PS210
PS210 is a potent and selective PDK1 activator with a Kd 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].
Product Specifications
CAS Number
1221962-86-2
UNSPSC
12352005
Target
PDK-1
Type
Reference compound
Related Pathways
PI3K/Akt/mTOR
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/ps210.html
Purity
99.79
Solubility
DMSO : 100 mg/mL (ultrasonic)
Smiles
O=C(C(C(O)=O)C(CC(C1=CC=C(C=C1)C(F)(F)F)=O)C2=CC=CC=C2)O
Molecular Formula
C19H15F3O5
Molecular Weight
380.31
References & Citations
[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.
Shipping Conditions
Blue Ice
Storage Conditions
-20°C, 3 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Available Sizes
Frequently Asked Questions
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