pyruvate

α-Cyano-4-hydroxycinnamic acid (α-CHCA) is an inhibitor of monocarboxylate transporter 1 (MCT1), which blocks pyruvate transport in rat heart mitochondria (IC50: 1.5 μM).

MSDC 0160 (CAY10415) is a prototype mTOT-modulating insulin sensitizer being used in trials studying the treatment of Type 2 Diabetes and Alzheimer's Disease.

GW604714X (2,4-Thiazolidinedione, 5-[[5-[6-(4-acetyl-1-piperazinyl)-3-nitro-2-pyridinyl]-2-fluorophenyl]methylene]-) were found to be potent inhibitors of mitochondrial respiration supported by pyruvate

Sodium 2-oxopropanoate (Sodium pyruvate) is a antioxidant potentially used to treatment of chronic obstructive pulmonary disease.

DL-Serine is a non-essential amino acid and a natural ligand and allosteric activator of pyruvate kinase M2.

Glymidine sodium is a sulfonamide hypoglycemic agent which stimulates insulin secretion.

(+)-Shikonin (Anchusa acid) is a natural product, a TMEM16A chloride channel inhibitor (IC50=6.5 μM) and selective PKM2 inhibitor. (+)-Shikonin exhibits antitumor, anti-inflammatory and wound healing activities.

KPLH1130, a specific pyruvate dehydrogenase kinase (PDK) inhibitor, enhances glucose tolerance in mice fed a high-fat diet (HFD). It effectively hinders macrophage polarization and mitigates proinflammatory reactions.

PDK4-IN-1 hydrochloride, an anthraquinone derivative, is a potent and orally active inhibitor of pyruvate dehydrogenase kinase 4 (PDK4) with an IC50 value of 84 nM.

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

AZD7545 is a potent PDHK inhibitor.

PKM2-IN-1 (compound 3k) exhibits inhibitory activity against PKM2 with an IC50 of 2.95 μM, while the IC50 for PKM1 is 4-5 times higher.

PKM2 inhibitor G is a inhibitor of pyruvate kinase.

DASA-58 is a specific and potent Pyruvate kinase M2 (PKM2) activator.

TEPP-46 (ML265) is an activator of pyruvate kinase M2 (PKM2) (AC50=92 nM), selective for PKM1, PKL and PKR. TEPP-46 has antitumor activity.

Pyruvate Carboxylase-IN-5 (compound 6m) is a selective and permeable inhibitor of pyruvate carboxylase. This mitochondrial enzyme plays a critical role in catalyzing the conversion of pyruvate to oxaloacetate, a process essential for maintaining the steady-state levels of tricarboxylic acid cycle intermediates, which serve as precursors for the synthesis of biomacromolecules, including amino acids, fatty acids, and glucose.

Pyruvate Carboxylase-IN-1 (compound 37), a natural analog of erianin, is a potent inhibitor of pyruvate carboxylase (PC), with inhibitory concentrations (IC50) of 0.204 μM and 0.104 μM in cell lysate-based and cell-based PC activity assays, respectively. This compound effectively inhibits PC enzymatic activity, contributing to its anticancer effects in human hepatocellular carcinoma (HCC) [1].

Pyruvate Carboxylase-IN-2 is a natural analog of erianin. Pyruvate Carboxylase-IN-2 (compound 29) is a potent inhibitor of pyruvate carboxylase (PC). In cell lysate-based and cell-based PC activity assays, Pyruvate Carboxylase-IN-2 shows IC 50 s of 0.065 and 0.097 μM, respectively. Pyruvate Carboxylase-IN-2 mediates the anticancer effect in human hepatocellular carcinoma (HCC).

Pyruvate kinase is a glycolytic enzyme that catalyzes the conversion of phosphoenolpyruvate and ADP to pyruvate and ATP [1] .

Pyruvate carboxylase, a biotin-containing enzyme, catalyzes the carboxylation of pyruvate to oxaloacetate, a reaction dependent on HCO3− and MgATP. This enzyme is crucial for regulating whole-body energetics, influencing gluconeogenesis in the liver, fatty acid synthesis in adipocytes, and insulin secretion in pancreatic β-cells [1] [2].

Pyruvate Carboxylase-IN-4 (Compd 8V) acts as a competitive inhibitor of Pyruvate Carboxylase, demonstrating potency with an IC 50 value of 4.3 μM.

Ethyl pyruvate is a simple aliphatic ester of pyruvic acid and has been shown to have robust neuroprotective effects via its anti-inflammatory, anti-oxidative, and anti-apoptotic functions.

Isoniazid pyruvate is a metabolite of isoniazid. Isoniazid (Laniazid, Nydrazid), also known as isonicotinylhydrazine (INH), is an organic compound that is the first-line medication in prevention and treatment of tuberculosis.

Pyruvate oxidase (PoxB) is a thiamine pyrophosphate-dependent oxidase, a key enzyme in glucose metabolism, and is used in the study of invasive pneumococcal disease.