Uses
Pluripotin is a dual inhibitor of ERK1 and RasGAP with KDs of 98 nM and 212 nM, respectively. Pluripotin also inhibits RSK1, RSK2, RSK3, and RSK4 with IC50s of 0.5, 2.5, 3.3, and 10.0 μM, respectively.
Biological Activity
Pluripotin is an activator of murine embryonic stem (ES) cell self-renewal. It appears th at pluripotin mediates the activity by dual RasGAP and ERK1 inhibition.
IC 50
ERK1: 98 nM (Kd); RasGAP: 212 nM (Kd); RSK1: 0.5 μM (IC
50); RSK2: 2.5 μM (IC
50); RSK3: 3.3 μM (IC
50); RSK4: 10 μM (IC
50)
References
[1] Chen S, et al. Self-renewal of embryonic stem cells by a small molecule. Proc Natl Acad Sci U S A. 2006 Nov 14;103(46):17266-71. DOI:
10.1073/pnas.0608156103[2] Mertins SD, et al. A small molecule (pluripotin) as a tool for studying cancer stem cell biology: proof of concept. PLoS One. 2013;8(2):e57099. DOI:
10.1371/journal.pone.0057099