Bedaquiline

Catalog No.S5623 Synonyms: TMC-207, R207910

Bedaquiline Chemical Structure

Molecular Weight(MW): 555.50

Bedaquiline, a diarylquinoline, binds to subunit c of mycobacterial ATP synthase and inhibits its activity. It is highly selective for mycobacterial ATP synthase enzyme compared to homologous eukaryotic enzyme (Selectivity Index >20 000).

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Biological Activity

Description Bedaquiline, a diarylquinoline, binds to subunit c of mycobacterial ATP synthase and inhibits its activity. It is highly selective for mycobacterial ATP synthase enzyme compared to homologous eukaryotic enzyme (Selectivity Index >20 000).
Targets
mycobacterial ATP synthase [1]
()
In vitro

Bedaquiline targets against Mycobacterial ATP synthase complex[1]. Bedaquiline has anti-cancer activity, directed against Cancer Stem-like Cells (CSCs). Bedaquiline treatment of MCF7 breast cancer cells inhibits mitochondrial oxygen-consumption, as well as glycolysis, but induces oxidative stress. Bedaquiline reduces mitochondrial membrane potential, with a significant rise in ROS levels. It specifically inhibits mitochondrial respiration in cancer cells, while enhancing mitochondrial function in normal cells. Bedaquiline dramatically inhibits oxygen consumption and ATP production in the low micromolar range. In addition, bedaquiline treatment also reduced aerobic glycolysis[2].

In vivo Bedaquiline follows triphasic elimination and characterized by an outstandingly long terminal half-life, around 173 h in humans[1].

Protocol

Cell Research:

[1]

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  • Cell lines: MCF-7 cells
  • Concentrations: 1μM and 10 μM
  • Incubation Time: 48 h
  • Method:

    MCF7 cells were treated with 10μM bedaquiline for 48 hours. Vehicle alone (DMSO) control cells were processed in parallel. After 48 hours, cells were washed with PBS, and incubated with CM-H2DCFDA (diluted in PBS/CM to a final concentration of 1 μM) for 20 minutes at 37°C. All subsequent steps were performed in the dark. Cells were rinsed, harvested, and re-suspended in PBS/CM. Cells were then analyzed by flow cytometry.


    (Only for Reference)

Solubility (25°C)

In vitro DMSO 12 mg/mL (21.6 mM)
Ethanol 3 mg/mL (5.4 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 555.50
Formula

C32H31BrN2O2

CAS No. 843663-66-1
Storage powder
in solvent
Synonyms TMC-207, R207910

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID