375240 HNF4 Antagonist, BI6015 - CAS 93987-29-2 - Calbiochem

Overview

Replacement Information

Key Specifications Table

Empirical FormulaCAS #
C₁₅H₁₃N₃O₄S 93987-29-2

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375240-25MG
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      Glass bottle 25 mg
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      Description
      OverviewA cell-permeable phenylsulfonylbenzimidazole that is shown to dock in the ligand-binding pocket of both HNF4α and HNF4γ and antagonize HNF4α DNA binding activity in HepG2 cells (by 93%; 10 µM overnight), effectively inhibiting HNF4α-dependent cellular activities (Effective conc. 1 to 5 µM). HNF4γ inhibition by BI6015 can also lead to decreased insulin promoter binding by transactivators E47 & PDX-1 in T6PNE cells (5 µM 48 h). Although BI6015 is found to exhibit cancer-selective cytotoxicity toward a panel of 58 human cancer cells and Hep3B-Luc (Effective conc. 1 to 10 µM), 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 10 µM), but not PPARγ or a panel of 41 receptors/enzymes of human, mouse, and rat origin.
      Catalogue Number375240
      Brand Family Calbiochem®
      SynonymsHepatocyte Nuclear Factor4 Antagonist, 2-Methyl-1-(2-methyl-5-nitrophenylsulfonyl)-1H-benzo[d]imidazole
      References
      ReferencesKiselyuk, A., et al. 2012. Chem. Biol. 19, 806.
      Product Information
      CAS number93987-29-2
      FormBeige powder
      Hill FormulaC₁₅H₁₃N₃O₄S
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetHNFα & γ
      Purity≥99% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      HNF4 Antagonist, BI6015 - CAS 93987-29-2 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      HNF4 Antagonist, BI6015 - CAS 93987-29-2 - Calbiochem Certificates of Analysis

      TitleLot Number
      375240

      References

      Reference overview
      Kiselyuk, A., et al. 2012. Chem. Biol. 19, 806.
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision11-October-2012 JSW
      SynonymsHepatocyte Nuclear Factor4 Antagonist, 2-Methyl-1-(2-methyl-5-nitrophenylsulfonyl)-1H-benzo[d]imidazole
      DescriptionA cell-permeable phenylsulfonylbenzimidazole compound that is shown to dock in the ligand-binding pocket of both HNF4α and HNF4γ via in silico structural analyses and antagonizes HNF4α DNA binding activity (by 93% after 10 µM overnight treatment of HepG2 cells), effectively inhibiting HNF4α-dependent cellular activities, including HNF4α mRNA transcription (by 62% in murine insulinoma MIN6 and 84% in human hepatoma HepG2 cultures after 5 h and 48 h 5 µM inhibitor treatment, respectively) and OTC (omithine transcarbamoylase) promoter transcription (by 85% & >95% in human HNF4α-transfected HepG2 & CV-1 cells, respectively; 48 hr 1 µM treatment). HNF4γ inhibition by BI6015 is also reported to indirectly lead to decreased binding of transactivators, E47 & PDX-1, to insulin promoter in T6PNE cells (48 h 5 µM treatment). Although BI6015 is found to exhibit cancer-selective cytotoxicity toward a panel of 58 human cancer cells and Hep3B-Luc (Effective conc. 1 to 10 µM), but not primary murine hepatocytes, it does cause hepatic steatosis both in vitro (primary murine hepatocytes; 5 µM for 3 days) and in mice in vivo (10 to 30 mg/kg/day for 5 days via i.p.) and is effectively metabolized by liver enzymes, limiting its in vivo efficacy in treating human Hep3B-derived liver tumor in mice. BI6015 also inhibits Human CYP450 2C19 and rat L-type calcium channel (by 94% and 83%, respectively, at 10 µM), but not PPARγ or a panel of 41 receptors/enzymes of human, mouse, and rat origin.
      FormBeige powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number93987-29-2
      Structure formulaStructure formula
      Purity≥99% by HPLC
      SolubilityDMSO (10 mg/ml)
      Storage +2°C to +8°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesKiselyuk, A., et al. 2012. Chem. Biol. 19, 806.