Gboxin

Gboxin is an inhibitor of oxidative phosphorylation in cancer cells, which have a higher mitochondrial proton gradient and pH compared with non-cancerous cells.¹ It increases the mitochondrial membrane potential and reduces the oxygen consumption rate, which can be bypassed by the proton ionophore FCCP (Item No. 15218), indicating that it inhibits F₀F₁ ATP synthase/complex V. Gboxin decreases viability of three primary mouse glioblastoma cell lines (IC₅₀s = ~150 nM) and three patient-derived glioblastoma cultures (IC₅₀s = ~1 µM) but does not affect the viability of primary mouse embryonic fibroblasts or astrocytes. It halts the cell cycle in the G₁/G₀ phase and induces apoptosis of primary low-passage glioblastoma cells pooled from multiple tumors.

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1. Shi, Y., Lim, S.K., Liang, Q., et al. Gboxin is an oxidative phosphorylation inhibitor that targets glioblastoma. Nature 567(7748), 341-346 (2019).