PS48---PDK1Activator

PS48 is a novel PDK1 (phosphoinositide-dependent protein kinase 1) activator (Kd = 10.3 μM), which binds to the HM/PIF binding pocket rather than the ATP-. PS48 has been used to enhance iPSC reprogramming from human epidermal keratinocytes and endothelial cells.

How to Use:

• In vitro: PS48 was used at 5 µM concentration in cell culture.
• In vivo: n/a

Reference:

1. 1. Hindie V, et al. Structure and allosteric effects of low-molecular- weight activators on the protein kinase PDK1. (2009) Nature Chem Biol. 5: 758-764.
2. 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. (2009) J Med Chem. 52(15):4683-93.
3. 3. Zhu S, et al. Reprogramming of Human Primary Somatic Cells by Oct4 and Chemical Compounds. (2010) Cell Stem Cell. 7 (6)651-655.