Gboxin |
| Catalog No.GC33234 |
Gboxin은 암세포의 산화 인산화(OXPHOS)를 저해하는 저해제이고 교모세포종(GBM)을 저해할 수 있다.
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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Gboxin은 암세포의 산화 인산화(OXPHOS)를 저해하는 저해제이고 교모세포종(GBM)을 저해할 수 있다. Gboxin은 양전하를 포함하는 삼환형 벤즈이미다졸리움 화합물로 여러 암세포주들의 성장을 특이적으로 저해할 수 있다[2]. Gboxin은 F0F1 ATPase 복합체 V의 활성을 저해함으로써 GBM의 성장을 특이적으로 저해하지만 혈액순환 부전, 혈뇌장벽(BBB) 및 비특이적 GBM 조직/세포 흡수로 인해 항GBM 효과는 심각하게 제한된다[3]. Gboxin은 포도당 흡수와 소비를 조절하는 조절 인자이고 산화 인산화(OXPHOS)의 표적으로 작용하는 티오레독신 상호 작용 단백질의 발현을 저해할 수 있다[4].
체외 실험에서 0-15 µM의 Gboxin으로 HTS 세포, 일차 MEFs, 성상세포를 96시간 처리하면 HTS 세포의 성장을 유의하게 저해하지만 원발 MEFs 세포 및 잠재적인 초전도 세포의 성장은 저해하지 않고 HTS 세포의 미토콘드리아 막 전위를 감소시킨다[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.
| 세포 실험 [1]: | |
세포 라인 | HTS 세포, 일차 MEFs, 성상세포 |
제조 방법 | HTS 세포, 일차 MEFs, 성상세포를 96시간 동안 점점 높은 농도(0, 185, 555, 1667, 5000, 15000 nM)의 Gboxin에 노출시킨 후 세포 생존력 시험을 실시했습니다. |
반응 조건 | 0, 185, 555, 1667, 5000, 15000nM; 96시간 동안 |
응용 분야 | Gboxin은 HTS 세포의 성장을 특이적으로 억제하지만 순환 일차 MEFs 또는 성상 세포의의 성장은 저해하지 않습니다. |
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. |
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| 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 | 0.509 mL | 2.5448 mL | 5.0896 mL |
| 10 mM | 0.2545 mL | 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 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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 23 reference(s) in Google Scholar.)
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