[CAS NO. 1221962-86-2] PS210
PRODUCTS SPECIFICATIONS [1221962-86-2]
DESCRIPTION [1221962-86-2]
Overview
| MDL | MFCD32701991 |
|---|---|
| Molecular Weight | 380.31 |
| Molecular Formula | C19H15F3O5 |
| SMILES | O=C(C(C(O)=O)C(CC(C1=CC=C(C=C1)C(F)(F)F)=O)C2=CC=CC=C2)O |
Summary
PS210 is a potent and selective PDK1 activator with a K d 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] .
IC50 & 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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 100 mg/mL ( 262.94 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.6294 mL | 13.1472 mL | 26.2943 mL |
| 5 mM | 0.5259 mL | 2.6294 mL | 5.2589 mL |
| 10 mM | 0.2629 mL | 1.3147 mL | 2.6294 mL |
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.