Home Metabolism FABP inhibitor BMS309403 For research use only.

BMS309403

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

BMS309403 Chemical Structure

CAS No. 300657-03-8

Purity & Quality Control

BMS309403 Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation 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.

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

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


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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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