competitive inhibitor of pyruvate dehydrogenase kinase 4 (PDK4) with an inhibitory effect on PDK4, having an IC50 value of 648 μM. It i...
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.
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...
MP7
T12398
MP7 (PDK1 inhibitor) is a inhibitor of phosphoinositide-dependent kinase-1 (PDK1).
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...
Osu03012
T2466
Osu03012 (AR-12) is an orally bioavailable, small-molecule, celecoxib-derived inhibitor of phosphoinositide-dependent kinase-1 (PDK1) with potential antineoplast...
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...
Rabusertib
T6084
Rabusertib (IC-83) is an inhibitor of the cell cycle checkpoint kinase 1 (chk1) with potential chemopotentiating activity. Rabusertib has been used in trials stu...
6-Bromo-4-methoxypyrazolo[1,5-a]pyridine-3-carbonitrile
T77685
6-Bromo-4-methoxypyrazolo[1,5-a]pyridine-3-carbonitrile is a PDK1 inhibitor with anticancer and antiproliferative activity that can be used to study angiosarcoma...
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.
PS47
T24677
PS-47(PS 47) is an inactive E-isomer of PS48. PS48 is an activator of PDK1.
KPLH1130
T11765
KPLH1130, a specific pyruvate dehydrogenase kinase (PDK) inhibitor, enhances glucose tolerance in mice fed a high-fat diet (HFD). It effectively hinders macropha...
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...
RS1-PDK1 inhibitor
T24741
RS1-PDK1 inhibitor (RS 1) is a selective inhibitor of the protein kinase PDK1 that can be used to treat and prevent disease or disorders.
Sodium dichloroacetate
T3604
Sodium dichloroacetate (BCA) , a specific inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50 values of 183 and 80 μM for PDK2 and PDK4 respectively, has ...
PHT-427
T2420
PHT-427 (CS-0223) 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).
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).
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TargetMol