All tags Metabolism Molecular targets of glycolysis

Molecular targets of glycolysis

Quickly choose glycolysis related products based on your research needs.

To aid your research in the different stages of glycolysis, we have put together a piece highlighting the proteins involved in this process and recommended our top products for these targets – making it easier for you to select the best tools for your experiment.

The schematic below shows the different steps of glycolysis and the subcellular distribution of the molecules and enzymes involved (this image has been adapted from: Mol Cancer (2013)12:152).

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GLUT

The first step in the glycolysis process is the entrance of glucose into the cell, which is mediated by glucose binding transporters (GLUTs).

To alter metabolism at this stage or quantify expression levels see the recommended products below.


Recommended product

Application

Species reactivity

Antibody Anti-Glucose Transporter GLUT1 antibody [EPR3915]

Western blot, ICC, IHC, Flow cytometry

Ms, Rt, Hu

Anti-Glucose Transporter GLUT4 antibody

ICC/IF, WB, IP, IHC

Ms, Rt, Hu

Glucose Uptake Assay Kit (Colorimetric)

Functional studies

Hu

Inhibitors

Recommended product

Activity

Potency (IC50)

Phloretin

GLUT inhibitor

49 μM3

Cytochalasin B 

Selective GLUT1 inhibitor

0.44 μM3

Forskolin

Glucose transport inhibitor

2.35 μM4

See all other GLUT products here


HKII

Once glucose has entered the cell it is phosphorylated by hexokinase (HK) to glucose-6-phosphate, and the process of glycolysis is initiated. This stage is crucial for glycolysis as not only is it a rate limiting step, it’s high affinity for glucose means glycolysis can take place when serum levels of glucose are low. Out of the four types of the HK enzyme, HK2 is the most abundant, and is bound to the mitochondrial outer membrane.

To alter metabolism at this stage or quantify expression levels see the recommended products below.


Markers

Recommended product

Application

Species reactivity

Anti-Hexokinase II antibody [3D3]

ELISA, Flow cyt, ICC/IF, IHC-P, WB

Hu

Hexokinase Activity Assay Kit (Colorimetric)Functional studies    Hu

Recombinant human Hexokinase II protein

Functional studies, SDS-PAGE

Hu


Inhibitors

Recommended product

Selectivity

Potency (IC50)

Bromopyruvic acid (3-bromopyruvic acid)

Hexokinase II inhibitor

17µM5

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

Glycolytic inhibitor

2.5μM6

Lonidamine

Hexokinase inhibitor

850 μM

See all other HK products here


PFK

The next step of glycolysis is also a rate limiting one. In this stage the phosphorylation of fructose 6-phosphate to fructose-1,6-biphosphate takes place. This reaction is catalyzed by PFK1, and is modulated by the intracellular concentration of fructose 2,6 biphosphate, which is itself regulated by enzymes called PFKFBs.

To alter metabolism at this stage or quantify expression levels please see the recommended products below.


Markers

Recommended product

Application

Species reactivity

Anti-PFKFB3 antibody [EPR12594]

Flow cyt, ICC/IF, IHC-P, IP, WB

Ms, Rt, Hu

6-PFK Activity Assay Kit (Colorimetric)Functional studiesHu

Recombinant Human PFKFB3 protein

ELISA, SDS-PAGE, WB

Hu


Inhibitors

Recommended product

Selectivity

Potency (IC50)

YZ9

PFKFB3 inhibitor

0.18 µM

PFK15

PFK inhibitor

207 n

See all other PFK products here


GAPDH

GAPDH is one of the most important enzymes involved in cell energy metabolism, as it facilitates the first energy-producing reaction in the glycolysis pathway. It catalyses the oxidative phosphorylation of glyceraldehyde-3-phosphate to form nicotinamide adenine dinucleotide (NADH). NADH production not only effects metabolism but is involved in the regulation of intracellular ROS levels within the cell.  

