27-Norcholestenoic acid

27-Norcholestenoic acid (Compound 3) (10 μM; 18 h) acts as an inverse agonist of LXRα and LXRβ in HEK-293T cells, reducing basal luciferase activity at 10 μM and inhibiting the agonist effect of GW3965 (HY-10627)^[1].
27-Norcholestenoic acid (10 μM; 24 h) downregulates basal and GW3965-induced expression of FASN and SREBP-1a/c but does not affect ABCG1 expression, and does not affect the viability of HepG2 cells at the concentration used^[1].
27-Norcholestenoic acid (10 µM) induces conformational changes on the LXRβ AF-2 domain that favor corepressor over coactivator recruitment, supporting the inverse agonist activity^[1].
27-Norcholestenoic acid is not compatible with a proper recruitment of the NCoA1 coactivator NR-box, as the LXRβ/NCoA1 682-697 interaction is strongly destabilized in the MD simulation^[1].
27-Norcholestenoic acid (18 h) acts as an inverse agonist of LXRβ in HEK293 T cells, reducing basal luciferase activity^[2].
27-Norcholestenoic acid (400 ns) induces disruption of the His435-Trp457 interaction and destabilization of the H11-H12 region of the LXRβ ligand binding domain^[2].

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