PS210

Names

[ CAS No. ]:
1221962-86-2

[ Name ]:
PS210

Biological Activity

[Description]:

PS 210 is a potent, specific activator of PDK1 that target the PIF-binding pocket of PDK1, does not alter the activity of any of the 121 kinases (S6K, PKB/Akt or GSK3).

[Related Catalog]:

Signaling Pathways >> PI3K/Akt/mTOR >> PDK-1

Research Areas >> Cancer

[Target]

Kd: 3 μM (PDK1)[2]

[In Vitro]

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[1].

[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.

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₉H₁₅F₃O₅

[ Molecular Weight ]:
380.319

[ Storage condition ]:
-20°C

PS210

Names

Biological Activity

Chemical & Physical Properties

Related Compounds