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[1][2].

Product Specifications

CAS Number

1221962-86-2

UNSPSC

12352005

Target

PDK-1

Type

Reference compound

Related Pathways

PI3K/Akt/mTOR

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/ps210.html

Purity

99.79

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(C(C(O)=O)C(CC(C1=CC=C(C=C1)C(F)(F)F)=O)C2=CC=CC=C2)O

Molecular Formula

C19H15F3O5

Molecular Weight

380.31

References & Citations

[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.|[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.