(r)-ps-210

(R)-PS210, the R enantiomer of PS210, is a substrate-selective allosteric PDK1 activator with an (AC50 of 1.8 μM).

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 activation of S6K.