1221962-86-2

1221962-86-2 structure

Name: PS210
Chemical Name: PS 210
CAS Number: 1221962-86-2
Molecular Formula: C₁₉H₁₅F₃O₅
Molecular Weight: 380.319
Catalog: Signaling Pathways PI3K/Akt/mTOR PDK-1
Create Date: 2020-01-20 14:33:57
Modify Date: 2024-01-08 18:30:59
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).

Name	PS 210

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.