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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
(E)-2-Octenal V121734 (E)-2-Octenal 2548-87-0 (E)-2-Octenal is an antifungal agent.
(Rac)-Etavopivat ((Rac)-FT-4202) V73852 (Rac)-Etavopivat ((Rac)-FT-4202) 2622070-93-1 (Rac)-Etavopivat ((Rac)-FT-4202) is an isomer of Etavopivat.
2,5-Anhydro-D-glucitol-1,6-diphosphate 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.
CIAC001 V73849 CIAC001 2649154-82-3 CIAC001 is a pyruvate kinase PKM2 inhibitor (antagonist) with anti-neuroinflammatory activity.
Deoxytopsentin V133487 Deoxytopsentin 112515-42-1 Deoxytopsentin is a marine bisindole alkaloid and a pyruvate kinase inhibitor of methicillin-resistant Staphylococcus aureus (MRSA).
Etavopivat (FT-4202) 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.
GCN2 activator-1 V136551 GCN2 activator-1 315705-10-3 GCN2 activator-1 is a GCN2 activator.
LIQ1 V111335 LIQ1 2606032-80-6 LIQ1 is a flavonoid derivative and a potent allosteric inhibitor of pyruvate kinase M2 (PKM2) (IC50 = 0.39 μM; Kd = 4.5 μM), targeting Arg43 in the polyarginine binding pocket.
Mitapivat hemisulfate V94295 Mitapivat hemisulfate 2329710-91-8 Mitapivat hemisulfate is an oral allosteric activator of pyruvate kinase.
Mitapivat hydrochloride V139988 Mitapivat hydrochloride 2559738-69-9 Mitapivat hydrochloride is an orally effective selective allosteric pyruvate kinase R (PK-R) activator.
ML 083 V115306 ML 083 562867-96-3 ML083 is one of a series of highly specific allosteric activators that targets the tumor-specific subtype (M2 subtype) of human pyruvate kinase.
ML202 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.
Multi-target kinase-IN-9 V140512 Multi-target kinase-IN-9 Multi-target kinase-IN-9 is a multi-target enzyme inhibitor with anti-proliferative and anti-angiogenic activities, exhibiting significant selectivity against hepatocellular carcinoma cells.
NPD10084 V85026 NPD10084 1040706-91-9
PKCζ/ι pseudosubstrate inhibitor 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.
PKL-IN-1 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.
PKM2 activator 11 V110380 PKM2 activator 11 PKM2 activator 11 (compound 23) is a PKM2 activator with an AC50 value of 92.12 nM.
PKM2 activator 4 V73851 PKM2 activator 4 781656-66-4 PKM2 activator 4 is a PKM2 activator with an AC50 value of 1-10 μM.
PKM2 activator 5 V73858 PKM2 activator 5 796092-26-7 PKM2 activator 5 (Compound 8) is a PKM2 activator with an AC50 value of 0.316 µM.
PKM2 activator 6 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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