RJW103 is an acid-stable SF-1 (NR5A1) and LRH-1 agonist with pEC 50 values of 6.5 and 5.9, respectively. RJW103 activates SF-1 - and LRH-1 -mediated transcription of endogenous target genes. RJW103 can be used in research on cancer, endocrinology and metabolic diseases, such as adrenocortical tumors [1] [2].
In Vitro, RJW103 (10 μM; 24 h) activates SF-1-mediated transcription of SHP, StAR, G0S2, and MeOX1 in mSF-1-expressing HEK293 cells, and activates LRH-1-mediated transcription of StAR and G0S2 (but not SHP or MeOX1) in hLRH-1-expressing HEK293 cells[1].
References:
[1]. Whitby RJ, et al. Small molecule agonists of the orphan nuclear receptors steroidogenic factor-1 (SF-1, NR5A1) and liver receptor homologue-1 (LRH-1, NR5A2). J Med Chem. 2011;54(7):2266-2281.
[2]. Wu T, et al. Liver receptor homolog-1: structures, related diseases, and drug discovery. Acta Pharmacol Sin. 2024;45(8):1571-1581.
In Vitro, RJW103 (10 μM; 24 h) activates SF-1-mediated transcription of SHP, StAR, G0S2, and MeOX1 in mSF-1-expressing HEK293 cells, and activates LRH-1-mediated transcription of StAR and G0S2 (but not SHP or MeOX1) in hLRH-1-expressing HEK293 cells[1].
References:
[1]. Whitby RJ, et al. Small molecule agonists of the orphan nuclear receptors steroidogenic factor-1 (SF-1, NR5A1) and liver receptor homologue-1 (LRH-1, NR5A2). J Med Chem. 2011;54(7):2266-2281.
[2]. Wu T, et al. Liver receptor homolog-1: structures, related diseases, and drug discovery. Acta Pharmacol Sin. 2024;45(8):1571-1581.