PS-210 is an activator of phosphoinositide-dependent protein kinase 1 (PDK1) that increases its thermal stability. It is selective for PDK-1 over a panel of 120 kinases at 10 µM. PS-210 (2 µM) increases the activity of wild-type PDK1 but not PDK1 with a mutation in the PIF-binding pocket.Formal Name:...

Description: PS210 is a potent and selective activator of PDK1 (Kd: 3 µM), specifically targeting the PIF-binding pocket of PDK1 without affecting other protein kinases such as S6K, PKB/Akt, or GSK3. Its prodrug, PS423, serves as a substrate-selective inhibitor of PDK1 in cells, inhibiting the phosphorylation and...