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Tags Metabolism
ANGPTL
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PKM

Pyruvate kinase isozymes M1/M2 (PKM1/M2), also known as pyruvate kinase muscle isozyme (PKM), pyruvate kinase type K, cytosolic thyroid hormone-binding protein (CTHBP), thyroid hormone-binding protein 1 (THBP1), or opa-interacting protein 3 (OIP3), is an enzyme that in humans is encoded by the PKM2 gene.PKM2 is an isoenzyme of the glycolytic enzyme pyruvate kinase. Depending upon the different metabolic functions of the tissues, different isoenzymes of pyruvate kinase are expressed. PKM2 is expressed in some differentiated tissues, such as lung, fat tissue, retina, and pancreatic islets, as well as in all cells with a high rate of nucleic acid synthesis, such as normal proliferating cells, embryonic cells, and especially tumor cells.

TEPP-46
ML265
T72141221186-53-3
TEPP-46 (ML265) is an activator of pyruvate kinase M2 (PKM2) (AC50=92 nM), selective for PKM1, PKL and PKR. TEPP-46 has antitumor activity.
  • 36 €
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TargetMol | Citations Cited
Mitapivat
PKR-IN-1
T42231260075-17-9
Mitapivat (PKR-IN-1), also known as PKM2 activator 1020 is a PKM2 activator (pyruvate kinase activator) for the treatment of pyruvate kinase deficiency.
  • 30 €
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(+)-Shikonin
NSC 252844, Isoarnebin 4, C.I. 75535, Anchusa acid, Alkanna Red, (R)-(+)-Shikonin, (+)-Shikonin
T1125517-89-5
(+)-Shikonin (Anchusa acid) is a natural product, a TMEM16A chloride channel inhibitor (IC50=6.5 μM) and selective PKM2 inhibitor. (+)-Shikonin exhibits antitumor, anti-inflammatory and wound healing activities.
  • 26 €
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TargetMol | Citations Cited
PKM2-IN-1
PKM2 inhibitor, compound 3k
T417094164-88-2
PKM2-IN-1 (compound 3k) exhibits inhibitory activity against PKM2 with an IC50 of 2.95 μM, while the IC50 for PKM1 is 4-5 times higher.
  • 27 €
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TargetMol | Citations Cited
DASA-58
T68161203494-49-8
DASA-58 is a specific and potent Pyruvate kinase M2 (PKM2) activator.
  • 33 €
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TargetMol | Citations Cited
PKR-IN-2
T124991628428-01-2
PKR-IN-2 is a activator of pyruvate kinase (PKR).
  • 27 €
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Benserazide hydrochloride
Serazide, Ro 4-4602, Benserazide HCl
T151714919-77-8
Benserazide hydrochloride (Ro 4-4602) is a peripherally-acting L-amino acid decarboxylase (AAAD) or DOPA decarboxylase inhibitor.
  • 41 €
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PKM2 inhibitor G
T67900904457-46-1
PKM2 inhibitor G is a inhibitor of pyruvate kinase.
  • 105 €
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DL-Serine
T8363302-84-1
DL-Serine is a non-essential amino acid and a natural ligand and allosteric activator of pyruvate kinase M2.
  • 27 €
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7-Hydroxyflavone
T74726665-86-7
7-Hydroxyflavone is a potent inhibitor of CYP1A1 with a Ki value of 0.015 μM and exhibits 6-fold greater selectivity for CYP1A1 over CYP1A2.with anti-inflammatory activity
  • 27 €
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TargetMol | Citations Cited
PKM2 activator 2
T627581186660-06-9
PKM2 activator 2, with an AC50 value of 66 nM, is a pyruvate kinase M2 (PKM2) activator that demonstrates anti-tumor proliferative properties and attenuates the Warburg effect by normalizing cellular glycolytic metabolism through the activation of PKM2.
  • 46 €
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Disodium monofluorophosphate
NSC248
T074510163-15-2
Disodium monofluorophosphate (NSC248) is a competitive inhibitor of pyruvate kinase and alkaline phosphatase, which also irreversibly inhibits phosphorylase phosphatase.
