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.

Product Citations

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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

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

Conversion of different model animals based on BSA (PMID: 27057123)

Species	Mouse	Rat	Rabbit	Guinea pig	Hamster	Dog
Weight (kg)	0.02	0.15	1.8	0.4	0.08	10
Body Surface Area (m2)	0.007	0.025	0.15	0.05	0.02	0.5
Km factor	3	6	12	8	5	20

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the K_m factor for a mouse and then divide by the K_m factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] 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.

[2] 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.