PDK-1 Activator

Sexangularetin 3-sophoroside is a PDK1 and Akt phosphorylation activator with neuroprotective properties. Sexangularetin 3-sophoroside restores phosphorylated GSK-3β protein levels. Sexangularetin 3-sophoroside acts as a ROS inhibitor and regulates mRNA expression of superoxide dismutase 1 and catalase. Sexangularetin 3-sophoroside can be used for the research of Parkinson’s disease.

PS48 is an activator of PDK1 with an AC₅₀ of 8 μM.

PS210 is a potent and selective PDK1 activator with a K_d of 3 μM and targets the PIF-binding pocket of PDK1. PS210 is inactive against other protein kinases, including PDK1 downstream signaling components such as S6K, PKB/Akt or GSK3. In cells, the prodrug of PS210 (PS423) acts as a substrate-selective inhibitor of PDK1, inhibiting the phosphorylation and activation of S6K.

CRTh2 antagonist 3 is a potent chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTh2) antagonist. CRTh2 antagonist 3 enhances the activity of PDK1 toward a short peptide substrate, with an EC₅₀ of 2 μM and a K_d of 8.4 μM. CRTh2 antagonist 3 has the potential for cardiovascular inflammation.