BI 6015HNF4α antagonist CAS# 93987-29-2 |
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Quality Control & MSDS
3D structure
Package In Stock
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| Cas No. | 93987-29-2 | SDF | Download SDF |
| PubChem ID | 3269393 | Appearance | Powder |
| Formula | C15H13N3O4S | M.Wt | 331.35 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 20 mM in DMSO | ||
| Chemical Name | 2-methyl-1-(2-methyl-5-nitrophenyl)sulfonylbenzimidazole | ||
| SMILES | CC1=C(C=C(C=C1)[N+](=O)[O-])S(=O)(=O)N2C(=NC3=CC=CC=C32)C | ||
| Standard InChIKey | ILVCPQPMRPHZSG-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C15H13N3O4S/c1-10-7-8-12(18(19)20)9-15(10)23(21,22)17-11(2)16-13-5-3-4-6-14(13)17/h3-9H,1-2H3 | ||
| 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. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Hepatocyte nuclear factor 4α (HNF4α) antagonist. Represses expression of known HNF4α target genes. Decreases HNF4α DNA binding. Exhibits cytotoxic activity in a range of tumor cell lines, including human hepatocellular carcinoma. |
BI 6015 Dilution Calculator
BI 6015 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.018 mL | 15.0898 mL | 30.1796 mL | 60.3591 mL | 75.4489 mL |
| 5 mM | 0.6036 mL | 3.018 mL | 6.0359 mL | 12.0718 mL | 15.0898 mL |
| 10 mM | 0.3018 mL | 1.509 mL | 3.018 mL | 6.0359 mL | 7.5449 mL |
| 50 mM | 0.0604 mL | 0.3018 mL | 0.6036 mL | 1.2072 mL | 1.509 mL |
| 100 mM | 0.0302 mL | 0.1509 mL | 0.3018 mL | 0.6036 mL | 0.7545 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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HNF4alpha antagonists discovered by a high-throughput screen for modulators of the human insulin promoter.[Pubmed:22840769]
Chem Biol. 2012 Jul 27;19(7):806-18.
Hepatocyte nuclear factor (HNF)4alpha is a central regulator of gene expression in cell types that play a critical role in metabolic homeostasis, including hepatocytes, enterocytes, and pancreatic beta cells. Although fatty acids were found to occupy the HNF4alpha ligand-binding pocket and were proposed to act as ligands, there is controversy about both the nature of HNF4alpha ligands as well as the physiological role of the binding. Here, we report the discovery of potent synthetic HNF4alpha antagonists through a high-throughput screen for effectors of the human insulin promoter. These molecules bound to HNF4alpha with high affinity and modulated the expression of known HNF4alpha target genes. Notably, they were found to be selectively cytotoxic to cancer cell lines in vitro and in vivo, although in vivo potency was limited by suboptimal pharmacokinetic properties. The discovery of bioactive modulators for HNF4alpha raises the possibility that diseases involving HNF4alpha, such as diabetes and cancer, might be amenable to pharmacologic intervention by modulation of HNF4alpha activity.
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