2-Deoxy-D-glucose
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
2-Deoxy-D-glucose(2DG)（葡萄糖模拟物）是一个竞争性糖酵解的抑制剂[1 - 3]。细胞毒性试验中对KIT-阳性细胞株GIST882和GIST430的IC50值分别为0.5 μM和2.5 μM[4]。
糖酵解是ATP-产生的一个子系统[5]。
如果2DG/葡萄糖的生理相关比率是0.8，在包含25 mmol/L葡萄糖的DMEM中生长的FaDu细胞中葡萄糖代谢将会被抑制。相比于对照细胞，2DG处理导致总谷胱甘肽含量减少了30%到40%，细胞被杀死了32%[2]。2DG以浓度依赖式地抑制PEDV传播，诱导Vero细胞内质网应激反应。2-DG没有明显地影响病毒数。但进一步的研究表明，2-DG降低病毒蛋白质翻译，这意味着在病毒感染的早期阶段，2-DG可能影响病毒的复制。此外，在病毒感染的早期阶段2-DG增加了CD13表达水平[6]。
在体内，2-DG在人骨肉瘤和非小细胞肺癌中增加阿霉素和紫杉醇的疗效，可阻碍肿瘤的生长，延长存活时间[3]。在金头鲷中，2-DG显著地增加血糖水平，引起非统计性显著降低头肾白细胞呼吸活性。头肾白细胞血清中过氧化物酶活性与对照相比无显著差异[7]。
参考文献：
[1]. John Laszlo, William R. Harlan, Robert F. Klein, et al. The Effect of 2-Deoxy-D-Glucose Infusions on Lipid and Carbohydrate Metabolism in Man. J Clin Invest., 1961, 40(1):171-176.
[2]. Andrean L. Simons, Iman M. Ahmad, David M. Mattson, et al. 2-Deoxy-D-Glucose Combined with Cisplatin Enhances Cytotoxicity via Metabolic Oxidative Stress in Human Head and NeckCancer Cells. Cancer Research, 2007, 67(7): 3364-3371.
[3]. Gregory Maschek, Niramol Savaraj, Waldemar Priebe, et al. 2-Deoxy-D-glucose Increases the Efficacy of Adriamycin and Paclitaxel in Human Osteosarcoma and Non-Small Cell Lung Cancers In Vivo. Cancer Research, 2004, 64:31-34.
[4]. Thomas Mühlenberg, Susanne Grunewald, Jürgen Treckmann, et al. Inhibition of KIT-Glycosylation by 2-Deoxyglucose Abrogates KIT-Signaling and Combination with ABT-263 Synergistically Induces Apoptosis in Gastrointestinal Stromal Tumor. PLOS ONE, 2015, 10(3):e0120531.
[5]. R. J. Connett, C. R. Honig, T. E. Gayeski, et al. Defining hypoxia: a systems view of VO2, glycolysis, energetics, and intracellular PO2. Journal of Applied Physiology, 1990, 68(3): 833-842.
[6]. Yue Wang, Jia-rong Li, Ming-xia Sun, et al. Triggering unfolded protein response by 2-Deoxy-D-glucose inhibits porcine epidemic diarrhea virus propagation. Antiviral Research, 2014, 106: 33–41.
[7]. F.A. Guardiola, R. Cerezuela, J. Meseguer, et al. Effects of 2-deoxy-D-glucose on the immune system of seabream (Sparus aurata L.). Fish & Shellfish Immunology, 2011, 30: 592-599.
