PS 210 Property

Boiling point:

577.9±50.0 °C(Predicted)

Density 

1.400±0.06 g/cm3(Predicted)

solubility 

DMSO:100.0(Max Conc. mg/mL);262.94(Max Conc. mM)

form 

A crystalline solid

pka

2.93±0.10(Predicted)

color 

White to off-white

Hazard and Precautionary Statements (GHS)

PS 210 Chemical Properties,Usage,Production

Uses

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[1][2].

References

[1] Busschots K, et al. Substrate-selective inhibition of protein kinase PDK1 by small compounds that bind to the PIF-pocket allosteric docking site. Chem Biol. 2012 Sep 21;19(9):1152-63. DOI:10.1016/j.chembiol.2012.07.017
[2] Rettenmaier TJ, et al. A small-molecule mimic of a peptide docking motif inhibits the protein kinase PDK1. Proc Natl Acad Sci U S A. 2014 Dec 30;111(52):18590-5. DOI:10.1073/pnas.1415365112