Gboxin |
Catalog No.GC33234
One-Click Copy Product Info
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Gboxin es un inhibidor de la fosforilación oxidativa (OXPHOS) en las células cancerosas y puede ser el objetivo de inhibir el glioblastoma (GBM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2101315-36-8
Sample solution is provided at 25 µL, 10mM.
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Gboxin es un inhibidor de la fosforilación oxidativa (OXPHOS) en las células cancerosas y puede ser el objetivo de inhibir el glioblastoma (GBM)[1]. Gboxin es un compuesto de benzimidazol trisustituido que contiene una carga positiva que puede inhibir específicamente el crecimiento de múltiples líneas celulares cancerosas[2]. Gboxin inhibe específicamente el crecimiento de GBM al inhibir la actividad del complejo V de ATPase F0F1, pero su efecto anti-GBM está severamente limitado por la mala circulación sanguínea, la barrera hematoencefálica (BBB) y la absorción de tejido/células de GBM no específica[3]. Gboxin puede inhibir la expresión de la proteína que interactúa con la tioredoxina, que es un regulador de la absorción y el consumo de glucosa y un objetivo de la fosforilación oxidativa OXPHOS[4].
In vitro, el tartamiento con Gboxin (0-15μM) de células HTS, células MEF primarias y astrocitos durante 96h inhibió significativamente el crecimiento de células HTS, pero no inhibió el crecimiento de MEFs primarios y astrocitos, y redujo el potencial de membrana mitocondrial en las células HTS[5].
References:
[1]?Zou Y, Sun Y, Wang Y, et al. Cancer cell-mitochondria hybrid membrane coated Gboxin loaded nanomedicines for glioblastoma treatment[J]. Nature Communications, 2023, 14(1): 4557.
[2]?Yao S, Yin J, Liu W, et al. A novel Gboxin analog induces OXPHOS inhibition and mitochondrial dysfunction-mediated apoptosis in diffuse large B-cell lymphoma[J]. Bioorganic Chemistry, 2022, 127: 106019.
[3]?Jiao X, Yu X, Gong C, et al. Erythrocyte-cancer hybrid membrane-camouflaged mesoporous silica nanoparticles loaded with gboxin for glioma-targeting therapy[J]. Current Pharmaceutical Biotechnology, 2022, 23(6): 835-846.
[4]?Crunkhorn S. Targeting cancer cell metabolism in glioblastoma[J]. Nature Reviews Cancer, 2019, 19(5): 250-250.
[5] Shi Y, Lim S K, Liang Q, et al. Gboxin is an oxidative phosphorylation inhibitor that targets glioblastoma[J]. Nature, 2019, 567(7748): 341-346.
| Experimentos celulares [1]: | |
Líneas celulares | Células HTS , MEFs primarios, astrocitos |
Método de preparación | Las células HTS, los MEFs y los astrocitos estuvieron expuestos a dosis crecientes (0, 185, 555, 1667, 5000, 15000nM) de Gboxin durante 96h, seguidas de ensayos de viabilidad celular. |
Condiciones de reacción | 0, 185, 555, 1667, 5000, 15000nM; 96h |
Áreas de aplicación | Gboxin inhibe específicamente el crecimiento de las células HTS, pero no el de los MEFs primarios o astrocitos en bicicleta. |
References: | |
| Cas No. | 2101315-36-8 | SDF | |
| Canonical SMILES | O=C(O[C@H]1[C@H](C(C)C)CC[C@@H](C)C1)CN2C(CC)=[N+](C)C3=CC=CC=C23.[Cl-] | ||
| Formula | C22H33ClN2O2 | M.Wt | 392.96 |
| Solubility | DMSO : 32.5 mg/mL (82.71 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.5448 mL | 12.7239 mL | 25.4479 mL |
| 5 mM | 509 μL | 2.5448 mL | 5.0896 mL |
| 10 mM | 254.5 μL | 1.2724 mL | 2.5448 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
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 saline, 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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 23 reference(s) in Google Scholar.)