| Description: |
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. |
| Target: |
ERK1:98 nM (Kd)
RasGAP:212 nM (Kd)
RSK1:0.5 μM (IC50)
RSK2:2.5 μM (IC50)
RSK3:3.3 μM (IC50)
RSK4:10 μM (IC50) |
| In Vitro: |
Pluripotin (SC-1) inhibits Abl1, p70S6K, PLK2, RSK1, RSK2, RSK3, RSK4 with IC50s of 0.005, 1.4, 2.2, 0.5, 2.5, 3.3, 10.0 µM,respectively. Pluripotin (SC-1) decreases cell growth for 7 colon tumor cell lines. After a five day exposure to 0.1 µM SC-1, the seven colon tumor lines are evaluated for changes in cell number and viability. There is a statistically significant decrease in cell number but >95% viability[2]. |
| Cell Assay: |
The seven colon cancer lines (COLO 205, HCC-2998, HCT-15, HCT-116, HT29, KM12, SW-620) are used. In all experiments, each tumor line is cultured in 60 mm2 tissue culture treated dishes at an initial concentration of 62,500/mL (total 4 mL) before addition of 0.1 µM Pluripotin (SC-1) or an equivalent amount of diluent (DMSO) the next day. Five day exposures are conducted. The final concentration utilized for treatment for all tumor lines is determined by evaluating a range of SC-1 concentrations (0.01 to 10 µM) for sphere formation and any cytotoxic effects in the HCT-116 tumor line. Cell viability is routinely evaluated with the trypan blue exclusion test and is always >95% for concentrations at or below 0.1 µM[2]. |
| 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.
[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. |