- 1. Ye Liu, Wenna Chi, et al. "Ablation of Proton/glucose Exporter SLC45A2 Enhances Melanosomal Glycolysis to Inhibit Melanin Biosynthesis and Promote Melanoma Metastasis." J Invest Dermatol . 2022 Apr 23;S0022-202X(22)00301-3. PMID: 35469906
- 2. Fang Wang, Jing Zhang, et al. "2-Deoxy-D-glucose impedes T cell-induced apoptosis of keratinocytes in oral lichen planus." J Cell Mol Med. 2021 Nov;25(21):10257-10267. PMID: 34672419
- 3. Beatriz Lapa, Ana Cristina Gonçalves, et al. "Acute myeloid leukemia sensitivity to metabolic inhibitors: glycolysis showed to be a better therapeutic target." Med Oncol. 2020 Jul 28;37(8):72. PMID: 32725458
- 4. Wang F, Zhang J, et al. "HIF1α/PLD2 axis linked to glycolysis induces T-cell immunity in oral lichen planus." Biochim Biophys Acta Gen Subj. 2020;1864(7):129602. PMID: 32205175
- 5. Wang F, Zhang J, et al. "The mTOR-glycolytic pathway promotes T-cell immunobiology in oral lichen planus." Immunobiology. 2020;225(3):151933. PMID: 32201095
- 6. Li X, Zhang Y, et al. "Enhanced glucose metabolism mediated by CD147 contributes to immunosuppression in hepatocellular carcinoma." Cancer Immunol Immunother. 2020;10.1007/s00262-019-02457-y. PMID: 31965268
- 7. Barot S, Abo-Ali EM, et al. "Inhibition of glycogen catabolism induces intrinsic apoptosis and augments multikinase inhibitors in hepatocellular carcinoma cells." Exp Cell Res. 2019 Aug 15;381(2):288-300. PMID: 31128107
- 8. Tian C, Yuan Z, et al. "Inhibition of glycolysis by a novel EGFR/HER2 inhibitor KU004 suppresses the growth of HER2+ cancer." Exp Cell Res. 2017 May 19. pii: S0014-4827(17)30297-5. PMID: 28532652
| Storage | Store at -20°C |
| M.Wt | 164.16 |
| Cas No. | 154-17-6 |
| Formula | C6H12O5 |
| Solubility | ≥105 mg/mL in H2O; ≥2.37 mg/mL in EtOH with gentle warming and ultrasonic; ≥8.2 mg/mL in DMSO |
| Chemical Name | (4R,5S,6R)-6-(hydroxymethyl)tetrahydro-2H-pyran-2,4,5-triol |
| SDF | Download SDF |
| Canonical SMILES | [H][C@]([C@](C1([H])[H])([H])O[H])([C@](C([H])([H])O[H])([H])OC1([H])O[H])O[H] |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验 [1, 2]: | |
|
细胞系 |
GIST细胞系，感染PEDV的Vero细胞 |
|
溶解方法 |
该化合物在DMSO中的溶解度大于8.2 mg/mL。若获取更高浓度的溶液，可在37℃下孵育10分钟，随后在超声波浴中摇匀。-20℃以下可储存数月。 |
|
反应条件 |
5 mM，10 mM，24 h |
|
应用 |
2-DG以剂量依赖性方式诱导细胞在G1期的积累及减少S期细胞，IC50值为0.5 μM-2.5 μM之间。 2-DG抑制Vero细胞中的PEDV复制和基因表达。2-DG（10 mM，24 h）影响病毒包装。 |
| 动物实验 [3]: | |
|
动物模型 |
人类骨肉瘤和非小细胞肺癌的裸鼠异种移植模型 |
|
给药剂量 |
500 mg/kg，腹腔注射，每周3次 (周一、周三、周五) |
|
应用 |
与单独使用2-DG相比，ADR (6 mg/kg, i.v.) + 2-DG (500 mg/kg, i.p.) 组合使用显著降低肿瘤生长。 |
|
注意事项 |
由于实验环境的不同，实际溶解度可能与理论值略有不同，请测试室内所有化合物的溶解度。 |
|
References: [1]. Mühlenberg T, Grunewald S, Treckmann J, et al. Inhibition of KIT-glycosylation by 2-deoxyglucose abrogates KIT-signaling and combination with ABT-263 synergistically induces apoptosis in gastrointestinal stromal tumor[J]. PloS one, 2015, 10(3): e0120531. [2]. Wang Y, Li J, Sun M, et al. Triggering unfolded protein response by 2-Deoxy-D-glucose inhibits porcine epidemic diarrhea virus propagation[J]. Antiviral research, 2014, 106: 33-41. [3]. Gregory Maschek, Niramol Savaraj, Waldemar Priebe, et al. 2-Deoxy-D-glucose Increases the Efficacy of Adriamycin and Paclitaxel in Human Osteosarcoma and Non-Small Cell Lung Cancers In Vivo. Cancer Research, 2004, 64:31-34. |
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质量控制和MSDS
- 批次:
化学结构
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