RS-246204

RS-246204 is a R-spondin-1 substitute compound that is able initiate small intestinal organoids without the use of the R-spondin-1 protein.

Signaling Pathways >> Others >> Others

Research Areas >> Cancer

R-spondin-1 protein is added at a high concentration for the initiation and maintenance of the organoids. RS-246204 is a R-spondin-1 substitute that could promote the initial formation and growth of enteroids in the medium without R-spondin-1. The enteroids grown with RS-246204 had a similar differentiation capacity as well as self-renewal capacity as the enteroids grown with R-spondin-1. Furthermore, the RS-246204-derived enteroids could successfully produce the forskolin induced swelling and the organoid based epithelial to mesenchymal transition model[1].

RS-246204 significantly increased BrdU+ cells and body weight in the DSS induced colitis model. These results suggest that RS-246204 activates the R-spondin dependent pathway in Lgr5 stem cells, thereby enhancing proliferation or the anti-apoptotic effect, promoting regeneration of the intestinal epithelium and reducing the disease severity[1].

Mice[1] Seven-week-old C57Bl/6 mice are given a 2.5% dextran sulfate sodium treatment in drinking water for 5 days. RS-246204 (10 mg/kg in DMSO) is administered intraperitoneally at the end of the DSS exposure. The RS-246204 treatment is repeated every 24 h for 5 days. Daily assessments of disease activity are performed including measuring body weight and evaluating stool consistency. The mice are sacrificed the next day after the last injection of RS-246204. BrdU (50 mg/kg in saline) is administered intraperitoneally 24 hours before sacrifice[1].

[1]. Nam MO, et al. Effects of a small molecule R-spondin-1 substitute RS-246204 on a mouse intestinal organoid culture. Oncotarget. 2017 Dec 26;9(5):6356-6368.

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