PDK1-IN-RS2 inhibits the activation of the downstream kinases S6K1 by PDK1. PDK1-IN-RS2 is a mimic of the peptide docking motif (PIFtide) and is a substrate-selective PDK1 inhibitor (Kd: 9 μM).

Because the sulfonamide is likely ionized under the crystallization conditions, the sulfonyl group of PDK1-IN-RS2 interacts with Arg131 through a salt bridge. PDK1-IN-RS2 stimulates the catalytic activity of PDK1 toward a peptide substrate by sixfold [1].

1643958-89-7

C15H9ClN2O2S3

380.89

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years