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].

SS-RJW100 targets liver receptor homolog-1 (LRH-1) and steroidogenic factor-1 (SF-1), crucial nuclear hormone receptors (NR) for metabolism, inflammation, and cell proliferation. It exhibits selective affinity with Ki values of 1.2 μM for LRH-1 and 30 μM for SF-1. Treatment with SS-RJW100 at 30 μM for 24 hours increases LRH-1 transcriptional activity in Hela cells overexpressing wild-type and mutant LRH-1 (T352V, H390A, A349F), indicating its efficacy is not compromised by these mutations, thus showing potential for activating LRH-1-dependent transcription in diverse cellular contexts despite common LRH-1 mutations.