PS 210|PS210|CAS 1221962-86-2|DC Chemicals

Cas No.:	1221962-86-2
Chemical Name:	PS210
Synonyms:	PS210; PS-210; PS 210;
SMILES:	O=C(O)C(C(C1=CC=CC=C1)CC(C2=CC=C(C(F)(F)F)C=C2)=O)C(O)=O
Formula:	C₁₉H₁₅F₃O₅
M.Wt:	380.319
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

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).
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.

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