(R)-PS210, the R enantiomer of PS210 (compound 4h-eutomer), is a substrate-selective allosteric activator of PDK1 with an AC 50 value of 1.8 μM. (R)-PS210 targets to the PIF-binding pocket of PDK1. PIF: The protein kinase C-related kinase 2 (PRK2)-interacting fragment
In Vitro
(R)-PS210 displays an AC 50 value of 1.8 μM towards PDK1 in a Cell-Free Kinase Activity Assay. And the maximum activation of PDK1 compared to DMSO control of (R)-PS210 is 5.5 fold. MCE has not independently confirmed the accuracy of these methods. They are for reference only.