| Bioactivity | 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]. | ||||||||||||
| Target | hepatocyte nuclear factor 4α (HNF4α) | ||||||||||||
| Invitro | 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: | ||||||||||||
| 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]. | ||||||||||||
| Name | BI-6015 | ||||||||||||
| CAS | 93987-29-2 | ||||||||||||
| Formula | C15H13N3O4S | ||||||||||||
| Molar Mass | 331.35 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |