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(R)-PS210

Names

[ CAS No. ]:
1410101-89-1

[ Name ]:
(R)-PS210

Biological Activity

[Description]:

(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].

[Related Catalog]:

Signaling Pathways >> PI3K/Akt/mTOR >> PDK-1
Research Areas >> Cancer

[Target]

AC50: 1.8 μM (PDK1)[1]


[In Vitro]

(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].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C19H15F3O5

[ Molecular Weight ]:
380.31

Related Compounds