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) are closely related nuclear hormone receptors (NR) that play key roles as regulators of metabolism, inflammation, and proliferation [1]. SS-RJW100 (1 nM-1 mM; ) binds LRH-1 and SF-1, with binding affinity K i values of 1.2 μM (LRH-1), 30 μM (SF-1), respectively [1]. SS-RJW100 (30 μM; 24 h) increases LRH-1 transcriptional activity in both wild-type and mutant LRH-1 overexpressed Hela cells, without being affected by mutations [1]. RT-PCR [1] Cell Line: Wild-type (WT) and mutant LRH-1 overexpressed Hela cells (T352V, H390A, A349F) Concentration: 30 μM Incubation Time: 24 hours; for pre-treatment Result: Increased increases LRH-1 transcriptional activity. Showed activation effect on LRH-1 expressing cells without being affected by T352V LRH-1 mutant or H390A LRH-1 mutant.