PS210, inhibitor

PS210

Cat. Num. AAA5764695

• Synonyms: PS210; inhibitor

• Form/Format: Solid

• Solubility: (<1mg/ml refers to the product slightly soluble or insoluble)
• SMILES: C1=CC=C(C=C1)C(CC(=O)C2=CC=C(C=C2)C(F)(F)F)C(C(=O)O)C(=O)O
• Formula: C19H15F3O5
• Target & IC50: PDK1
• In vitro: 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].
• CAS Number: 1221962-86-2
• Preparation and Storage: Store at 0-4 degree C for short term (days to weeks), or -20 degree C for long term (months).

Chemical Structure

Related Product Information for PS210, inhibitor

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: 3uM) 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.

Product Categories/Family for PS210, inhibitor

PI3K/Akt/mTOR signaling; PDK

References

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.
Retteaier 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.