An activator of PDK1
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PS-210

Item No. 30923

Technical Information
Formal Name
2-[3-oxo-1-phenyl-3-[4-(trifluoromethyl)phenyl]propyl]-propanedioic acid
CAS Number
1221962-86-2
Molecular Formula
C19H15F3O5
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
λmax
235 nm
SMILES
FC(F)(F)C1=CC=C(C(CC(C2=CC=CC=C2)C(C(O)=O)C(O)=O)=O)C=C1
InChi Code
InChI=1S/C19H15F3O5/c20-19(21,22)13-8-6-12(7-9-13)15(23)10-14(11-4-2-1-3-5-11)16(17(24)25)18(26)27/h1-9,14,16H,10H2,(H,24,25)(H,26,27)
InChi Key
MLJPLHGJBUWCBA-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    PS-210 is an activator of phosphoinositide-dependent protein kinase 1 (PDK1) that increases its thermal stability.1,2 It is selective for PDK-1 over a panel of 120 kinases at 10 µM.1 PS-210 (2 µM) increases the activity of wild-type PDK1 but not PDK1 with a mutation in the PIF-binding pocket.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Busschots, K., Lopez-Garcia, L.A., Lammi, C., et alSubstrate-selective inhibition of protein kinase PDK1 by small compounds that bind to the PIF-pocket allosteric docking site. Chem. Biol. 19(9), 1152-1163 (2012).

    2. Wilhem, A., Lopez-Garcia, L.A., Busschots, K., et al2-(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. 55(22), 9817-9830 (2012).