GAC0001E5

GAC0001E5 (also known as 1E5) is a **small molecule** inverse agonist of the **liver X receptor (LXR)**, specifically targeting the LXRβ isoform. It exhibits potent anti-cancer activity by inhibiting cell growth and proliferation in **pancreatic ductal adenocarcinoma** and multiple subtypes of **breast cancer**, including luminal A, triple-negative, and endocrine-resistant types[1][2][3][4][5]. Mechanistically, it reduces LXRβ protein and transcript levels, disrupts **glutaminolysis** (notably lowering intracellular glutamate), impairs downstream glutamine metabolism genes (GLS1, GOT1, GOT2, GLUD1), and induces oxidative stress by increasing cellular reactive oxygen species[2][4][5]. These effects culminate in blocked tumor cell colony formation and synergize with GLS inhibitors to further suppress glutamine metabolism[1][2]. Developed and characterized for anti-cancer research, GAC0001E5 is not for human use and is supplied for laboratory applications only[1].

Other names

GAC0001E5GAC-0001E5GAC 0001E51E5LXR ligand 1E5