PS210

PS210 is a potent and selective PDK1 activator with a Kd 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.

98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

PS 210

DMSO ：76 mg/mL (199.84 mM)
Ethanol ：76 mg/mL (199.84 mM)

PDK1

When PS210 induces a stabilization of PDK1 to the temperature gradien, PS210 stabilized the residue Arg131, located opposite to the helix a-B at the other extreme of the helix a-C. Thus, the residues forming part of the phosphate-binding site appear to be a fixed point that allows for the relative movement of the helices in the process of PDK1 activation.