Pyruvate Kinase

Pyruvate Kinase

Pyruvate kinase is an enzyme that catalyzes the conversion of phosphoenolpyruvate and ADP to pyruvate and ATP in glycolysis and plays a role in regulating cell metabolism. Mammalian pyruvate kinase exists in four isoforms, each of which has distinct tissue expression patterns and regulatory characteristics. Animals have four tissue-specific isozymes of pyruvate kinase: PKL, PKR, PKM1, and PKM2. While PKM2 is expressed in early embryonic cells and other proliferating cells, and PKM1 is expressed in the brain, skeletal muscle, and heart, which require high levels of energy, the L and R isozymes are found in the liver (L) and red blood cells (R), respectively.

PKM1 and PKM2 are created by alternative splicing from a single mRNA transcript of the PKM gene. PKM2 oligomers come in both low activity dimer and high activity tetramer forms. The dimer PKM2 controls the rate-limiting step of glycolysis, which causes tumor cells to produce lactate instead of using the normal respiratory chain for the metabolism of glucose. In addition to controlling metabolism, it also functions as a protein kinase, which aids in the development of tumors. PKM2 is a promising target for the treatment of cancer.

Pyruvate Kinase related products

Structure Cat No. Product Name CAS No. Product Description
V73852 (Rac)-Etavopivat ((Rac)-FT-4202) 2622070-93-1 (Rac)-Etavopivat ((Rac)-FT-4202) is an isomer of Etavopivat.
V73856 2,5-Anhydro-D-glucitol-1,6-diphosphate 4429-47-4 2,5-Anhydro-D-glucitol-1,6-diphosphate is a limited stimulator of yeast Pyruvate Kinase.
V73849 CIAC001 2649154-82-3 CIAC001 is a pyruvate kinase PKM2 inhibitor (antagonist) with anti-neuroinflammatory activity.
V73850 Etavopivat (FT-4202) 2245053-57-8 Etavopivat is a potent, selective, orally bioavailable red blood cell (RBC) pyruvate kinase (PKR) activator with potent anti-sickling effects.
V3215 Mitapivat 1260075-17-9 Mitapivat (previously PKM2 activator 1020; AG-348; PKR-IN-1; trade name Pyrukynd) is a PKM2 activator (pyruvate kinase activator) that has potential use for the treatment of pyruvate kinase deficiency.
V73857 ML202 1221186-52-2 ML202 is a specific allosteric activator of human pyruvate kinase M2 (hPK-M2) that affects the cooperativity of phosphoenolpyruvate (PEP) binding and has almost no effect on adenosine diphosphate (ADP) binding.
V85026 NPD10084 1040706-91-9
V73853 PKCζ/ι pseudosubstrate inhibitor 799764-07-1 PKCζ/ι pseudosubstrate inhibitor has broad spectrum (a wide range) effects on the PKC enzyme family and can induce memory impairment.
V73851 PKM2 activator 4 781656-66-4 PKM2 activator 4 is a PKM2 activator with an AC50 value of 1-10 μM.
V73858 PKM2 activator 5 796092-26-7 PKM2 activator 5 (Compound 8) is a PKM2 activator with an AC50 value of 0.316 µM.
V81160 PKM2 activator 6 PKM2 activator 6 (Compound Z10) is a PKM2 activator and PDK1 inhibitor (KD 121 and 19.6 μM, respectively).
V73855 PKM2-IN-3 2408841-19-8 PKM2-IN-3 is an inhibitor (blocker/antagonist) of PKM2 kinase with IC50 of 4.1 μM.
V80173 PKM2-IN-4 PKM2-IN-4 (compound 5C) is a selective inhibitor of PKM2 (IC50=0.35 μM), which regulates pyruvate-dependent respiration and induces coupling of mitochondrial H202 production rate and electron transport system.
V81161 PKM2/PDK1-IN-1 PKM2/PDK1-IN-1 is a shikonin thioether analogue and a dual (bifunctional) inhibitor of PKM2/PDK1.
V73854 PKR activator 4 2283420-05-1 PKR activator 4 (example 7A) is a potent activator of pyruvate kinase R (PKR).
V73436 ZY-1 ZY-1 is the control molecule for ZY-2, a PKM2 fluorescent probe.
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