PS-210 |
| Katalog-Nr.GC48003 |
PS-210 ist ein potenter und selektiver PDK1-Aktivator mit einem Kd von 3 μM und zielt auf die PIF-Bindungstasche von PDK1 ab. PS-210 ist gegenüber anderen Proteinkinasen inaktiv, einschließlich nachgeschalteter PDK1-Signalkomponenten wie S6K, PKB/Akt oder GSK3. In Zellen wirkt das Prodrug von PS-210 (PS423) als substratselektiver Inhibitor von PDK1, indem es die Phosphorylierung und Aktivierung von S6K hemmt.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1221962-86-2
Sample solution is provided at 25 µL, 10mM.
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PS-210 is an activator of phosphoinositide-dependent protein kinase 1 (PDK1) that increases its thermal stability.1,2 It is selective for PDK-1 over a panel of 120 kinases at 10 µM.1 PS-210 (2 µM) increases the activity of wild-type PDK1 but not PDK1 with a mutation in the PIF-binding pocket.
1.Busschots, K., Lopez-Garcia, L.A., Lammi, C., et al.Substrate-selective inhibition of protein kinase PDK1 by small compounds that bind to the PIF-pocket allosteric docking siteChem. Biol.19(9)1152-1163(2012) 2.Wilhem, A., Lopez-Garcia, L.A., Busschots, K., et al.2-(3-Oxo-1,3-diphenylpropyl)malonic acids as potent allosteric ligands of the PIF pocket of phosphoinositide-dependent kinase-1: Development and prodrug conceptJ. Med. Chem.55(22)9817-9830(2012)
Average Rating: 5 (Based on Reviews and 35 reference(s) in Google Scholar.)
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