SS-RJW100 is a enantiomer of RJW100, which is a racemic agonist of nuclear receptor liver receptor homolog 1 (LRH-1) and steroidogenic factor 1 (SF-1). SS-RJW100 promotes recruitment of coregulator protein fragments in vitro, recruits the transcriptional intermediary factor 2 (Tif2) coactivator to LRH-1. SS-RJW100 diminishes LRH-1 allosteric activation networks, shows poor 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 Ki 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. |
[1]. Mays SG, et al. Enantiomer-specific activities of an LRH-1 and SF-1 dual agonist. Sci Rep. 2020 Dec 17;10(1):22279.
[2]. Stec J. Tandem reaction sequences on a zirconocene template[J]. University of Southampton, 2010.