PS210 是针对PDK1的 PIF 结合口袋的、选择性的、有效的PDK1激活剂，对其他蛋白激酶无活性。在细胞中，它的前药 PS423 可作为PDK1的底物选择性抑制剂，抑制 S6K 的磷酸化和活化。

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

PS210 stabilized the residue Arg131 when PS210 causes stabilization of PDK1 to the temperature gradient, located opposite to the helix a-B at the other extreme of the helix a-C. So, 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[1].

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C19H15F3O5

380.31

DMSO:60 mg/ml (157.77 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years