BI-6015

Hepatocyte nuclear factor 4? (HNF4?) is a nuclear receptor transcription factor that controls the expression of many genes including those involved in glucose and lipid homeostasis and maintenance of epithelial differentiation. BI-6015 is a small molecule antagonist of HNF4? that has been shown to repress the expression of known HNF4? target genes.{21357} At concentrations up to 20 ?M, BI-6015 has been shown to reduce endogenous insulin gene expression by as much as 50-fold in T6PNE cells.{21357} The hepatocytes from livers of mice injected with 10 and 30 mg/kg BI-6015 exhibit marked, dose-dependent fat accumulation (steatosis).{21357} Additionally, at a daily dose of 30 mg/kg, BI-6015 induces apoptosis in a human hepatocellular carcinoma mouse model.{21357}