BI-6015

Hepatocyte nuclear factor 4alpha (HNF4alpha) is a nuclear receptor transcription factor that controls the expression of many genes including those involved in glucose and lipid homeostasis and maintenance of epithelial differentiation. BI-6015 is a small molecule antagonist of HNF4alpha that has been shown to repress the expression of known HNF4alpha target genes. At concentrations up to 20 µM, BI-6015 has been shown to reduce endogenous insulin gene expression by as much as 50-fold in T6PNE cells. The hepatocytes from livers of mice injected with 10 and 30 mg/kg BI-6015 exhibit marked, dose-dependent fat accumulation (steatosis). Additionally, at a daily dose of 30 mg/kg, BI-6015 induces apoptosis in a human hepatocellular carcinoma mouse model.Formal Name: 2-methyl-1-[(2-methyl-5-nitrophenyl)sulfonyl]-1H-benzimidazole. CAS Number: 93987-29-2. Molecular Formula: C15H13N3O4S. Formula Weight: 331.3. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 16 mg/ml, DMSO: 14 mg/ml, DMSO:PBS (pH 7.2) (1:10): 0.09 mg/ml. lambdamax: 245 nm. SMILES: CC1=NC2=CC=CC=C2N1S(C3=C(C)C=CC([N+]([O-])=O)=C3)(=O)=O. InChi Code: InChI=1S/C15H13N3O4S/c1-10-7-8-12(18(19)20)9-15(10)23(21,22)17-11(2)16-13-5-3-4-6-14(13)17/h3-9H,1-2H3. InChi Key: ILVCPQPMRPHZSG-UHFFFAOYSA-N.