BI-6015

BI-6015 is a small-molecule antagonist of hepatocyte nuclear factor 4 alpha (HNF4α) and hepatocyte nuclear factor 4 gamma (HNF4γ). Developed by the Sanford Burnham Prebys Medical Discovery Institute, BI-6015 acts as a chemical probe to study nuclear receptor-mediated gene regulation and metabolic homeostasis. It binds to the ligand-binding pocket of HNF4α, inhibiting its DNA-binding and transcriptional regulatory functions, which leads to the downregulation of HNF4α target genes involved in glucose metabolism, lipid processing, and liver-specific protein expression. BI-6015 has been investigated in preclinical research for its potential antineoplastic activity in various cancers, including hepatocellular carcinoma and gastric cancer, as well as its role in metabolic diseases, chronic kidney disease progression, and parenteral nutrition-associated cholestasis.

Other names

2-methyl-1-(2-methyl-5-nitrophenylsulfonyl)-1H-benzimidazole2-methyl-1-(2-methyl-5-nitrophenylsulfonyl)-1H-benzo[d]imidazole