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PS48 is an allosteric small molecule that activates phosphoinositide-dependent protein kinase 1 (PDK1) by binding exclusively to the HM/PIF binding pocket rather than the ATP-binding site (1,2). PS48 metabolically facilitates a conversion from mitochondrial oxidation to glycolysis during the reprogramming process. PS48 enhances reprogramming efficiency by about 15-fold (3).
CAS Number
1118807-13-8
Chemical Formula
C17H15ClO2
Chemical Name
5-(4-Chloro-phenyl)-3-phenyl-pent-2-enoic acid
Molecular Weight
286.75
QC Specifications
MASS Spec
Mouse ESC culture for toxicity
Shipping Information
on blue ice
Storage
4°C protected from light
Stability
Stable for up to 6 months from date of receipt when stored as directed.
Reference
1. Hindie et al (2009) Structure and allosteric effects of low-molecular-weight activators on the protein kinase PDK1. Nat.Chem.Biol. 5 758.
2. Stroba et al (2009) 3,5-diphenylpent-2-enoic acids as allosteric activators of the protein kinase PDK1: structure-activity relationships and thermodynamic characterization of binding as paradigms for PIF-binding pocket-targeting compounds. J.Med.Chem. 52 4683.
3. Williams (2010) Elastic network model of allosteric regulation in protein kinase PDK1. BMC Struct.Biol. 10 11
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