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GSK2334470 is a potent and selective PDK1 (3-Phosphoinositide dependent protein kinase-1) inhibitor. GSK2334470 blocks the phosphorylation of known PDK1 substrates, but surprisingly find that the potency and kinetics of inhibition vary for different PDK1 targets. GSK2334470 subsequent activation of PDK1 substrates S6K1, SGK and RSK in HEK293, U87 and mouse embryonic fibroblast cell lines. GSK2334470 inhibited activation of an Akt1 mutant lacking the PH domain (pleckstrin homology domain) more potently than full-length Akt1, suggesting that GSK2334470 is more effective at inhibiting PDK1 substrates that are activated in the cytosol rather than at the plasma membrane. GSK2334470 also suppressed T-loop phosphorylation and activation of RSK2 (p90 ribosomal S6 kinase 2), another PDK1 target activated by the ERK (extracellular-signal-regulated kinase) pathway.
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Source | Oncogene (2014). Figure 2. GSK2334470 |
| Method | H&E stain | |
| Cell Lines | mice | |
| Concentrations | 2.5 μM | |
| Incubation Time | 7 days | |
| Results | It is noteworthy that while administration of PDKi did not inhibit development of localized melanomas (local application of 4-HT), it reduced metastasis burden in lymph nodes as quantitated by S100 stain |
| Molecular Weight | 462.59 |
| Formula | C25H34N8O |
| CAS Number | 1227911-45-6 |
| Solubility (25°C) | DMSO Ethanol |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Knight ZA. Biochem J. For a PDK1 inhibitor, the substrate matters.
| Related PDK1 Products |
|---|
| MP7
MP7 (PDK1 inhibitor) is a phosphoinositide-dependent kinase-1 (PDK1) inhibitor. |
| PDKtide
PDKtide is a biological active peptide. |
| PDK1-IN-RS2
PDK1-IN-RS2 is a mimic of peptide docking motif (PIFtide) and is a substrate-selective PDK1 inhibitor with a Kd of 9 μM. PDK1-IN-RS2 suppresses the activation of the downstream kinases S6K1 by PDK1. |
| PS47
PS47 is an inactive E-isomer of PS48. PS48 is an activator of PDK1. PS47 can be used as a negative control for PS48. |
| PS210
PS210 is a potent activator of PDK1 that binds to the PIF-pocket and allosterically modulates the active site of PDK1. |
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