  • 26 €
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Dimethylaminomicheliolide HCl
T60102L1403357-80-1
Dimethylaminomicheliolide HCl has potential anti-inflammatory and anti-tumor activity and inhibits the proliferation of glioblastoma cells by targeting pyruvate kinase 2 (PKM2) and reconnecting aerobic cell populations.
  • 175 €
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Iminostilbene
Dibenzazepine
T0598256-96-2
Iminostilbene (Dibenzazepine) (Dibenzazepine) is a chemical precursor of carbamazepine which is used primarily in the treatment of epilepsy and neuropathic pain.
  • 26 €
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TargetMol | Inhibitor Sale
TargetMol | Citations Cited
(Rac)-Etavopivat
(Rac)-FT-4202
T726632622070-93-1In house
(Rac)-Etavopivat ((Rac)-FT-4202), an isomer of Etavopivat, is an orally active erythrocyte pyruvate kinase-R (PKR) activator used in sickle cell disease and haemoglobinopathy research [1].
  • 1.503 €
6-8 weeks
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PKM2-IN-3
PKM2-IN-3
T399842408841-19-8
PKM2-IN-3 is a potent PKM2 kinase inhibitor, displaying an IC50 value of 4.1 μM. The compound effectively suppresses PKM2-mediated glycolysis and NLRP3 activation, thereby exerting an anti-neuroinflammatory effect.
  • 873 €
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PF-06284674
T706651434288-24-0
PF-06284674 is a cell permeable, potent and selective M2 isoform of pyruvate kinase (PKM2) activator.
  • 1.368 €
6-8 weeks
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PKM2 activator 5
T72693796092-26-7
PKM2 activator 5 is a novel and potent PKM2 activator (AC50: 0.316 µM) with potential anticancer activity for the study of cancer metabolism-related diseases.
  • 42 €
6-8 weeks
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PKM2 activator 4
T72692781656-66-4
PKM2 Activator 4, a chemical compound, functions as an activator of PKM2 with an activation concentration (AC 50) ranging from 1 to 10 μM. It is primarily utilized in cancer research.
  • 1.368 €
6-8 weeks
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NPD10084
T870331040706-91-9
NPD10084 is an inhibitor that targets the pyruvate kinase M2 subtype (PKM2). NPD10084 inhibits downstream signaling by interfering with protein-protein interactions between PKM2 and β-catenin or STAT3 through its action on the non-glucolytic signaling function of PKM2, thereby exhibiting antiproliferative activity against multiple colorectal cancer cell lines (in vitro IC50 range: 0.8–1.9 μM).
  • 31 €
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Mitapivat hydrochloride
AG-348 hydrochloride
T2061722559738-69-9
Mitapivat (AG-348) hydrochloride is an orally active and selective allosteric activator of pyruvate kinase R (PK-R). It enhances the PK-R-catalyzed conversion of phosphoenolpyruvate to pyruvate, thereby promoting the glycolysis pathway, increasing ATP production in red blood cells, and decreasing 2,3-diphosphoglycerate (2,3-DPG) levels. Mitapivat hydrochloride is being investigated for potential use in the study of pyruvate kinase deficiency and other anemia-related disorders.
  • Inquiry Price
10-14 weeks
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PKM2-IN-9
T204898498568-75-5
PKM2-IN-9 (compound C1) is a potent inhibitor of PKM2, demonstrating a 75% inhibition rate at 50 μM. It plays a significant role in cancer research.
  • 1.503 €
8-10 weeks
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Vitamin K5 hydrochloride
T87621130-24-5
Vitamin K5 hydrochloride is a photosensitizer and antimicrobial agent that functions as a specific inhibitor of pyruvate kinase M2 (PKM2), with IC50 values of 28 μM for PKM2, 191 μM for PKM1, and 120 μM for PKL. Vitamin K5 hydrochloride induces apoptosis in colon 26 cells, supporting its application in infection and cancer research as well as its practical use as a preservative in pharmaceutical, food, and beverage formulations.
  • 27 €
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PKR Inhibitor, negative control
T209999852547-30-9
The PKR Inhibitor, negative control, is an inactive structural analog of RNA-dependent protein kinase (PKR) inhibitors, serving as a negative control. Additionally, it can inhibit LK-induced neuronal death, demonstrating significant neuroprotective properties.
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10-14 weeks
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