PDK
Signaling Pathway Map
Research Area
Inhibitory Selectivity
PDK Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| 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. |
Serum-deprived HEK293-AT1A cells were pretreated with PD98059 (20 uM; 1 h) or OSU03012 (10 uM; 6 h) prior to 5 min stimulation with AngII (100 nm) or SII (50 uM). A, abundance of phospho-Akt T308 in whole cell detergent lysates. Representative phospho-Akt and total Akt immunoblots are shown above a bar graph depicting the mean ?S.E. of three biological replicates.
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| S1274 |
BX-795BX795 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. |
(A) Washed human platelets were untreated or pretreated with the PDK1 inhibitor BX-795 (1 μM) for 5 min, and this was followed by stimulation with 2-methylthio-ADP (2MeSADP) (50 nM) under stirring for 5 min. Western blots were then probed for phosphorylated Akt (Thr308), Akt (Ser473), glycogen synthase kinase 3b (GSK3b) (Ser9), mitogen-activated protein kinase kinase 1/2 (MEK1/2) (Ser217/221), extracellular signal-regulated kinase 1/2 (ERK1/2) (Thr202/Tyr204), and cytosolic phospholipase A2 (cPLA2) (Ser505). The western blots shown are representative of three independent experiments.
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| S1275 |
BX-912BX912 is a potent and specific PDK1 inhibitor with IC50 of 12 nM, 9- and 105- fold greater selectivity for PDK1 than PKA and PKC in cell-free assays, respectively. In comparison to GSK3β, selectivity for PDK1 is 600-fold. |
Inhibition of PDK1 or MEK1/2 abrogated Erk1/2 phosphorylation. Cells were treated with pharmacological inhibitors of Raf (AZ 628, PLX4032), MEK1/2 (AZD6244), p90RSK (BI-D1870), PI3Kδ (X-370), PDK1 (BX-912), Akt (MK-2206), mTOR (AZD8055) or mTORC1 (Rapamycin) respectively and indicated proteins were detected. |
|
| S1556 |
PHT-427PHT-427 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. |
Luciferase reporter assays. 32D/BCR-ABL cells transfected with the reporter construct containing 1548 bp of the Atf5 promoter were treated with either DMSO, imatinib (5 μM for 24 hours), LY294002 (20 μM for 48 hours), PHT-427 (20 μM for 24 hours), or JAK inhibitor I (10 μM for 24 hours). Error bars represent SD. |
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| S7087 |
GSK2334470GSK2334470 is a novel PDK1 inhibitor with IC50 of ~10 nM in a cell-free assay, with no activity at other close related AGC-kinases. |
(G) Effect of the PDK1 inhibitor GSK2334470 on MYC and P70 phosphorylation in CNE2/235 cell line by immunoblotting analysis. (H) Sensitivity to GSK2334470 in CNE2/235 cells after treatment with GSK2334470 for 5 d using the MTT assay. (I) Inhibitory effect of GSK2334470 in combination with BEZ235 on cell proliferation in CNE2/235 cells using the MTT assay. (J) IC50 values of BEZ235 with or without GSK2334470 in CNE2 and CNE2/235 cell lines. The data shown are representative of 3 individual experiments.
|
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| 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. |
Serum-deprived HEK293-AT1A cells were pretreated with PD98059 (20 uM; 1 h) or OSU03012 (10 uM; 6 h) prior to 5 min stimulation with AngII (100 nm) or SII (50 uM). A, abundance of phospho-Akt T308 in whole cell detergent lysates. Representative phospho-Akt and total Akt immunoblots are shown above a bar graph depicting the mean ?S.E. of three biological replicates.
|
|
| S1274 |
BX-795BX795 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. |
(A) Washed human platelets were untreated or pretreated with the PDK1 inhibitor BX-795 (1 μM) for 5 min, and this was followed by stimulation with 2-methylthio-ADP (2MeSADP) (50 nM) under stirring for 5 min. Western blots were then probed for phosphorylated Akt (Thr308), Akt (Ser473), glycogen synthase kinase 3b (GSK3b) (Ser9), mitogen-activated protein kinase kinase 1/2 (MEK1/2) (Ser217/221), extracellular signal-regulated kinase 1/2 (ERK1/2) (Thr202/Tyr204), and cytosolic phospholipase A2 (cPLA2) (Ser505). The western blots shown are representative of three independent experiments.
|
|
| S1275 |
BX-912BX912 is a potent and specific PDK1 inhibitor with IC50 of 12 nM, 9- and 105- fold greater selectivity for PDK1 than PKA and PKC in cell-free assays, respectively. In comparison to GSK3β, selectivity for PDK1 is 600-fold. |
Inhibition of PDK1 or MEK1/2 abrogated Erk1/2 phosphorylation. Cells were treated with pharmacological inhibitors of Raf (AZ 628, PLX4032), MEK1/2 (AZD6244), p90RSK (BI-D1870), PI3Kδ (X-370), PDK1 (BX-912), Akt (MK-2206), mTOR (AZD8055) or mTORC1 (Rapamycin) respectively and indicated proteins were detected. |
|
| S1556 |
PHT-427PHT-427 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. |
Luciferase reporter assays. 32D/BCR-ABL cells transfected with the reporter construct containing 1548 bp of the Atf5 promoter were treated with either DMSO, imatinib (5 μM for 24 hours), LY294002 (20 μM for 48 hours), PHT-427 (20 μM for 24 hours), or JAK inhibitor I (10 μM for 24 hours). Error bars represent SD. |
|
| S7087 |
GSK2334470GSK2334470 is a novel PDK1 inhibitor with IC50 of ~10 nM in a cell-free assay, with no activity at other close related AGC-kinases. |
(G) Effect of the PDK1 inhibitor GSK2334470 on MYC and P70 phosphorylation in CNE2/235 cell line by immunoblotting analysis. (H) Sensitivity to GSK2334470 in CNE2/235 cells after treatment with GSK2334470 for 5 d using the MTT assay. (I) Inhibitory effect of GSK2334470 in combination with BEZ235 on cell proliferation in CNE2/235 cells using the MTT assay. (J) IC50 values of BEZ235 with or without GSK2334470 in CNE2 and CNE2/235 cell lines. The data shown are representative of 3 individual experiments.
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