BI6015

Catalog No.E0401 Purity:99.91%

BI6015, a hepatocyte nuclear factor 4α (HNF4α) antagonist, induces loss of HNF4α expression and hepatic steatosis in vivo. BI6015 is cytotoxic to human hepatocellular carcinoma (HCC).

BI6015 Chemical Structure

CAS No. 93987-29-2

Purity & Quality Control

Batch: Purity: 99.91%

99.91

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Biological Activity

Description	BI6015, a hepatocyte nuclear factor 4α (HNF4α) antagonist, induces loss of HNF4α expression and hepatic steatosis in vivo. BI6015 is cytotoxic to human hepatocellular carcinoma (HCC).

In vitro
In vitro	BI-6015 is a hepatocyte nuclear factor 4α (HNF4α) antagonist, which represses insulin promoter activity through HNF4α antagonism.^[1]
Cell Research	Cell lines	T6PNE, MIN6 and HepG2 cells
	Concentrations	1.25, 2.5, 5, 10, 20 μM
	Incubation Time	5 or 48 h
	Method	T6PNE, MIN6, and HepG2 cells are cultured for 5 or 48 h in the presence of BI6015. HNF4a mRNA levels are normalized to 18S rRNA or GAPDH to control for nonspecific compound effects.

In Vivo
In vivo	BI-6015 induces loss of HNF4α expression and hepatic steatosis in mice, also induces apoptosis in a human hepatocellular carcinoma mouse model.^[1]
Animal Research	Animal Models	mice, human hepatocellular carcinoma mouse model
	Dosages	10-30 mg/kg
	Administration	i.p.

References
[1] Kiselyuk A, et al. Chem Biol. 2012 Jul 27;19(7):806-18.

References

[1] Kiselyuk A, et al. Chem Biol. 2012 Jul 27;19(7):806-18.

Chemical Information & Solubility

Molecular Weight	331.35	Formula	C₁₅H₁₃N₃O₄S
CAS No.	93987-29-2	SDF	--
Smiles	CC1=CC=C(C=C1[S](=O)(=O)[N]2C(=NC3=CC=CC=C23)C)[N+]([O-])=O
Storage (From the date of receipt)	3 years -20°C powder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years -20°C powder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 33 mg/mL ( (99.59 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.					In vivo Formulation Calculator
	Clear solution	5%DMSO 1 Corn oil	1.0mg/ml (3.02mM)	Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.	In vivo Formulation Calculator
Clear solution	5% DMSO 1 95% Corn oil	0.8mg/ml (2.41mM)	Taking the 1 mL working solution as an example, add 50 μL of 16 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	1.65mg/ml (4.98mM)	Taking the 1 mL working solution as an example, add 50 μL of 33 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

Preparing Stock Solutions

Molarity Calculator

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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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