(R)-PS210 |
| رقم الكتالوجGC63802 |
(R) -PS210 ، المتماثل R لـ PS210 (مركب 4h-eutomer) ، هو منشط خيفي انتقائي للركيزة لـ PDK1 بقيمة AC50 تبلغ 1.8 ميكرومتر(R) - أهداف PS210 إلى جيب ربط PIF لـ PDK1PIF: جزء التفاعل كيناز 2 المرتبط ببروتين كيناز سي (PRK2)
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Cas No.: 1410101-89-1
Sample solution is provided at 25 µL, 10mM.
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(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].
[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.
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