93987-29-2

93987-29-2 structure

Name: BI 6015
Chemical Name: 2-methyl-1-(2-methyl-5-nitro-benzenesulfonyl)-1H-benzoimidazole
CAS Number: 93987-29-2
Molecular Formula: C₁₅H₁₃N₃O₄S
Molecular Weight: 331.35
Catalog: Research Areas Cancer
Create Date: 2017-03-14 20:03:46
Modify Date: 2024-01-10 20:53:03
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].

Name	2-methyl-1-(2-methyl-5-nitro-benzenesulfonyl)-1H-benzoimidazole
Synonyms	1-<4-methyl-phenylsulfonyl>-3-butyl-2,4,5-trioxo-imidazolidin 1H-Benzimidazole, 2-methyl-1-[(2-methyl-5-nitrophenyl)sulfonyl]- 2,4,5-Trioxo-1-<p-tolylsulfonyl>-3-butyl-imidazolidin 3-Tosyl-1-butyl-parabansaeure 2-Methyl-1-[(2-methyl-5-nitrophenyl)sulfonyl]-1H-benzimidazole

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].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Others >> Others Research Areas >> Metabolic Disease
Target	hepatocyte nuclear factor 4α (HNF4α)[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.
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].
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.