(R)-PS210

• CAT Number: I016812
• CAS Number: 1410101-89-1
• Molecular Formula: C19H15F3O5
• Molecular Weight: 380.31
• Purity: ≥95%
• Synonyms: 2-[(1R)-3-oxo-1-phenyl-3-[4-(trifluoromethyl)phenyl]propyl]propanedioic acid
• InChI: InChI=1S/C19H15F3O5/c20-19(21,22)13-8-6-12(7-9-13)15(23)10-14(11-4-2-1-3-5-11)16(17(24)25)18(26)27/h1-9,14,16H,10H2,(H,24,25)(H,26,27)/t14-/m0/s1
• InChIKey: MLJPLHGJBUWCBA-AWEZNQCLSA-N
• SMILES: C1=CC=C(C=C1)C(CC(=O)C2=CC=C(C=C2)C(F)(F)F)C(C(=O)O)C(=O)O

(R)-PS210, the R enantiomer of PS210 (compound 4h-eutomer), is a substrate-selective allosteric activator of PDK1 with an AC50 value of 1.8 μM. (R)-PS210 targets to the PIF-binding pocket of PDK1. PIF: The protein kinase C-related kinase 2 (PRK2)-interacting fragment[1].
(R)-PS210 displays an AC50 value of 1.8 μM towards PDK1 in a Cell-Free Kinase Activity Assay. And the maximum activation of PDK1 compared to DMSO control of (R)-PS210 is 5.5 fold[1].

Reference

[1]. Wilhelm A, et al. 2-(3-Oxo-1,3-diphenylpropyl)malonic acids as potent allosteric ligands of the PIF pocket of phosphoinositide-dependent kinase-1: development and prodrug concept.J Med Chem. 2012 Nov 26;55(22):9817-30.
 [Content Brief]