SS-RJW100 is an enantiomer of RJW100, known as a racemic agonist that targets two nuclear receptors: liver receptor homolog 1 (LRH-1) and steroidogenic factor 1 (SF-1). In vitro experiments reveal that SS-RJW100 promotes the recruitment of coregulator protein fragments and enhances the interaction with the transcriptional intermediary factor 2 (Tif2) coactivator specifically for LRH-1. Additionally, SS-RJW100 disrupts the allosteric activation networks of LRH-1, displaying suboptimal thermal stability [1] [2].

Liver receptor homolog-1 (LRH-1) and steroidogenic factor-1 (SF-1), which are essential nuclear hormone receptors (NR) involved in regulating metabolism, inflammation, and cell proliferation, are specifically targeted by SS-RJW100. This compound demonstrates selective affinity towards LRH-1 and SF-1, displaying Ki values of 1.2 μM and 30 μM, respectively. Upon treatment with SS-RJW100 at a concentration of 30 μM for 24 hours, an increase in LRH-1 transcriptional activity is observed in Hela cells overexpressing both wild-type and mutant forms of LRH-1 (T352V, H390A, A349F), indicating the compound's efficacy is unaffected by these mutations. This suggests SS-RJW100's potential in activating LRH-1 dependent transcription in various cellular environments without being hindered by common LRH-1 mutations.