glycolytic

BAY-876 is an orally active, selective inhibitor of glucose transporter 1 (GLUT1, IC50= 2 nM), exhibiting over 130-fold greater selectivity for GLUT1 than GLUT2, GLUT3, and GLUT4. It also inhibits glycolytic metabolism and ovarian cancer growth.

Lonidamine (Diclondazolic Acid) is an indazole carboxylic acid derivative, principally inhibiting aerobic glycolytic activity, by its effect on mitochondrially-bound hexokinase (HK).

D-Fructose-6-phosphate (sodium salt hydrate) is a sugar intermediate in the glycolytic pathway produced by the isomerization of glucose 6-phosphate by glucose phosphate isomerase, and is used in cancer research.

2-Deoxy-D-galactose is a glucose analog and glucose antagonist that inhibits the maintenance of hippocampal LTP and can suppress tumor growth by inhibiting the glycolytic process.

hydrocotarnine is an inhibitor of Cbl.

2-deoxy-D-Glucose-13C6is intended for use as an internal standard for the quantification of 2-deoxy-D-glucose by GC- or LC-MS. 2-deoxy-D-Glucose is a glucose antimetabolite and an inhibitor of glycolysis.1,2It inhibits hexokinase, the enzyme that converts glucose to glucose-6-phosphate, as well as phosphoglucose isomerase, the enzyme that converts glucose-6-phosphate to fructose-6-phosphate.32-deoxy-D-Glucose (16 mM) induces apoptosis in SK-BR-3 cells, as well as inhibits the growth of 143B osteosarcoma cells cultured under hypoxic conditions when used at a concentration of 2 mg ml.4,5In vivo, 2-deoxy-D-glucose (500 mg kg) reduces tumor growth in 143B osteosarcoma and MV522 non-small cell lung cancer mouse xenograft models when used alone or in combination with doxorubicin or paclitaxel .6 1.Kang, H.T., and Hwang, E.S.2-Deoxyglucose: An anticancer and antiviral therapeutic, but not any more a low glucose mimeticLife Sci.78(12)1392-1399(2006) 2.Aft, R.L., Zhang, F.W., and Gius, D.Evaluation of 2-deoxy-D-glucose as a chemotherapeutic agent: Mechanism of cell deathBr. J. Cancer87(7)805-812(2002) 3.Ralser, M., Wamelink, M.M., Struys, E.A., et al.A catabolic block does not sufficiently explain how 2-deoxy-D-glucose inhibits cell growthProc. Natl. Acad. Sci. USA105(46)17807-17811(2008) 4.Liu, H., Savaraj, N., Priebe, W., et al.Hypoxia increases tumor cell sensitivity to glycolytic inhibitors: A strategy for solid tumor therapy (Model C)Biochem. Pharmacol.64(12)1745-1751(2002) 5.Zhang, X.D., Deslandes, E., Villedieu, M., et al.Effect of 2-deoxy-D-glucose on various malignant cell lines in vitroAnticancer Res.26(5A)3561-3566(2006) 6.Maschek, G., Savaraj, N., Priebe, W., et al.2-deoxy-D-glucose increases the efficacy of adriamycin and paclitaxel in human osteosarcoma and non-small cell lung cancers in vivoCancer Res.64(1)31-34(2004)

1,2,3-Trioctanoyl-rac-glycerol-13C3 is intended for use as an internal standard for the quantification of 1,2,3-trioctanoyl-rac-glycerol by GC- or LC-MS. 1,2,3-Trioctanoyl-rac-glycerol is a triacylglycerol that contains octanoic acid at the sn-1, sn-2, and sn-3 positions. Dietary administration of 1,2,3-trioctanoyl-rac-glycerol increases hippocampal levels of the glycolytic metabolites glucose 6-phosphate, fructose 6-phosphate, and β-hydroxybutyrate and the seizure threshold in the 6 Hz psychomotor seizure test in mice.1 Formulations containing 1,2,3-trioctanoyl-rac-glycerol have been used in cosmetic products as thickening and skin-conditioning agents.

TRAP1-IN-1 (compound 35) is a potent, selective TRAP1 inhibitor affecting the mitochondrial variant of Hsp90. It exhibits over 250-fold greater selectivity for TRAP1 compared to Grp94, destabilizes TRAP1 tetramers, and promotes the degradation of TRAP1 client proteins. Additionally, TRAP1-IN-1 impedes mitochondrial complex I activity involved in oxidative phosphorylation (OXPHOS), compromises the mitochondrial membrane potential, and augments glycolytic metabolism [1].

NCI-006 is a potent new inhibitor of lactate dehydrogenase (LDH) that disrupts tumor growth in mice. LDH inhibition slows tumor growth but rapidly redirects pyruvate to support mitochondrial metabolism. Inhibiting both mitochondrial complex 1 and LDH suppresses metabolic plasticity of glycolytic tumors in vivo, significantly prolonging tumor growth inhibition.

