Hepatocyte nuclear factor 4alpha (HNF4alpha) antagonist. HNF4alpha is a central regulator of gene expression in cell types that play a central role in metabolic homeostasis. 1 BI-6015 binds to HNF4alpha 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 Represents the first small molecule tool for pharmacologic modulation of HNF4alpha activity. 2 Cell permeable.
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