1221962-86-2
Chemical Structure
PS210
- CAS No.: 1221962-86-2
- Formula:C19H15F3O5
- Molecular Weight:380.31
IUPAC Name: 2-(3-oxo-1-phenyl-3-(4-(trifluoromethyl)phenyl)propyl)malonic acid
InChIKey: MLJPLHGJBUWCBA-UHFFFAOYSA-N
SMILES: O=C(C(C(O)=O)C(CC(C1=CC=C(C=C1)C(F)(F)F)=O)C2=CC=CC=C2)O
Biological Activity: 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].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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PS210 | 98.03% | 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. | ||||||||||||||||||||
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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. [Content Brief]
- [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. [Content Brief]
