Gboxin

For research use only.

Catalog No.S8828

Gboxin Chemical Structure

Molecular Weight(MW): 392.96

Gboxin is an inhibitor of oxidative phosphorylation in cancer cells. It specifically inhibits the growth of primary mouse and human glioblastoma cells but not that of mouse embryonic fibroblasts or neonatal astrocytes.

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Biological Activity

Description Gboxin is an inhibitor of oxidative phosphorylation in cancer cells. It specifically inhibits the growth of primary mouse and human glioblastoma cells but not that of mouse embryonic fibroblasts or neonatal astrocytes.
Targets
oxidative phosphorylation [1]
()
In vitro

Gboxin rapidly and irreversibly compromises GBM oxygen consumption. Reliant on its positive charge, Gboxin associates with mitochondrial oxidative phosphorylation complexes in a proton gradient dependent manner and inhibits F0F1 ATP synthase activity. Gboxin targets unique features of mitochondrial pH in GBM and other cancer cells, independent of their genetic composition, and exerts its tumor cell specific toxicity in primary culture and in vivo[1].

Assay
Methods Test Index PMID
Western blot
ATF4 / p-S6 / S6 ; 

PubMed: 30842654     


HTS specific upregulation of ATF4 and suppression of phospho-S6 (p-S6) by western blot analyses (DMSO or Gboxin; 1 μM; 6 hours ). n=3.

pAMPK / AMPK / pACC-79 / ACC ; 

PubMed: 30842654     


Western blot analyses indicating Gboxin (1 μM) mediated activation of phospho-AMPK (pAMPK) and phospho-ACC-79 (pACC-79) in HTS cells but not MEFs treated for the indicated time periods. n=2.

30842654
Growth inhibition assay
Cell viability ; 

PubMed: 30842654     


Cell viability assays (% Cell viability) for HTS, MEF and astrocyte cells exposed to increasing doses of Gboxin (96 hours. Mean ± SD; n=3).

30842654

Protocol

Cell Research:

[1]

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  • Cell lines: HTS, MEF and astrocyte cells
  • Concentrations: 0-15 μM
  • Incubation Time: 96 h
  • Method:

    --


    (Only for Reference)

Solubility (25°C)

In vitro DMSO 39 mg/mL (99.24 mM)
Water 2 mg/mL (5.08 mM)
Ethanol '79 mg/mL

* 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 392.96
Formula

C22H33ClN2O2

CAS No. 2101315-36-8
Storage powder
in solvent
Synonyms N/A
Smiles [Cl-].CCC1=[N+](C)C2=CC=CC=C2[N]1CC(=O)OC3CC(C)CCC3C(C)C

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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