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)