pyruvate kinase

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

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

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.

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.

PKM2 inhibitor G is a inhibitor of pyruvate kinase.

FX-11 (LDHA Inhibitor FX11) is A potent, selective and competitive specific inhibitor of lactate dehydrogenase A (LDHA) with a Ki of 8 μM. FX-11 can activate PKM2 (pyruvate kinase M2). FX-11 can reduce ATP levels, induce oxidative stress and ROS production, and cause cell death. FX-11 appeared antitumor activity during xenotransplantation of lymphoma and pancreatic cancer.

(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].

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.

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.

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

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

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.

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.

Mitapivat sulfate hydrate (AG 348 sulfate hydrate) is an erythrocyte pyruvate kinase (PK) allosteric activator. It enhances enzyme activity, protein stability, and ATP levels in various PKLR genotypes and can be used in pyruvate kinase deficiency research.

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.

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

PDHK-IN-7 (compound 32) acts as an inhibitor of pyruvate dehydrogenase kinase, exhibiting an IC50 value of 17 nM. Additionally, it activates PDH in rat liver and demonstrates a glucose-lowering effect in Zucker obese rats.

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

AZD7545 is a potent PDHK inhibitor.

TLN-232, also known as CAP-232, is a synthetic cyclic heptapeptide with potential antineoplastic activity. Pyruvate kinase (PK) inhibitor TLN-232 targets pyruvate kinase M2 (M2PK), which may disrupt tumor cell anaerobic glycolysis. M2PK is a dimeric isoform of PK and the predominant PK isoform found in tumor cells.

PF-06284674 is a cell permeable, potent and selective M2 isoform of pyruvate kinase (PKM2) activator.

Alkannin is a potent and specific inhibitor of tumor-specific pyruvate kinase-M2 (PKM2) without affecting PKM1 or pyruvate kinase-L (PKL), making it a potential anticancer agent [1].

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.

SET-171 is a JNK (c-Jun N-terminal kinase) inhibitor that exhibits significant anticancer activity by suppressing the expression of hepatic pyruvate kinase (PKL) and offers potential in regulating lipid metabolism. In antitumor studies, SET-171 shows notable cytotoxicity against human liver cancer cell lines HepG2 and Huh7, with IC50 values of 8.82 μM and 2.97 μM, respectively. Additionally, in research related to non-alcoholic fatty liver disease (NAFLD), SET-171 significantly reduces triglyceride (TAG) levels and inhibits the expression of proteins associated with steatosis. This compound holds promise for hepatocellular carcinoma (HCC) and NAFLD research.