PDK1-IN-RS2 is a mimic of peptide docking motif (PIFtide) and is a substrate-selective PDK1 inhibitor with a K d of 9 μM. PDK1-IN-RS2 suppresses the activation of the downstream kinases S6K1 by PDK1 In Vitro PDK1-IN-RS2 stimulates the catalytic activity of PDK1 toward a peptide substrate by sixfold. The sulfonyl group of PDK1-IN-RS2 interacts with Arg131 through a salt bridge, because the sulfonamide is likely ionized under the crystallization conditions. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:Kd: 9 μM (PDK1)