BI-6015

BI6015 is a small molecule antagonist of Hepatocyte nuclear factor 4α (HNF4α) that has been shown to repress the expression of known HNF4α target genes. 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.

Product information

CAS Number: 93987-29-2

Molecular Weight: 331.35

Formula: C15H13N3O4S

Smiles: CC1=CC=C(C=C1S(=O)(=O)N1C2=CC=CC=C2N=C1C)[N+]([O-])=O

InChiKey: ILVCPQPMRPHZSG-UHFFFAOYSA-N

InChi: 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

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: To be determined

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

BI-6015 (1.25-20 μM; 24-72 h) is cytotoxic to human hepatocellular carcinoma (HCC). BI-6015 (2.5-10 μM; 5-48 h) inhibits HNF4α gene expression in HepG2 cells. BI-6015 (5 μM; 3 d) induces hepatic steatosis in primary murine 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. 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.

References:

1. Kiselyuk A, Lee SH, Farber-Katz S, Zhang M, Athavankar S, Cohen T, Pinkerton AB, Ye M, Bushway P, Richardson AD, Hostetler HA, Rodriguez-Lee M, Huang L, Spangler B, Smith L, Higginbotham J, Cashman J, Freeze H, Itkin-Ansari P, Dawson MI, Schroeder F, Cang Y, Mercola M, Levine F. HNF4α antagonists discovered by a high-throughput screen for modulators of the human insulin promoter. Chem Biol. 2012 Jul 27;19(7):806-18. doi: 10.1016/j.chembiol.2012.05.014. PubMed PMID: 22840769; PubMed Central PMCID: PMC3447631.
2. Mayati A, Le Vee M, Moreau A, Jouan E, Bucher S, Stieger B, Denizot C, Parmentier Y, Fardel O. Protein kinase C-dependent regulation of human hepatic drug transporter expression. Biochem Pharmacol. 2015 Dec 15;98(4):703-17. doi: 10.1016/j.bcp.2015.10.007. PubMed PMID: 26462574.

Products are for research use only. Not for human use.