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.

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.

hydrocotarnine is an inhibitor of Cbl.

6PPD-Q (6PPD-Quinone) is an environmental pollutant that can target CNR2, CNR1, AA2AR, LCAT and TRPA1. Among them, CNR2 has the highest binding affinity and may act as a CNR2 receptor agonist to activate cannabinoid receptors. 6PPD-Q can damage the sperm quality and induce the impairment of male reproductive ability in mice. 6PPD-Q can induce intestinal inflammation and barrier damage by disrupting mitochondrial function, reducing neuronal glycolytic metabolites and TCA cycle intermediates, and exacerbating α-synuclein (α-syn) aggregation.

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

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 (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.

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

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.

Lon-TK is a glycolysis inhibitor of LTB, linked with a linker conjugate. LTB is an intelligent responsive prodrug, comprised of Lonidamine (Lon) and a PD-L1 inhibitor (BMS-1), which are connected through a thioketal linkage. It effectively inhibits glycolytic metabolism in tumor cells and blocks the PD-1/PD-L1 immune escape pathway. Lon-TK holds potential for use in photodynamic-enhanced immunotherapy research.

ML 083 is a highly specific allosteric activator of the tumor-associated M2 isoform of human pyruvate kinase that modulates phosphoenolpyruvate binding cooperativity, and it is used as a metabolic research tool to investigate tumor-specific glycolytic regulation and cancer-associated metabolic reprogramming.

DC-PGKI is an orally active ATP-competitive inhibitor of PGK1, with an IC50 of 0.16 μM and a Kd of 99.08 nM. It stabilizes PGK1 both in vitro and in vivo, inhibiting glycolytic activity and PGK1's kinase function. This inhibition induces the accumulation of NRF2 (nuclear factor erythroid 2-related factor 2, NFE2L2), which then translocates to the nucleus, binds to the proximal regions of IL-1β and IL-6 genes, and inhibits their LPS-induced expression. DC-PGKI is applicable for research in colitis.

SU212 is a podophyllotoxin-derived ENO1 inhibitor and AMPK activator. It selectively induces oxidative phosphorylation in cells, reduces glycolytic activity and glucose uptake in tumor cells, and directly binds ENO1 without affecting pathways in normal cells. SU212 induces apoptosis and facilitates ENO1 degradation via proteasomal and autophagic pathways without inhibiting its catalytic activity. It activates AMPK independently of energy stress and without being affected by glucose or insulin levels, resulting in M phase arrest and apoptosis in triple-negative breast cancer (TNBC) cells, demonstrating potent in vitro antitumor activity. Additionally, SU212 inhibits tumor growth and metastasis in syngeneic, xenograft, and diabetic mouse models, showing excellent safety profiles. This compound can be utilized in research on TNBC, diabetes, and fatty liver disease.

PKM2-IN-13 is a selective inhibitor of PKM2 with an IC50 value of 55.13 μM. This compound demonstrates broad-spectrum anticancer activity while exhibiting low toxicity to normal cells. PKM2-IN-13 induces apoptosis by elevating reactive oxygen species (ROS) levels and activating Caspase-3/7. It interacts with pyruvate kinase M2 in vitro, inhibiting its glycolytic function. Additionally, PKM2-IN-13 has shown a good safety profile, with no significant adverse effects observed in in vivo experiments. It can be utilized in research studies involving oral squamous cell carcinoma, colon cancer, breast cancer, and melanoma.

Dactylarin is a cytotoxic antibiotic. Dactylarin isolated from Dactylaria lutea. Dactylarin interacts with thiols, which explains its inhibitory effect on the above glycolytic enzymes.

NHI-2 is a lactate dehydrogenase A (LDHA) inhibitor with an IC50 value of 14.7 µM, demonstrating high selectivity for LDHA over LDHB, for which the IC50 is 55.8 µM. NHI-2 functions as an efficient anti-glycolytic agent, enhancing apoptosis, inducing cell cycle arrest at the S and G2 phases, and exerting broad-spectrum antiproliferative effects in cancer cells. NHI-2 additionally affects extracellular acidification rates and ATP production and has demonstrated tumor growth suppression in murine B78 melanoma models, highlighting its role in cancer metabolism research.

GNE-140 is a novel and potent lactate dehydrogenase A (LDHA) inhibitor that disrupts glycolytic metabolism in MIA PaCa-2 human pancreatic cancer cells, inducing rapid metabolic reprogramming prior to delayed cell death, with intrinsic resistance observed in OXPHOS-dependent pancreatic cell lines that can be reversed by phenformin, while acquired resistance is driven by AMPK-mTOR-S6K pathway activation, highlighting its value for studying metabolic plasticity and therapeutic resistance.

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.

CC260, a selective inhibitor for PI5P4Kα and PI5P4Kβ with Kis of 40 nM and 30 nM respectively, exhibits minimal to no inhibition against other protein kinases like Plk1 and RSK2. It is applicable in the research of cell energy metabolism, diabetes, and cancer[1].

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.

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.

Etavopivat is a potent, selective, and orally active activator of erythrocyte pyruvate kinase (PKR) that enhances red blood cell glycolytic flux and energy metabolism, exhibiting strong antisickling effects by improving erythrocyte deformability and reducing hemoglobin polymerization. Etavopivat is therefore widely applied in translational and mechanistic studies of sickle cell disease and other inherited haemoglobinopathies.

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+.