| BI 6015HNF4α antagonist |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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| Cas No. | 93987-29-2 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | 2-methyl-1-((2-methyl-5-nitrophenyl)sulfonyl)-1H-benzo[d]imidazole | ||
| Canonical SMILES | O=S(N1C2=CC=CC=C2N=C1C)(C3=CC([N+]([O-])=O)=CC=C3C)=O | ||
| Formula | C15H13N3O4S | M.Wt | 331.35 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
BI 6015 is an antagonist of hepatocyte nuclear factor 4α [1].
Hepatocyte nuclear factor 4α (HNF4α) is a nuclear receptor and regulates gene expression in enterocytes, hepatocytes and pancreatic β cells [1].
BI 6015 is a HNF4α antagonist. BI6015 inhibited the insulin promoter. In T6PNE cells, BI6015 reduced the expression of endogenous insulin by 50-fold. In MIN6 and HepG2 cells, BI6015 inhibited the expression of HNF4α. Also, BI6015 changed HNF4α protease sensitivity [1]. In T6PNE cells, BI 6015 reduced the levels of longer chain acylcarnitines (C18, C18:1, C16, and C14) and increased acetylcarnitine, which suggested that BI 6015 increased fatty acid oxidation. In the human hepatoma cell line Hep3B, BI 6015 exhibited cytotoxic activity [1].
In mice, BI6015 (30 mg/kg) induced a loss of HNF4α protein in the liver, but not in the kidney and intestine. Also, BI6015 caused fat accumulation and steatosis and vesicular changes in a dose-dependent way [1].
Reference:[1]. Kiselyuk A, Lee SH, Farber-Katz S, et al. HNF4a Antagonists Discovered by a High-Throughput Screen for Modulators of the Human Insulin Promoter. Chem Biol, 2012, 19(7): 806-818.
