BI-6015 - 5 mg

Activity: HNF4α inhibitor . Function/Pharmacology: 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 Represents the first small molecule tool for pharmacologic modulation of HNF4α activity. 2 Cell permeable. Chemical Name: 2-Methyl-1-[(2-methyl-5-nitrophenyl)sulfonyl]-1H-benzimidazole