BI-6015 (93987-29-2) is a hepatocyte nuclear factor 4α (HNF4α) antagonist. HNF4α is a central regulator of gene expression in cell types that play a central role in metabolic homeostasis.1 BI-6015 binds to HNF4α with high affinity and modulates the expression of known target genes. It was shown to be selectively cytotoxic to cancer cell lines in vitro and in vivo however in vivo potency was limited by suboptimal pharmacokinetics.2 BI-6015 represents the first small molecule tool for pharmacologic modulation of HNF4α activity.2 Cell permeable.
1) Wang et al. (2000), Hepatocyte Nuclear Factor 4α Regulates the Expression of Pancreatic β-Cell Genes Implicated in Glucose Metabolism and Nutrient-induced Insulin Secretion; J. Biol. Chem., 275 35953
2) Kiselyuk et al. (2012), HNF4α antagonists discovered by a high-throughput screen for modulators of the human insulin promotor; Chem. Biol., 19 806