Pyruvate Kinase Activator

TEPP-46 (ML-265) is a potent and selective pyruvate kinase M2 (PKM2) activator with an AC₅₀ of 92 nM, showing little or no effect on PKM1, PKL and PKR.

DASA-58 is a potential pyruvate kinase isozyme (PKM2) allosteric activator. DASA-58 can be used for the research of metabolism and kinds of cancer.

Mitapivat (AG-348) is an orally active pyruvate kinase allosteric activator. Mitapivat increases enzymatic activity, protein stability, and ATP levels over a broad range of PKLR genotypes, shows the potential to restore the activity of PK (pyruvate kinase)-deficient glycolytic pathways. Mitapivat can be used in study of PK deficiency.

Tebapivat (PKR activator 2) is a potent pyruvate kinase-R (PKR) activator extracted from patent WO2019035863A1, compound 385.

Etavopivat is a potent, selective, and orally active erythrocyte pyruvate kinase (PKR) activator. Etavopivat has potent antisickling effects that can be used in studies of sickle cell disease and other haemoglobinopathies.

PKM2 activator 2 (compound 28) is a pyruvate kinase M2 (PKM2) activitor with an AC₅₀ value of 66 nM. PKM2 activator 2 can restore normal glycolytic metabolism in cells.

PT109 is an orally active, blood-brain barrier permeable multi-kinase inhibitor. By inhibiting PTBP1, PT109 promotes the switch of pyruvate kinase isoform from PKM2 to PKM1, thereby effectively inhibiting the proliferation and migration of glioblastoma multiforme and inducing its reprogramming into oligodendrocytes. PT109 also targets and regulates key signaling molecules such as JNK, SGK1, GSK3β to exert neuroprotective effects including promoting neurogenesis, inducing synapse formation and alleviating neuroinflammation. In Alzheimer's disease models, PT109 exhibits significant efficacy in improving spatial learning ability, along with excellent in vivo pharmacokinetic properties. PT109 can be used to investigate metabolic reprogramming of glioblastoma multiforme and neuroprotective mechanisms of Alzheimer's disease.

PKR activator 3 (Compound 160) is a red blood cell pyruvate kinase (PKR) activator. PKR activator 3 can be used in the research of diseases related to PKR function, such as pyruvate kinase deficiency (PKD).

PKM2 activator 5 (compound 8) is a PKM2 activator with an AC₅₀ value of 0.316 µM. PKM2 activator 5 has the potential to alter the aberrant metabolism of cancer cells.

PKR activator 1 is a potent pyruvate kinase-R (PKR) activator extracted from patent WO2019035865A1, compound E7-93.

PKM2 activator 6 (Compound Z10) is a PKM2 activator and PDK1 inhibitor (K_D: 121 and 19.6 μM respectively). PKM2 activator 6 induces colorectal cell apoptosis, and inhibits cell proliferation and migration . PKM2 activator 6 inhibits glycolysis. PKM2 activator 6 inhibits proliferation of DLD-1, HCT-8, HT-29, MCF-10A cells (IC₅₀: 10.04, 2.16, 3.57, 66.39 μM).

PF-06284674 (PKM2 activator 1) (Compound 8) is a PKM2 activator that can be used in cancer research.

ML202 is a highly specific allosteric activator of human pyruvate kinase M2 (hPK-M2), which can affect the cooperativity of phosphoenolpyruvate (PEP) binding, while adenosine diphosphate (ADP) binding almost no effect.

(Rac)-Etavopivat ((Rac)-FT-4202) is an isomer of Etavopivat (HY-139573). Etavopivat is an orally active erythrocyte pyruvate kinase-R (PKR) activator that can be used in studies of sickle cell disease and other haemoglobinopathies.

PKR activator 5 (Compound 18) is an activator for pyruvate kinase R (PKR) with an AC₅₀ of 28 nM.

PKM2 activator 10 (Compd I) is a PKM2 activator with anti-tumor activity. PKM2 activator 10 can be utilized in cancer research.

Mitapivat-d₈ (AG-348-d₈) is the deuterium labeled Mitapivat (HY-12689). Mitapivat (AG-348) is an orally active pyruvate kinase allosteric activator. Mitapivat increases enzymatic activity, protein stability, and ATP levels over a broad range of PKLR genotypes, shows the potential to restore the activity of PK (pyruvate kinase)-deficient glycolytic pathways. Mitapivat can be used in study of PK deficiency.

Mitapivat hemisulfate is an orally active pyruvate kinase allosteric activator. Mitapivat hemisulfate increases enzymatic activity, protein stability, and ATP levels over a broad range of PKLR genotypes, shows the potential to restore the activity of PK (pyruvate kinase)-deficient glycolytic pathways. Mitapivat hemisulfate can be used in study of PK deficiency.

Mitapivat hemisulfate sesquihydrate (AG-348) is an orally active pyruvate kinase allosteric activator. Mitapivat increases enzymatic activity, protein stability, and ATP levels over a broad range of PKLR genotypes, shows the potential to restore the activity of PK (pyruvate kinase)-deficient glycolytic pathways. Mitapivat can be used in study of PK deficiency.

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.