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BI-6015 | HNF4α inhibitor

CAS:
93987-29-2
Catalog Number:
10-1402
Activity:
HNF4α inhibitor
Chemical Name:
2-Methyl-1-[(2-methyl-5-nitrophenyl)sulfonyl]-1H-benzimidazole
Molecular Weight:
331.35
Molecular Formula:
C15H13N3O4S
Solubility:
Soluble in DMSO (up to 25 mg/ml) or in Ethanol (up to 10 mg/ml).
Physical Properties:
Tan solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 2 months.
Shipping Code:
RT

BI-6015 (93987-29-2) is a hepatocyte nuclear factor 4α (HNF4α) antagonist. HNF4α is a central regulator of gene expression in cell types that play a central role in metabolic homeostasis.1 BI-6015 binds to HNF4α with high affinity and modulates the expression of known target genes. It was shown to be selectively cytotoxic to cancer cell lines in vitro and in vivo however in vivo potency was limited by suboptimal pharmacokinetics.2 BI-6015 represents the first small molecule tool for pharmacologic modulation of HNF4α activity.2 Cell permeable.

References/Citations:

1) Wang et al. (2000), Hepatocyte Nuclear Factor 4α Regulates the Expression of Pancreatic β-Cell Genes Implicated in Glucose Metabolism and Nutrient-induced Insulin Secretion; J. Biol. Chem., 275 35953
2) Kiselyuk et al. (2012), HNF4α antagonists discovered by a high-throughput screen for modulators of the human insulin promotor; Chem. Biol., 19 806

BI-6015 | HNF4α inhibitor is also available in the Cellular Metabolism Library.
CAS:
93987-29-2
Catalog Number:
10-1402
Activity:
HNF4α inhibitor
Chemical Name:
2-Methyl-1-[(2-methyl-5-nitrophenyl)sulfonyl]-1H-benzimidazole
Molecular Weight:
331.35
Molecular Formula:
C15H13N3O4S
Solubility:
Soluble in DMSO (up to 25 mg/ml) or in Ethanol (up to 10 mg/ml).
Physical Properties:
Tan solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 2 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

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