Pyruvate Kinase Activator

Mitapivat (AG-348) hydrochloride is an orally active and selective allosteric pyruvate kinase R (PK-R) activator. Mitapivat hydrochloride accelerates the reaction of PK-R catalyzing the conversion of phosphoenolpyruvate to pyruvate, thereby promoting the glycolytic pathway, increasing the production of adenosine triphosphate (ATP) in red blood cells, and reducing the level of 2,3-diphosphoglycerate (2,3-DPG). Mitapivat hydrochloride is promising for research of pyruvate kinase deficiency and other anemia-related diseases.

PKM2 activator 7 (Compd B4) is a PKM2 activator with the AC₅₀ of 0.144 μM. PKM2 activator 7 suppresses DSS (HY-116282C)-induced colitis by inhibiting T cell growth in mouse colitis model.

PKM2 activator 3 is a potent PKM2 activator with an AC₅₀ value of 90 nM. PKM2 activator 3 has good Caco-2 permeability, a low efflux ratio and high microsomal stability. PKM2 activator 3 can be used for researching anticancer.
(AC₅₀: the concentration which gives 50% activation of enzyme.)

PKR activator 4 (example 7A) is a potent pyruvate kinase R (PKR) activator. PKR activator 4 has the potential for the research of blood disorders.

PKM2 activator 11 (Compound 23) is a PKM2 activator with an AC₅₀ value of 92.12 nM. PKM2 activator 11 promotes PKM2 tetramerization and inhibits its nuclear translocation. PKM2 activator 11 suppresses glycolysis and the PKM2/STAT3 signaling pathway. PKM2 activator 11 induces Apoptosis. PKM2 activator 11 exhibits anti-CRC activity in vitro with potency and selectivity.

ML083 is a member of a series of highly specific allosteric activators for the tumor-specific isoform of human pyruvate kinase (M2 isoform). ML083 affects the cooperativity of phosphoenolpyruvate (PEP) binding. ML083 can be used in the research of tumors.

ZINC08383544 is a PKM2 activator with anti-tumor activity. ZINC08383544 binds to the dimer-dimer interface of PKM2, promotes tetramer formation, blocks nuclear translocation, inhibits the expression of glycolysis-related genes such as GLUT1, and reduces T cell-mediated inflammatory responses. ZINC08383544 can be used in cancer-related research such as cervical cancer.

PKM2 activator 4 is a PKM2 activator with an AC₅₀ value of 1-10 μM. PKM2 activator 4 can be used for the research of cancer.

ML202 (Standard) is the analytical standard of ML202 (HY-110124). This product is intended for research and analytical applications. ML202 is a highly specific allosteric activator of human pyruvate K_inase M2 (hPK-M2), which can affect the cooperativity of phosphoenolpyruvate (PEP) binding, while adenosine diphosphate (ADP) binding almost no effect.