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BI-6015

  Cat. No.:  DC47522   Featured
Chemical Structure
93987-29-2
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More than 5000 active chemicals with high quality for research!
Field of application
BI-6015 is a hepatocyte nuclear factor 4α (HNF4α) antagonist that can inhibit the expression of known HNF4α target genes. BI6015 represses insulin promoter activity through HNF4α antagonism. BI-6015 can be used for the research of cancer and diabetes.
Cas No.: 93987-29-2
Chemical Name: BI-6015
Synonyms: BI 6015;2-Methyl-1-(2-methyl-5-nitrophenylsulfonyl)-1H-benzo[d]imidazole;2-Methyl-1-[(2-methyl-5-nitrophenyl)sulfonyl]-1H-benzimidazole (ACI);Benzimidazole, 2-methyl-1-[(5-nitro-o-tolyl)sulfonyl]- (7CI);2-Methyl-1-(2-methyl-5-nitrobenzenesulfonyl)-1H-1,3-benzodiazole;2-Methyl-1-(2-methyl-5-nitrophenyl)sulfonylbenzimidazole;BI-6015
SMILES: [O-][N+](C1C=C(S(N2C(C)=NC3C2=CC=CC=3)(=O)=O)C(C)=CC=1)=O
Formula: C15H13N3O4S
M.Wt: 331.346421957016
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: [1]. Kiselyuk A, et, al. HNF4α antagonists discovered by a high-throughput screen for modulators of the human insulin promoter. Chem Biol. 2012 Jul 27;19(7):806-18.
Description: BI-6015 is a hepatocyte nuclear factor 4α (HNF4α) antagonist that can inhibit the expression of known HNF4α target genes. BI6015 represses insulin promoter activity through HNF4α antagonism. BI-6015 can be used for the research of cancer and diabetes[1].
In Vivo: BI-6015 (10-30 mg/kg; i.p. once daily for 5 days) induces loss of HNF4α expression and hepatic steatosis in mice[1]. BI-6015 (10-30 mg/kg; i.p. daily or every other day for 20-57 days) induces apoptosis in a human hepatocellular carcinoma mouse model[1].
In Vitro: BI-6015 (1.25-20 μM; 24-72 h) is cytotoxic to human hepatocellular carcinoma (HCC)[1]. BI-6015 (2.5-10 μM; 5-48 h) inhibits HNF4α gene expression in HepG2 cells[1]. BI-6015 (5 μM; 3 d) induces hepatic steatosis in primary murine hepatocytes[1]. Cell Viability Assay[1] Cell Line: Hep3B-Luc cells and primary hepatocytes Concentration: 1.25, 2.5, 5, 10, 20 μM Incubation Time: 24, 48, 72 hours Result: Was markedly toxic to Hep3B cells but spared primary hepatocytes.
References: [1]. Kiselyuk A, et, al. HNF4α antagonists discovered by a high-throughput screen for modulators of the human insulin promoter. Chem Biol. 2012 Jul 27;19(7):806-18.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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