BI-6015, HNF4a inhibitor (TBI1402)

Description

Product Details

Formal Name: 2-Methyl-1-[(2-methyl-5-nitrophenyl)sulfonyl]-1H-benzimidazole

Molecular Formula: C₁₅H₁₃N₃O₄S

Formula Weight: 331.35

CAS Number: 93987-29-2

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to 25 mg/ml) or in Ethanol (up to 10 mg/ml).

Storage: -20°C

Stability: ≥ 1 year.

Applications

HNF4a inhibitor

Functions

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. 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. Represents the first small molecule tool for pharmacologic modulation of HNF4α activity. Cell permeable.

Application Procedures

First dissolved in DMSO (up to 25 mg/ml) or in Ethanol (up to 10 mg/ml), then diluted to aqueous buffer. Solutions in DMSO or ethanol may be stored at -20° for up to 2 months.