2-Deoxy-D-glucose

Biological Activity

2-Deoxy-D-Glucose (2-DG) is a glucose analog that inhibits glycolysis via its actions on hexokinase, the rate limiting step of glycolysis. It is phosphorylated by hexokinase to 2-DG-P which cannot be further metabolized by phosphoglucose isomerase. Most tumor cells showed higher DG uptake and 3-O-MG transport than the human fibroblast cells. The 2DG6P content in isolated rat soleus muscle after incubation with 2-deoxyglucose (2DG) was increased in a dose-dependent manner by insulin (ED(50) = 0.6 mU/ml), the maximum response being about 5 times that of the basal content in vitro. 2-DG increased mitochondrial dysfunction and upregulated Bax/Bcl-2, promoting cytochrome c release to initiate procaspase 3 cleavage induced by buforin IIb.

2-DG plus BCNU significantly suppressed tumor growth with lower side effects compared with BCNU alone in tumor-bearing mice. 2-DG also exerts anticonvulsant effects in vivo against perforant path kindling in rats. Rats fed the 2-DG diet exhibited significant reductions in resting BP, attenuated BP responses during stress, and accelerated recovery to baseline after stress. Plasma concentrations of ACTH and corticosterone were elevated under nonstress conditions in rats fed the 2-DG diet and exhibited differential responses to single (enhanced response) and multiple (reduced response) stress sessions compared with rats fed control rat chow ad libitum. The 2-DG diet improved glucose metabolism, as indicated by decreased concentrations of blood glucose and insulin under nonstress conditions, but glucose and insulin responses to stress were maintained.

DEN and 2-DG model in the rat
Male 10–12 week old Sprague Dawley rats, weighing 220–240 g were maintained at an animal facility under pathogen-free conditions. To induce HCC, N-diethylnitrosamine (DEN) at a dilution of 1/10,000 (95 mg/l), was added to the drinking water of rats for 13 weeks. Subsequently, the water was replaced by normal sterile water and certain rats received 0.75 g/kg 2-DG, dissolved in normal saline solution via intraperitoneal (IP) injection once every 3 days until the end of the 17th week after initial DEN administration. A total of 30 rats (control group, n=5; 2-DG group, n=5; DEN group, n=10; DEN+2-DG group, n=10) were kept and assessed for survival time and 20 rats (DEN group, n=10; DEN+2-DG group, n=10) were sacrificed through cervical dislocation at 17 weeks in order to observe their primary liver tumors. The tumors were measured with a micrometer up to a maximum diameter of 3 mm. The tumor volumes were calculated using the following formula: Volume=axb2/2 (‘a’ is the maximal diameter and ‘b’ was the minimal diameter).
https://www.spandidos-publications.com/mmr/11/3/1917

2-DG in an Animal Model With CIA
Bovine type II collagen (2 mg/ml) was mixed with complete Freund's adjuvant (2 mg/ml) at a one to one ratio. One hundred microliters of emulsion was injected intradermally into six-week-old Sprague–Dawley (SD) rats at the tail root (n=12). One week later, these rats received an intradermal booster injection with 100 μL of emulsion of bovine type II collagen and incomplete Freund's adjuvant at a one to one ratio. Other rats injected with phosphate-buffered saline (PBS) were used as healthy controls (n=12). An aqueous solution of 2-DG (100 mg/mL) was prepared by dissolving 0.1 g of 2-DG powder in sterile water and was intraperitoneally injected on 3 day before the first injection of collagen. Those rats receiving collagen injections were intraperitoneally administered PBS (n=6) or 2-DG (n=6) (50 mg/kg) twice per week (a total of 6 times, once every 3.5 days). Additionally, those healthy rats receiving the PBS injection in place of collagen were simultaneously treated with 2-DG as a control (n=6). Clinical arthritis scores were calculated according to paw thickness measurements and histologic evidence. The rats were sacrificed on the 21 day after the first 2-DG injection. The hind paws of the rats were collected, fixed in 4% paraformaldehyde and embedded in paraffin for histochemical analysis.
https://pmc.ncbi.nlm.nih.gov/articles/PMC8440946/

Product Citations

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  Cell Death Dis. 2025 Aug 12;16(1):613.

  Degradation of IRF6 by TRIM59 in tumor cells triggers PGM1-mediated glycolysis to regulate cell proliferation in neuroblastoma
  2-Deoxy-D-glucose purchased from AbMole

• 

  Commun Biol. 2025 Aug 30;8(1):1314.

  Histone H3K27 acetylation mediated by KAT8 maintains antiviral trained immunity in shrimp induced by inactivated white spot syndrome virus
  2-Deoxy-D-glucose purchased from AbMole

• 

  Mol Med Rep. 2025 Aug 29;32(5):301.

  Aberrant activation of the PI3K/AKT/HIF‑1α pathway promotes glycolysis and lenvatinib resistance in liver cancer
  2-Deoxy-D-glucose purchased from AbMole

• 

  J Transl Med. 2024 Aug 12;22(1):754.

  Paired organoids from primary gastric cancer and lymphatic metastasis are useful for personalized medicine
  2-Deoxy-D-glucose purchased from AbMole

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  Transl Cancer Res. 2023 Oct 31;12(10):2823-2836.

  Ubenimex suppresses glycolysis mediated by CD13/Hedgehog signaling to enhance the effect of cisplatin in liver cancer
  2-Deoxy-D-glucose purchased from AbMole

• 

  Front Immunol. 2021 Feb 25;12:620365.

  Circulating Neutrophil Dysfunction in HBV-Related Acute-on-Chronic Liver Failure
  2-Deoxy-D-glucose purchased from AbMole

• 

  Redox Biol. 2020 Oct;37:101761.

  Stat2-Drp1 mediated mitochondrial mass increase is necessary for pro-inflammatory differentiation of macrophages
  2-Deoxy-D-glucose purchased from AbMole

• 

  Cell Death Dis. 2020 Oct 23;11(10):902.

  The miR-30a-5p/CLCF1 axis regulates sorafenib resistance and aerobic glycolysis in hepatocellular carcinoma
  2-Deoxy-D-glucose purchased from AbMole

Protocol (for reference only)

Cell Experiment
Cell lines	T cells
Preparation method	Activated T cells (1 × 10^6 cells/ml) were cultured with 2-DG (1 or 5 mM) or/and Rapamycin (100 nM) for 24 h. 2-DG and Rapamycin were dissolved in dimethylsulfoxide (DMSO).
Concentrations	1 or 5 mM
Incubation time	24 h

Animal Experiment
Animal models	Wild-type C57BL/6J mice
Formulation	Saline
Dosages	1000 mg/kg
Administration	Intraperitoneally

Chemical Information

Molecular Weight	164.16
Formula	C6H12O5
CAS Number	154-17-6
Solubility (25°C)	Water 30 mg/mL DMSO 15 mg/mL
Storage	Powder          -20°C   3 years ;  4°C   2 years In solvent       -80°C   6 months ;  -20°C   1 month

References

[1] Carl E Stafstrom, et al. Ann Neurol. Anticonvulsant and antiepileptic actions of 2-deoxy-D-glucose in epilepsy models

[2] Ueyama A,et.al. Biol Signals Recept Nonradioisotope assay of glucose uptake activity in rat skeletal muscle using enzymatic measurement of 2-deoxyglucose 6-phosphate in vitro and in vivo.

[3] Waki A,et.al. Nucl Med Biol The importance of glucose transport activity as the rate-limiting step of 2-deoxyglucose uptake in tumor cells in vitro.