Biological Activity
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PS48 is an allosteric small molecule activator of phosphoinositide-dependent protein kinase 1 (PDK1) that binds exclusively to the HM/PIF binding pocket distinct from rather than the ATP-binding site [1-2]. PS48 has been reported to enhance reprogramming efficiency of neonatal human epidermal keratinocytes (NHEKs) by about 15-fold. Additionally, PS48, in combination with sodium butyrate (NaB), could further increase the reprogramming efficiency over 25-fold [3].
Chemical Properties
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Cas No.: 1180676-32-7 |
M. Wt.: 286.75 |
Formula: C17H15ClO2 |
Purity: ≥98% by HPLC |
Chemical Name: (2Z)-5-(4-Chlorophenyl)-3-phenyl-2-pentenoic acid |
Appearance: White to off-white solid |
Solubility: Soluble in DMSO (>20 mg/ml) and ethanol (>10 mg/ml) |
Storage: Store solid at 4 ºC desiccated for the stability up to two years |
Application Concentration (Just for reference)
The appropriate working concentration of PS48 depends on cell types, cell culture properties and specific applications. It is recommended that researchers start with optimal experiments for first use.
Reference
[1] Hindie, V. et al. Structure and allosteric effects of low-molecular-weight activators on the protein kinase PDK1. Nat Chem Biol. 5:758-64 (2009).
[2] Stroba, A. et al. 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: 4683-93 (2009).
[3] Zhu S, et al. Reprogramming of Human Primary Somatic Cells by Oct4 and Chemical Compounds. Cell Stem Cell. 7 (6): 651-5 (2009).