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.

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].

[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.