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BI 6015

Names

[ CAS No. ]:
93987-29-2

[ Name ]:
BI 6015

[Synonym ]:
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

Biological Activity

[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.

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
570.6±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C15H13N3O4S

[ Molecular Weight ]:
331.35

[ Flash Point ]:
298.9±32.9 °C

[ Exact Mass ]:
331.062683

[ PSA ]:
106.16000

[ LogP ]:
3.53

[ Vapour Pressure ]:
0.0±1.6 mmHg at 25°C

[ Index of Refraction ]:
1.679

Related Compounds