A cell-permeable phenylsulfonylbenzimidazole that is shown to dock in the ligand-binding pocket of both HNF4a and HNF4g and antagonize HNF4a DNA binding activity in HepG2 cells (by 93%, 10uM overnight), effectively inhibiting HNF4a-dependent cellular activities (Effective conc. 1 to 5uM). HNF4g inhibition by BI6015 can also lead to decreased insulin promoter binding by transactivators E47 & PDX-1 in T6PNE cells (5uM 48h). Although BI6015 is found to exhibit cancer-selective cytotoxicity toward a panel of 58 human cancer cells and Hep3B-Luc (Effective conc. 1 to 10uM), but not primary murine hepatocytes, it does cause hepatic steatosis both in vitro and in mice in vivo, limiting its use in animal studies. BI6015 also inhibits Human CYP450 2C19 and rat L-type calcium channel (by 94% and 83%, respectively, at 10uM), but not PPARg or a panel of 41 receptors/enzymes of human, mouse, and rat origin. Synonyms: Hepatocyte Nuclear Factor4 Antagonist, 2-Methyl-1-(2-methyl-5-nitrophenylsulfonyl)-1H-benzo[d]imidazole CAS No: 93987-29-2 Molecular Formula: C15H13N3O4S Molecular Weight: 331.35 Appearance: Off-white to beige powder Purity: 97% (HPLC) Solubility: DMSO (10mg/ml) Storage and Stability: Powder may be stored at -20C. Stable for 12 months at -20C. Reconstitute with sterile ddH2O. Aliquot to avoid repeated freezing and thawing. Store at -20C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
Molekulargewicht:
331.35
Reinheit:
97% (HPLC)
Formulierung:
Off-white to beige powder
CAS Nummer:
[93987-29-2]
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