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Liver X receptor (LXR) agonists and antagonists act on oxysterol-activated nuclear receptors. LXRα and LXRβ were shown in 1996 to respond to oxidized cholesterol derivatives such as 24,25-epoxycholesterol. Through sterol regulatory element-binding protein 1c (SREBP-1c) they link sterol sensing to fatty acid synthesis in liver, and they also drive genes of reverse cholesterol transport. GW3965 and GW3965 HCl are synthetic agonists of both subtypes and are widely used in such gene expression work. T0901317 activates LXR but also acts on the farnesoid X receptor, so selectivity controls matter. GSK-2033 acts as an antagonist and SR9243 as an inverse agonist, which allows loss-of-function comparisons in the same system.
SR9243 is a potent and selective LXR inverse agonist. SR9243 kills cancer cells by inhibiting lipid production and the Warburg effect. It induces cell death in multiple types of cancer and does not cause the side effects that have derailed previous attempts to target these processes.
SR9238 is a potent and selective LXR inverse agonist (IC50 values are 43 and 214 nM for LXRβ and LXRα, respectively).
GAC0001E5 is an inverse agonist of liver X receptors (LXR) that exhibits significant antiproliferative activity. This compound is relevant in cancer research, as it modulates lipid metabolism and cellular proliferation pathways. Its mechanism of action may provide insights into therapeutic strategies targeting LXR-related signaling in tumorigenesis.
BE1218 is an inverse agonist of the liver X receptors (LXR), with IC50 values of 9 nM for LXRα and 7 nM for LXRβ. This compound modulates cholesterol and fatty acid metabolism by inhibiting LXR-mediated gene expression. BE1218 is useful for research applications exploring the role of LXRs in metabolic disorders and potential therapeutic interventions in dyslipidemia.
