PDK
シグナル伝達経路
研究分野
阻害剤の選択性比較
| カタログ番号 | 製品カタログ | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | アルコール | ||
| S1106 | OSU-03012 (AR-12) | <1 mg/mL | 11 mg/mL | <1 mg/mL |
| S1274 | BX-795 | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S1556 | PHT-427 | <1 mg/mL | 82 mg/mL | 60 mg/mL |
| S7087 | GSK2334470 | <1 mg/mL | 90 mg/mL | 90 mg/mL |
| S3233 | Emetine hydrochloride | -1 mg/mL | 100 mg/mL | -1 mg/mL |
| S6504 | BX517 | <1 mg/mL | 56 mg/mL | <1 mg/mL |
| S0983 | JX06 | <1 mg/mL | 65 mg/mL | <1 mg/mL |
| S3462 | PS210 | <1 mg/mL | 76 mg/mL | ''76 mg/mL |
| S7586 | PS-48 | <1 mg/mL | 57 mg/mL | '''57 mg/mL |
| S2272 | Indoprofen | <1 mg/mL | 52 mg/mL | <1 mg/mL |
亜型選択性的な製品
PDK製品
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| 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-795BX-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. |
Induction of basal p62 Ser403 phosphorylation in ULK1/2-deficient MEF was suppressed by BX-795, an inhibitor of TBK1. WT ( Ulk1 +/+/Ulk2 +/+) and Ulk1 -/- /Ulk2 -/-(KO) MEF were treated with NaCl/Pi (Con) or 10 uM BX-795 for 6 h, and subjected to immunoblotting with indicated antibodies.
|
|
| S1556 |
PHT-427PHT-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. |
The inhibition of PI3K/Akt pathway is involved in ATG-induced FOXO3a dephosphorylation in PDGF-BB-activated HSCs. Serum-starved LX-2 human HSCs were pretreated with or without DMSO (vehicle) or ATG (0.5 uM) for 4 h, in the absence or presence of PI3K inhibitor LY294002 (20 uM) or Akt inhibitor PHT-427 (20 uM), and then incubated with or without 50 ng/ml PDGF-BB for 4 h. After treatment, aliquots of whole cell lysates were collected and subjected to Western blotting analysis. The experiments were repeated three times with similar results and a representative blot was shown for each protein. Total protein levels of Akt and FOXO3a served as internal controls.
|
|
| 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.
|
|
| S3233 |
Emetine hydrochlorideEmetine 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 |
BX517BX517 is a potent and selective inhibitor of PDK1 that binds to the ATP binding pocket of the protein (IC50 = 6 nM). |
||
| S0983 |
JX06JX06 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. |
||
| S3462 |
PS210PS210 is a potent activator of PDK1 that binds to the PIF-pocket and allosterically modulates the active site of PDK1. |
||
| S7586 |
PS-48PS-48 is an allosteric activator of phosphoinositide-dependent protein kinase-1 (PDK1). |
||
| S2272 |
IndoprofenIndoprofen 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. |
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| 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-795BX-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. |
Induction of basal p62 Ser403 phosphorylation in ULK1/2-deficient MEF was suppressed by BX-795, an inhibitor of TBK1. WT ( Ulk1 +/+/Ulk2 +/+) and Ulk1 -/- /Ulk2 -/-(KO) MEF were treated with NaCl/Pi (Con) or 10 uM BX-795 for 6 h, and subjected to immunoblotting with indicated antibodies.
|
|
| S1556 |
PHT-427PHT-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. |
The inhibition of PI3K/Akt pathway is involved in ATG-induced FOXO3a dephosphorylation in PDGF-BB-activated HSCs. Serum-starved LX-2 human HSCs were pretreated with or without DMSO (vehicle) or ATG (0.5 uM) for 4 h, in the absence or presence of PI3K inhibitor LY294002 (20 uM) or Akt inhibitor PHT-427 (20 uM), and then incubated with or without 50 ng/ml PDGF-BB for 4 h. After treatment, aliquots of whole cell lysates were collected and subjected to Western blotting analysis. The experiments were repeated three times with similar results and a representative blot was shown for each protein. Total protein levels of Akt and FOXO3a served as internal controls.
|
|
| 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.
|
|
| S3233 |
Emetine hydrochlorideEmetine 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 |
BX517BX517 is a potent and selective inhibitor of PDK1 that binds to the ATP binding pocket of the protein (IC50 = 6 nM). |
||
| S0983 |
JX06JX06 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. |
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S3462 |
PS210PS210 is a potent activator of PDK1 that binds to the PIF-pocket and allosterically modulates the active site of PDK1. |
||
| S7586 |
PS-48PS-48 is an allosteric activator of phosphoinositide-dependent protein kinase-1 (PDK1). |
||
| S2272 |
IndoprofenIndoprofen 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. |
