pyruvate kinase

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

Mitapivat (PKR-IN-1), also known as PKM2 activator 1020 is a PKM2 activator (pyruvate kinase activator) for the treatment of pyruvate kinase deficiency.

Disodium monofluorophosphate (NSC248) is a competitive inhibitor of pyruvate kinase and alkaline phosphatase, which also irreversibly inhibits phosphorylase phosphatase.

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

(+)-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.

PKR-IN-2 is a activator of pyruvate kinase (PKR).

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 Kinase/Lactic Dehydrogenase enzymes, Rabbit catalyze the ATP-dependent phosphorylation of glycolate to produce 2-phosphoglycolate. The activation of pyruvate kinase requires divalent cation Mg2+ and monovalent cation K+.

M77976 is a selective ATP-competitive inhibitor of pyruvate dehydrogenase kinase 4 (PDK4) with an inhibitory effect on PDK4, having an IC50 value of 648 μM. It is used for research related to obesity and diabetes.

(Rac)-Etavopivat ((Rac)-FT-4202), an isomer of Etavopivat, is an orally active erythrocyte pyruvate kinase-R (PKR) activator used in sickle cell disease and haemoglobinopathy research [1].

Dehydroabiethylamine (NSC-2955) is an inducer of hepatic CYP2B activity. Dehydroabiethylamine inhibits pyruvate dehydrogenase kinases (PDKs) and intracellular cholesterol transport with anti-tumor activity.

Sodium dichloroacetate (BCA) , a specific inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50 values of 183 and 80 μM for PDK2 and PDK4 respectively, has been shown to derepress a mitochondrial potassium-ion channel axis, trigger apoptosis in cancer cells, and inhibit tumor growth.

Potassium 1-carboxyvinyl hydrogenphosphate (PEP-K) is involved in glycolysis and gluconeogeneis. In glycolysis, PEP is metabolized by Pyruvate Kinase to yield pyruvate. In plants, PEP is involved in the formation of aromatic amino acids as well as in the carbon fixation pathway.

Acetyl phosphate lithium potassium (Lithium potassium acetyl phosphate) is a compound involved in taurine and hypotaurine metabolism as well as pyruvate metabolism. Acetyl phosphate lithium potassiu is generated from sulfoacetaldehyde, converted to acetyl-CoA and acetate via phosphate acetyltransferase and acetate kinase respectively. Acetyl phosphate lithium potassiu is also an intermediate in pyruvate metabolism.

GSK-7227, a novel compound representing a novel class of peroxisome proliferator-activated receptor delta (PPARδ) partial agonists, demonstrates potent partial agonistic activity by upregulating the expression of PPARδ target genes, specifically carnitine palmitoyltransferase 1a (CPT1a) and pyruvate dehydrogenase kinase 4 (PDK4), in cultured skeletal muscle cells, indicating its potential role in modulating skeletal muscle metabolism and energy homeostasis.

Dicoumarol (Dicumarol) is a hydroxycoumarin originally isolated from molding sweet-clover hay, with anticoagulant and vitamin K depletion activities. Dicoumarol is a competitive inhibitor of vitamin K epoxidereductase; thus, it inhibits vitamin K recycling and causes depletion of active vitamin K in blood. This prevents the formation of the active form of prothrombin and several other coagulant enzymes, and inhibits blood clotting.

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

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.

PKR activator 1 is a potent activator of pyruvate kinase-R (PKR).

PKR activator 2 is a potent activator of pyruvate kinase-R (PKR).