1410101-89-1

(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].

[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. DOI:10.1021/jm3010477