In HEK293 cells expressing LXRs, SR9243 inhibits LXR activation by enhancing LXR-corepressor recruitment. In a variety of cancer cell types, SR9243 reduces cancer cell viability, induces apoptotic cell death, and sensitizes cancer cells to chemotherapeutic treatments.
In vivo
In Ob/Ob mice fed a high-fat diet, SR9243 (60 mg/kg, i.p.) inhibits LXR-dependent lipogenic enzyme gene expression and tumor growth.