research use only

Gboxin OXPHOS inhibitor

Cat.No.S8828

Gboxin is an inhibitor of oxidative phosphorylation in cancer cells. This compound inhibits the activity of F0F1 ATP synthase. It specifically inhibits the growth of primary mouse and human glioblastoma cells but not that of mouse embryonic fibroblasts or neonatal astrocytes.
Gboxin OXPHOS inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 392.96

Quality Control

Batch: S882801 Ethanol]79 mg/mL]false]DMSO]39 mg/mL]false]Water]2 mg/mL]false Purity: 99.76%
99.76

Chemical Information, Storage & Stability

Molecular Weight 392.96 Formula

C22H33ClN2O2

Storage (From the date of receipt) 3 years -20°C powder
CAS No. 2101315-36-8 -- Storage of Stock Solutions

Synonyms N/A Smiles CCC1=[N+](C2=CC=CC=C2N1CC(=O)OC3CC(CCC3C(C)C)C)C.[Cl-]

Solubility

In vitro
Batch:

Ethanol : 79 mg/mL

DMSO : 39 mg/mL ( (99.24 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 2 mg/mL

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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% DMSO % % Tween 80 % ddH2O
%DMSO %

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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.

Mechanism of Action

Targets/IC50/Ki
oxidative phosphorylation [1]
F0F1 ATP synthase [1]
In vitro

Gboxin rapidly and irreversibly compromises GBM oxygen consumption. Reliant on its positive charge, this compound associates with mitochondrial oxidative phosphorylation complexes in a proton gradient dependent manner and inhibits F0F1 ATP synthase activity. It 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].

References

Applications

Methods Biomarkers Images PMID
Western blot ATF4 / p-S6 / S6 pAMPK / AMPK / pACC-79 / ACC S8828-WB1 30842654
Growth inhibition assay Cell viability S8828-viability1 30842654

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