glycolytic metabolism

hydrocotarnine is an inhibitor of Cbl.

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.

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

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.

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.

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].

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.

L-Lactic acid-13C3 is a stable-isotope-labeled analog of L-lactic acid in which three carbon atoms are substituted with the non-radioactive 13C isotope, enabling precise tracing of lactate flux within metabolic pathways. L-Lactic acid-13C3 is widely used in metabolic profiling, isotope-tracing experiments, and studies of glycolytic reprogramming, offering high analytical sensitivity for quantifying lactate turnover in physiological and pathological settings.

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].

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.

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.

Misetionamide is an orally active oxathiazin-like compound that functions as a glyceraldehyde-3-phosphate dehydrogenase (GAPDH) inhibitor with antineoplastic activity, Misetionamide is widely used in cancer research to investigate metabolic reprogramming, glycolytic dependency, and metabolism-targeted anticancer therapeutic strategies.

Aldolase is a glycolytic enzyme and component of the VATPase complex that catalyzes the reversible cleavage of fructose 1,6-bisphosphate into dihydroxyacetone phosphate and D-glyceraldehyde 3-phosphate. Aldolase plays a critical role in cellular energy metabolism, metabolic flux regulation, and enzymatic studies of glycolysis and related pathways.

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].

TRAP1-IN-1 (compound 35) is a selective TRAP1 inhibitor that disrupts TRAP1 tetramer stability, induces degradation of TRAP1 downstream proteins, inhibits OXPHOS, and disrupts mitochondrial membrane potential.

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.

Malonyl-NAC increases cellular propylation, reducing endogenous GAPDH activity, increases GAPDH malonylation in cells, and inhibits pyruvate kinase activity. Additionally, malonyl-NAC limits the metabolism and proliferation of a highly glycolytic kidney cancer cell line harboring a tricarboxylic acid cycle mutation [1].

Keap1-Nrf2-IN-21 (compound 4d) acts as an inhibitor of glucose metabolism with anti-tumoral properties. It targets the glycolytic pathway by affecting the Keap1-Nrf2 signaling pathway, which in turn suppresses glycolytic activity in cancer cells and inhibits tumor growth. Additionally, Keap1-Nrf2-IN-21 exhibits cytotoxic effects on the HEC1A cell line with an IC50 value of 2.60 μM.

Lactic acid (Standard) is a reference standard for L-lactic acid, suitable for biochemical assays, metabolomics, and quality control. As a key glycolytic metabolite, it plays a crucial role in tumor immune evasion and energy metabolism by modulating the microenvironmental pH.