Gboxin is an inhibitor of oxidative phosphorylation that targets glioblastoma, inhibits the activity of F0F1 ATP synthase, with antitumour activity. Gboxin rapidly and irreversibly compromises oxygen consumption in glioblastoma cells. Gboxin relies on its positive charge to associate with mitochondrial oxidative phosphorylation complexes in a manner that is dependent on the proton gradient of the inner mitochondrial membrane. Gboxin-resistant cells require a functional mitochondrial permeability transition pore that regulates pH and thus impedes the accumulation of Gboxin in the mitochondrial matrix.
| Molecular Weight | 392.96 |
| Formula | C22H33ClN2O2 |
| CAS Number | 2101315-36-8 |
| Solubility (25°C) | DMSO 35 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related ATPase Products |
|---|
| Prilocaine acetate
Prilocaine acetate, an amino amide, is a Na/K-ATPase inhibitor. |
| Chamigrenol
Chamigrenol is a Na+/K+-ATPase inhibitor with an IC50 value of 15.9 μg/mL. |
| ZW290
ZW290 is a compound to activate brown adipose tissue (BAT) thermogenic function. |
| ATP synthase inhibitor 2 TFA
ATP synthase inhibitor 2 TFA is a Pseudomonas aeruginosa (PA) ATP synthase inhibitor (IC50=10 μg/mL). |
| Apicularen B
Apicularen B is a cytotoxic macrolide produced by Archangium gephyra and is also a specific V-ATPase inhibitor. Its IC50 values range from 0.2 to 1.2 μg/mL and it exhibits weak activity against some Gram-positive bacteria. |
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