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

製品コードS4701 バッチS470111

化学情報

	Synonyms	2-deoxyglucose, NSC 15193, 2-Deoxy-D-arabino-hexose, D-Arabino-2-deoxyhexose	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₆H₁₂O₅
	分子量	164.16	CAS No.	154-17-6
Solubility (25°C)*	体外	DMSO	33 mg/mL (201.02 mM)
		Water	33 mg/mL (201.02 mM)
		Ethanol	8 mg/mL (48.73 mM)
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	グルコースアナログである2-DG (2-Deoxy-D-glucose)は、抗ウイルス活性を持つ解糖系阻害剤です。2-Deoxy-D-glucoseはアポトーシスを誘導し、単純ヘルペスウイルス1型（HSV-1）受容体の発現を阻害します。
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.
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.

プロトコル(参考用のみ)

細胞アッセイ	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.
動物実験	動物モデル	Adult C57BL/6J mice
	投薬量	1000 mg/kg
	投与方法	i.p.

参考

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/

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カスタマーフィードバック

: Data from [Data independently produced by , , Int J Oncol, 2018, 52(6):1899-1911]

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人間や獣医の診断であるか治療的な使用のためにでない。

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