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.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V73852 | (Rac)-Etavopivat ((Rac)-FT-4202) | 2622070-93-1 | (Rac)-Etavopivat ((Rac)-FT-4202) is an isomer of Etavopivat. |
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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. |
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V73849 | CIAC001 | 2649154-82-3 | CIAC001 is a pyruvate kinase PKM2 inhibitor (antagonist) with anti-neuroinflammatory activity. |
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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. |
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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. |
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V85026 | NPD10084 | 1040706-91-9 | |
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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. |
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V87696 | PKL-IN-1 | PKL-IN-1 (Compound 12a) is a potent inhibitor of pyruvate kinase (PKL) with IC50 values of 0.07 μM and 0.18 μM for PKL and PKR isoforms, respectively. | |
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V73851 | PKM2 activator 4 | 781656-66-4 | PKM2 activator 4 is a PKM2 activator with an AC50 value of 1-10 μM. |
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V73858 | PKM2 activator 5 | 796092-26-7 | PKM2 activator 5 (Compound 8) is a PKM2 activator with an AC50 value of 0.316 µM. |
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V81160 | PKM2 activator 6 | PKM2 activator 6 (Compound Z10) is a PKM2 activator and PDK1 inhibitor (KD 121 and 19.6 μM, respectively). | |
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V87698 | PKM2 activator 7 | PKM2 activator 7 (Compd B4) is a PKM2 activator with an AC50 of 0.144 μM. | |
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V73855 | PKM2-IN-3 | 2408841-19-8 | PKM2-IN-3 is an inhibitor (blocker/antagonist) of PKM2 kinase with IC50 of 4.1 μM. |
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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. | |
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V87700 | PKM2-IN-5 | 904457-46-1 | PKM2-IN-5 (Compound G1) is a pyruvate kinase M2 (PKM2) inhibitor with IC50 >70 μM. |
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V81161 | PKM2/PDK1-IN-1 | PKM2/PDK1-IN-1 is a shikonin thioether analogue and a dual (bifunctional) inhibitor of PKM2/PDK1. | |
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V73854 | PKR activator 4 | 2283420-05-1 | PKR activator 4 (example 7A) is a potent activator of pyruvate kinase R (PKR). |
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V87699 | PKR activator 5 | 2761226-35-9 | PKR activator 5 (Compound 18) is an activator of pyruvate kinase R (PKR) with an AC50 of 28 nM. |
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V73436 | ZY-1 | ZY-1 is the control molecule for ZY-2, a PKM2 fluorescent probe. | |
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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. |
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