To alter metabolism at this stage or quantify expression levels see the recommended products below.


Markers

Recommended product

Application

Species reactivity

Anti-GAPDH antibody [EPR16891]

Flow cyt, ICC/IF, IHC-P, IP, WB

Ms, Rt, Hu, and more

GAPDH ELISA Kit

ELISA

Ms, Hu

Mitochondria fraction Western Blot Cocktail

Activity assay

Ms, Rt, Hu

GAPDH Activity Assay Kit (Colorimetric)Functional studiesHu


Inhibitors

Recommended product

Selectivity

Potency (IC50)

Heptelidic acid (Koningic acid)

GAPDH inhibitor

40 μM

See all other GAPDH products here


PK-M2

The next stage of glycolysis is the conversion of phosphoenolpyruvate into pyruvate by pyruvate kinase (PK) and the generation of ATP in the process. Among the various isoforms of PK, the M2 isoform of muscle specific PK is widely expressed in cells with a high rate of nucleic acid synthesis, such as normal proliferating cells, embryonic cells, and tumor cells.

To alter metabolism at this stage or quantify expression levels see the recommended products below.


Markers

Recommended product

Application

Species reactivity

Anti-PKM2 antibody

ICC/IF, IHC-P, WB

Ms, Hu

PK Assay KitFunctional studiesHu 

Recombinant human PKM2 protein

FuncS, SDS-PAGE, WB

Hu


Inhibitors

Recommended product

Selectivity

Potency (EC50)

BML 283

Selective activator of PKM2

111 nM

See all other PK-M2 products here


LDH

The final step in glycolysis is the conversion of pyruvate into lactate, catalysed by LDH. LDH is also involved in the maintenance of a high glycolytic rate, and is transported into the extracellular space via monocarboxylate transporters (MCTs) to prevent harmful build-up within the cell.

To alter metabolism at this stage or quantify expression levels see the recommended products below.


Markers

Recommended product

Application

Species reactivity

Anti-LDHA antibody [EPR1564]

Flow cyt, ICC/IF, IHC-P, WB

Ms, Rt, Hu

Anti-Monocarboxylic acid transporter 1 antibody

ICC/IF, IHC-P, WB

Hu

Lactate Dehydrogenase (LDH) Assay Kit (Colorimetric)

Activity assay

Hu


Inhibitors

Recommended product

Selectivity

Potency (IC50)

Sodium oxamate

LDH inhibitor

600 μM

Galloflavin

LDH inhibitor

25 μM 7

See all other LDH products here


References 

1. Alfarouk, K. O. et al. Glycolysis, tumor metabolism, cancer growth and dissemination. A new pH-based etiopathogenic perspective and therapeutic approach to an old cancer question. Oncoscience 1, 777–802 (2014).

2. Alfarouk, K. O. Tumor metabolism, cancer cell transporters, and microenvironmental resistance. J. Enzyme Inhib. Med. Chem. 31, (2016).

3. Augustin, R. The protein family of glucose transport facilitators: It’s not only about glucose after all. IUBMB Life 62, 315–333 (2010).

4. Iancu, C. V, Zamoon, J., Woo, S. B., Aleshin, A. & Choe, J. Crystal structure of a glucose/H+ symporter and its mechanism of action. Proc. Natl. Acad. Sci. U. S. A. 110, 17862–7 (2013).

5. Bhardwaj, V., Rizvi, N., Lai, M., Lai, J. & Bhushan, A. Iodoacetate and 3-bromopyruvate modulate cell signaling to decrease the pancreatic cancer cell survival. Cancer Res. 68, 4336 LP-4336 (2014).

6. Mühlenberg, T. 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 10, e0120531 (2015).

7. Han, X. et al. Evaluation of the anti-tumor effects of lactate dehydrogenase inhibitor galloflavin in endometrial cancer cells. J. Hematol Oncol. 8, 2 (2015).


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