2-DG (2-Deoxy-D-glucose)

別名:2-deoxyglucose, NSC 15193, 2-Deoxy-D-arabino-hexose, D-Arabino-2-deoxyhexose

2-DG (2-Deoxy-D-glucose), an analog of glucose, is a glycolytic inhibitor with antiviral activity. 2-Deoxy-D-glucose induces apoptosis and inhibits Herpes Simplex Virus type-1 (HSV-1) receptor expression.

2-DG (2-Deoxy-D-glucose)化学構造

CAS No. 154-17-6

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2-DG (2-Deoxy-D-glucose)関連製品

Carbohydrate Metabolism阻害剤の選択性比較

生物活性

製品説明 2-DG (2-Deoxy-D-glucose), an analog of glucose, is a glycolytic inhibitor with antiviral activity. 2-Deoxy-D-glucose induces apoptosis and inhibits Herpes Simplex Virus type-1 (HSV-1) receptor expression.
Targets
glycolysis
In Vitro
In vitro 2-Deoxy-D-glucose (2-DG) activates AKT function through phosphatidylinositol 3-kinase (PI3K) and is independent of glycolysis or mTOR inhibition. Its treatments disrupt the binding between insulin-like growth factor 1 (IGF-1) and IGF-binding protein 3 (IGFBP3) so that the free form of IGF-1 could be released from the IGF-1·IGFBP3 complex to activate IGF-1 receptor (IGF1R) signaling. 2-DG-induced activation of many survival pathways can be jointly attenuated through IGF1R inhibition. This compound also induces time- and dose-dependent ERK phosphorylation. It is readily transported into cells and is phosphorylated by hexokinase, but cannot be metabolized further and accumulates in the cell. This leads to ATP depletion and the induction of cell-death. 2DG significantly suppresses proliferation, causes apoptosis and reduces migration of murine endothelial cells, inhibiting formation of lamellipodia and filopodia and causing disorganization of F-actin filaments in murine endothelial cell.
細胞実験 細胞株 H460 or H157 cells
濃度 5 mM
反応時間 48 h
実験の流れ

H460 or H157 cells (2×103) are seeded in 96-well cell culture plates and treated with 5 mM 2-Deoxy-D-glucose (2-DG) only, 5 or 10 μM IGF1R inhibitor II only, or a combination of it and IGF1R inhibitor II. Cell growth inhibition is determined after 48 h by the CellTiter 96® AQueous nonradioactive cell proliferation assay.

In Vivo
In Vivo Treatment of cancer patients with relatively high doses of 2-Deoxy-D-glucose (2-DG) (greater than 200 mg/kg) was largely ineffective in managing tumor growth. Side effects of this compound included elevated blood glucose levels, progressive weight loss with lethargy, and behavioral symptoms of hypoglycemia. It enhances isoflurane-induced loss of righting reflex in mice. By reducing metabolism, 2-DG treatment can decrease body temperature in rodent, enhancing sensitivity to anesthetics. A diet containing it significantly increased serum ketone body level and brain expression of enzymes required for ketone body metabolism. The 2-DG-induced maintenance of mitochondrial bioenergetics was paralleled by simultaneous reduction in oxidative stress. Further, treated mice exhibited a significant reduction of both amyloid precursor protein (APP) and amyloid beta (Aβ) oligomers, which was paralleled by significantly increased α-secretase and decreased γ-secretase expression, indicating that this compound induced a shift towards a non-amyloidogenic pathway. It increased expression of genes involved in Aβ clearance pathways, degradation, sequestering, and transport. Concomitant with increased bioenergetic capacity and reduced β-amyloid burden, 2-DG significantly increased expression of neurotrophic growth factors, BDNF and NGF, thus reduces pathology in female mouse model of Alzheimer's disease.
動物実験 動物モデル Adult C57BL/6J mice
投与量 1000 mg/kg
投与経路 i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02558140 Completed
Neoplasms
Hoffmann-La Roche
October 11 2015 Phase 1
NCT01998841 Completed
Alzheimer''s Disease
Genentech Inc.|Banner Alzheimer''s Institute|National Institute on Aging (NIA)
December 20 2013 Phase 2
  • https://pubmed.ncbi.nlm.nih.gov/19574224/
  • https://pubmed.ncbi.nlm.nih.gov/19032781/
  • https://pubmed.ncbi.nlm.nih.gov/25390277/
  • https://pubmed.ncbi.nlm.nih.gov/21747957/
  • https://pubmed.ncbi.nlm.nih.gov/26398947/

化学情報

分子量 164.16 化学式

C6H12O5

CAS No. 154-17-6 SDF Download 2-DG (2-Deoxy-D-glucose) SDFをダウンロードする
Smiles C(C=O)C(C(C(CO)O)O)O
保管

In vitro
Batch:

DMSO : 500 mg/mL ( (3045.8 mM); Warmed with 50℃ water bath; Ultrasonicated; 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : 83 mg/mL

Ethanol : 8 mg/mL

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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