RJW100 

RJW100 is a potent liver receptor homolog 1 (LRH-1, NR5A2) and steroidogenic factor-1 (SF-1, NR5A1) agonist with pEC₅₀s of 6.6 and 7.5, respectively^[1]. RJW100 also causes strong activation of the miR-200c (miRNA-200c, microRNA-200c) promoter^[2].

pEC50: 6.6 (LRH-1) and 7.5 (SF-1)^[1]

RJW100 (compound 24-exo) treatment induces a significant dose-dependent increase in small/short heterodimer partner (SHP) transcripts beginning at 5 µM^[1].
RJW100 (compound 24-exo) clearly displaces the bound PIP2 phospholipid from SF-1 almost completely at 1 µM^[1].
Using hLRH-1 LBD alone that had not been complexed with any phospholipids, the result shows a clear dose-dependent shift in hLRH-1 LBD (ligand binding domain) native PAGE migration upon RJW100 (compound 24-exo; 0-100 µM) binding^[1].
RJW100 causes strong activation of the miR-200c promoter and exhibits strong ability to downregulate ZEB1 and ZEB2 proteins^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

386.58

C₂₈H₃₄O

1276664-20-0

O[C@@H]1CC[C@@]2(C(C3=CC=CC=C3)=C)C(C4=CC=CC=C4)=C(CCCCCC)C[C@@]12[H].[Relative stereochemistry]

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Richard J Whitby, 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 Apr 14;54(7):2266-81.  [Content Brief]

  [2]. Yuxia Zhang, et al. Regulation of miR-200c by nuclear receptors PPARα, LRH-1 and SHP. Biochem Biophys Res Commun. 2011 Dec 9;416(1-2):135-9.  [Content Brief]