Pyruvate Kinase

PKM2 activator 3 is a potent activator of pyruvate kinase M2 (PKM2), exhibiting an AC50 value of 90 nM. This compound demonstrates favorable Caco-2 permeability, low efflux ratio, and high microsomal stability, making it an advantageous tool for in vitro studies. PKM2 activator 3 is primarily utilized in cancer research, facilitating the investigation of metabolic pathways and potential therapeutic strategies targeting PKM2.

PKR Activator 4 is a potent activator of pyruvate kinase R (PKR), enhancing its enzymatic activity. This compound demonstrates key biological activity by stimulating glycolytic flux and ATP production, making it instrumental in studies related to energy metabolism and blood disorders. Researchers can utilize PKR Activator 4 to investigate its effects on cellular metabolism and the potential therapeutic implications for metabolic dysfunctions.

Alkannin is a selective inhibitor of tumor-specific pyruvate kinase-M2 (PKM2), demonstrating potent activity without affecting PKM1 or pyruvate kinase-L (PKL). This compound has potential applications in cancer research, serving as a valuable tool for studying metabolic alterations in tumors and developing anticancer strategies. Alkannin's specificity for PKM2 highlights its utility in targeted therapeutic approaches in oncology.

ML083 is a selective allosteric activator for the tumor-specific isoform of human pyruvate kinase (PK-M2). By modulating the cooperativity of phosphoenolpyruvate (PEP) binding, ML083 enhances PK-M2 activity, making it a valuable tool for studying tumor metabolism. This compound is essential for research applications focusing on cancer biology and metabolic regulation within tumor cells.

PKM2 agonist-1 is an allosteric activator of pyruvate kinase M2 (PKM2) with a reported AC50 of 77 nM. This compound has been shown to inhibit angiotensin II-induced phenotypic switching in smooth muscle cells, demonstrating significant biological activity in vascular biology. Additionally, PKM2 agonist-1 effectively reduces the incidence of aortic dissection and associated mortality, making it a valuable tool for research in cardiovascular disease and cellular metabolism.

PKM2-IN-5 is a selective inhibitor of pyruvate kinase M2 (PKM2), a critical enzyme involved in cellular energy metabolism. This compound exhibits potential for modulating glucose metabolism and influencing tumorigenesis by inhibiting PKM2 activity. PKM2-IN-5 is valuable for research applications in cancer biology and metabolic disorders, providing insights into the role of PKM2 in various cellular processes.

2,5-Anhydro-D-glucitol-1,6-diphosphate is an allosteric stimulator of yeast Pyruvate Kinase, enhancing its enzymatic activity. This compound serves as an analogue of 2,5-anhydro-D-mannitol 1,6-bisphosphate, providing insights into the regulatory mechanisms of glycolysis. Its application in biochemical research facilitates the study of metabolic pathways and enzyme kinetics linked to energy production in yeast.

NCGC00188636 is a novel covalent inhibitor of pyruvate kinase (PYK). By blocking nucleotide binding at the active site, NCGC00188636 disrupts PYK activity, thereby influencing metabolic processes. This compound is suited for research into the metabolic pathways of various organisms and cell types, providing insights into cellular energy regulation and potential therapeutic targets.