HNF4α 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. BIM5078 is an HNF4α antagonist that can repress the expression of known HNF4α target genes, inhibiting endogenous insulin expression in T6PNE cells with an IC₅₀ value of 930 nM.¹ BIM5078 binds directly to the ligand binding pocket of HNF4α with an EC₅₀ value of 11.9 nM.¹ However, BIM5078 has unfavorable pharmacokinetic properties including low plasma and microsomal stability (8% remaining after 3 hours and 32% after 1.25 hours, respectively), high binding to plasma proteins (98% bound after 4 hours), and low solubility (0.17 mg/ml after 18 hours).¹ BI6015 (Item No. 12032) is a structural analog of BIM5078 developed for more favorable pharmacokinetics.

≥98%

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1.Kiselyuk, A.,Lee, S.H.,Farber-Katz, S., et al. HNF4α antagonists discovered by a high-throughput screen for modulators of the human insulin promoter. Chemistry & Biology 19, 806-818 (2012).