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BMS309403

Name: BMS309403
Brand: Selleck Chemicals
SKU: S6622
Rating: 5 (4 reviews)

Catalog No.S6622 Purity:99.94%

BMS309403 is a small-molecule FABP4 inhibitor with nM affinity (Kd=4 nM for FABP4) and >100-fold selectivity against FABP5 as well as the heart isoform FABP3.

BMS309403 Chemical Structure

CAS No. 300657-03-8

Purity & Quality Control

Batch: Purity: 99.94%

99.94

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Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
BL21(DE3)	Function assay			Displacement of 1,8-ANS from His6-tagged FABP4 (unknown origin) expressed in Escherichia coli BL21(DE3) cells by fluorescence assay, Ki=0.22μM	27460668
BL21(DE3)	Function assay			Direct binding to His6-tagged FABP4 (unknown origin) expressed in Escherichia coli BL21(DE3) cells by isothermal titration calorimetry, Kd=2.05μM	27460668
aP2+/+ macrophage cells	Function assay		24 hrs	Decrease in MCP1 production in mouse aP2+/+ macrophage cells after 24 hrs	17554340
aP2-/-R macrophage cells	Function assay		24 hrs	Decrease in MCP1 production in mouse aP2-/-R macrophage cells (re-expression of aP2) after 24 hrs	17554340
THP1	Function assay	25 uM	3 days	Reduction of transformation of human THP1 cells to foam cells at 25 uM after 3 days relative to control	17554340
aP2+/+ macrophage cells	Function assay	25 uM		Reduction in total cholesterol ester content in mouse aP2+/+ macrophage cells at 25 uM relative to control	17554340
aP2-/-R macrophage cells	Function assay	25 uM		Reduction in total cholesterol ester content in mouse aP2-/-R macrophage cells (re-expression of aP2) at 25 uM relative to control	17554340
THP1	Function assay	25 uM		Increase in APOA1-mediated cholesterol in human THP1 cells at 25 uM relative to control	17554340
THP1	Function assay	25 uM		Increase in ABCA1 mRNA level in human THP1 cells at 25 uM relative to control	17554340
THP1	Function assay	25 uM		Increase in ABCA1 protein level in human THP1 cells at 25 uM relative to control	17554340
aP2+/+ macrophage cells	Function assay	25 uM		Increase in cholesterol efflux in mouse aP2+/+ macrophage cells at 25 uM relative to control	17554340
aP2-/-R macrophage cells	Function assay	25 uM		Increase in cholesterol efflux in mouse aP2-/-R macrophage cells (re-expression of aP2) at 25 uM relative to control	17554340
THP1	Function assay			Reduction of Mcp1 expression in human THP1 cells expressing aP2 relative to control	17554340
aP2+/+ macrophage cells	Function assay			Reduction of Mcp1 expression mouse aP2+/+ macrophage cells relative to control	17554340
aP2-/-R macrophage cells	Function assay			Reduction of Mcp1 expression mouse aP2-/-R macrophage cells (re-expression of aP2) relative to control	17554340
THP1	Function assay			Reduction of IL1-beta expression in human THP1 cells expressing aP2 relative to control	17554340
aP2+/+ macrophage cells	Function assay			Reduction of IL1-beta expressed in mouse aP2+/+ macrophage cells relative to control	17554340
aP2-/-R macrophage cells	Function assay			Reduction of IL1-beta expressed in mouse aP2-/-R macrophage cells (re-expression of aP2) relative to control	17554340
THP1	Function assay			Reduction of IL6 expression in human THP1 cells expressing aP2 relative to control	17554340
aP2+/+ macrophage cells	Function assay			Reduction of IL6 expression mouse aP2+/+ macrophage cells relative to control	17554340
aP2-/-R macrophage cells	Function assay			Reduction of IL6 expression mouse aP2-/-R macrophage cells (re-expression of aP2) relative to control	17554340
THP1	Function assay			Reduction of TNF expression in human THP1 cells expressing aP2 relative to control	17554340
aP2+/+ macrophage cells	Function assay			Reduction of TNF expression in mouse aP2+/+ macrophage cells relative to control	17554340
aP2-/-R macrophage cells	Function assay			Reduction of TNF expression mouse aP2-/-R macrophage cells (re-expression of aP2) relative to control	17554340
Click to View More Cell Line Experimental Data

Biological Activity

Description

BMS309403 is a small-molecule FABP4 inhibitor with nM affinity (Kd=4 nM for FABP4) and >100-fold selectivity against FABP5 as well as the heart isoform FABP3.

Targets

FABP4 ^[1]
(Cell-free assay)

4 nM(Kd)

In vitro
In vitro	Treatment of BMS309403 (FABP4 inhibitor) comobined with SSO (CD36 inhibitor) significantly decreases the breast cancer cell viability, proliferative, migratory, and invasive abilities over 72 h. Inhibiting either at recommended concentrations does not significantly decrease the breast cancer cell viability over 72 h. Treatment with both SSO and BMS309403 results in clustering of cells and increased lipid content, indicating an inability to metabolise lipids resulting potentially in lipotoxicity-induced apoptosis.^[1]
Cell Research	Cell lines	Humen breast cancer cell lines
	Concentrations	20 μM
	Incubation Time	72 h
	Method	Cell viability after CD36 knockout or treatment with SSO and BMS-309403 is determined by seeding 2500 cells in 96-well plate, and cultured for 24 h, after which treatment agent is added at appropriate concentration and maintained for 72 h. Cell viabilities is evaluated at 6, 12, 24, 36, 48, 60 and 72 h using the EZ-CYTOX cell viability kit.

In Vivo
In vivo	Treatment with either BMS309403 or SSO alone decreases the rate of tumour formation and the combination of BMS309403 and SSO significantly decreased the rate of tumour formation.

References

Chemical Information & Solubility

Molecular Weight	474.55	Formula	C₃₁H₂₆N₂O₃
CAS No.	300657-03-8	SDF	--
Smiles	CCC1=C(C(=NN1C2=CC=CC=C2C3=CC(=CC=C3)OCC(=O)O)C4=CC=CC=C4)C5=CC=CC=C5
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 : 95 mg/mL ( (200.18 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 18 mg/mL

Water : 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 40%PEG300 2 5%Tween80 3 50%ddH2O	6.0mg/ml (12.64mM)	Taking the 1 mL working solution as an example, add 50 μL of 120 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.	In vivo Formulation Calculator
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	4.75mg/ml (10.01mM)	Taking the 1 mL working solution as an example, add 50 μL of 95 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.
Clear solution	5% DMSO 1 95% Corn oil	0.475mg/ml (1.00mM)	Taking the 1 mL working solution as an example, add 50 μL of 9.5 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.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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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

%DMSO+ %

Calculation results:

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

Tel: +1-832-582-8158 Ext:3
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