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Zymostenol is a late-stage precursor in the biosynthesis of cholesterol. It is an agonist of retinoic acid receptor-related orphan receptor γ (RORγ) with an EC50 value of 1 µM in a RORγ coactivator recruitment assay in the presence of ursolic acid . It increases the number of myelin basic protein-positive oligodendrocytes generated from oligodendrocyte precursor cells in vitro. Zymostenol accumulates in cells following administration of microsomal antiestrogen-binding site (AEBS) ligands, such as tamoxifen , which are associated with cell differentiation and a protective type of autophagy. When used alone at a concentration of 20 µM, zymostenol halts the cell cycle at the G0/G1 phase and increases the levels of free sterols, esterified sterols, and triacylglycerols in MCF-7 cells.

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