MOPIPP is a novel indolebased chalcone that can cross the blood-brain barrier. MOPIPP inhibits the tumor progression agaisnt glioblastoma cells. MOPIPP induces cellular vacuolization as well as increases autophagosomes numbers. MOPIPP also triggers methuosis and distrupts glucose uptake and glycolytic metabolism [1] [2] [3].

CBR-470-1 is a potent inhibitor of glycolytic phosphoglycerate kinase 1 (PGK1) that activates NRF2 by increasing methylglyoxal levels. CBR-470-1 is a non-covalent Nrf2 activator with neuroprotective activity that protects SH-SY5Y neuronal cells from MPP+-induced cytotoxicity by activating the Keap1-Nrf2 cascade. cytotoxicity induced by MPP+.

Pomhex, a cell-permeable potent enolase inhibitor with anticancer activity, is used in the study of cancer lethality.Pomhex, a racemic mixture, is a potent and selective ENO2 inhibitor.Pomhex is inhibitory to the glycolytic process, and shows anticancer activity at low concentrations in an ENO1-deficient tumor model.Pomhex, a cell-permeable potent enolase inhibitor with anticancer activity, is a potent and selective ENO2 inhibitor.

Phosphofructokinase, a crucial glycolytic enzyme, catalyzes the conversion of fructose-6-phosphate to fructose-1,6-bisphosphate in the glycolysis pathway. Its activity is inhibited by the binding of Phosphoenolpyruvate (PEP), which regulates the rate of glycolysis. Additionally, Phosphofructokinase is utilized in the measurement of fructose-6-phosphate (fructose-6-phosphate) levels.

VLX600 is an iron-chelating oxidative phosphorylation (OXPHOS) inhibitor, is a cell-permeable anticancer agent. It acts by reducing mitochondrial oxidative phosphorylation in tumor cells.

PKM2 activator 2, with an AC50 value of 66 nM, is a pyruvate kinase M2 (PKM2) activator that demonstrates anti-tumor proliferative properties and attenuates the Warburg effect by normalizing cellular glycolytic metabolism through the activation of PKM2.

Hexokinase (ScHEX1), a glycolytic enzyme, is inhibited by n-acetylglucosamine, which causes it to detach from the mitochondrial outer membrane. This detachment activates the NLRP3 inflammasome [1].

2,3-Diphosphoglyceric acid (2,3-DPG), an intermediate of the glycolytic pathway, allosterically binds to deoxygenated hemoglobin, stabilizing it and facilitating oxygen release at tissue sites. This binding decreases hemoglobin's oxygen affinity, promoting oxygen delivery to tissues [1] [2].

Glucose 6-phosphate isomerase (GPI), also known as phosphoglucose isomerase phosphoglucoisomerase (PGI) or phosphohexose isomerase (PHI), is a highly conserved glycolytic and dimeric enzyme often used in biochemical studies that catalyzes the reversible isomerization of glucose-6-phosphate to fructose-6-phosphate [1].

Phosphoglycerate kinase (PGK) is a glycolytic enzyme that catalyzes the reversible transfer of phosphate groups from 1,3-bisphosphoglycerate (1,3-BPG) to ADP, resulting in the production of 3-phosphoglycerate (3-PG) and ATP. This enzyme not only plays a crucial role in the glycolysis pathway but also participates in gluconeogenesis by catalyzing the reverse reaction to produce 1,3-BPGA and ADP. Phosphoglycerate kinase is essential for energy metabolism, nucleic acid interactions, tumor progression, cell death, and virus replication, among other processes [1].

Ellipyrone A, a γ-pyrone-based macrocyclic polyketide, demonstrates inhibitory activity against dipeptidyl peptidase-4 (IC 50 = 0.35 mM). Additionally, this compound exhibits anti-glycolytic effects on α-glucosidase (IC 50 = 0.74 mM) and α-amylase (IC 50 = 0.59 mM) [1].

Glycogen, Mussel is a glycolytic intermediate and high-energy phosphate that ACTS as a form of energy storage for humans, animals, fungi and bacteria.

D-Fructose-6-phosphate disodium salt (D-FRUCTOSE 6-PHOSPHATE DISODIUM SALT) is an important intermediate in the Carbohydrates pathway. The interconversion of glucose-6-phosphate and fructose-6-phosphate, the second step of the Embden-Meyerhof glycolytic pathway.

SF2312 is a natural phosphonate antibiotic produced by Actinobacillus microsporus and is a potent inhibitor of the glycolytic enzyme enolase.SF2312 has antimicrobial activity and inhibits bacterial growth against both Gram-negative and Gram-negative bacteria. SF2312 inhibits human recombinant ENO1 and ENO2.

VER-246608 is an effective and ATP-competitive inhibitor of pyruvate dehydrogenase kinase (IC50s: 35 nM, 40 nM, 84 nM, and 91 nM for PDK-1, PDK-3, PDK-2, and PDK-4, respectively).VER-246608 disrupts Warburg metabolism and induces context-dependent cytosta