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Metabolism

Acetyl-CoA Carboxylase

Amino Acids and Derivatives

Angiotensin-converting Enzyme (ACE)

Endogenous Metabolite

Glutathione Peroxidase

(73)

Glyoxalase

(17)

HIF/HIF Prolyl-Hydroxylase

Indoleamine 2,3-Dioxygenase (IDO)

(98)

Isocitrate Dehydrogenase (IDH)

Mitochondrial Metabolism

(212)

N-Acetylglucosaminyltransferase

Procollagen C Proteinase

(1)

Prolyl Endopeptidase (PREP)

Reactive Oxygen Species

Serine/threonin kinase

(90)

Stearoyl-CoA Desaturase (SCD)

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.

Filter HomeSignaling PathwaysMetabolismPKM

TEPP-46

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.

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Mitapivat

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.

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(+)-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.

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PKM2-IN-1

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.

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Mitapivat sulfate hydrate

T698652151847-10-6

Mitapivat sulfate hydrate (AG 348 sulfate hydrate) is an erythrocyte pyruvate kinase (PK) allosteric activator. It enhances enzyme activity, protein stability, and ATP levels in various PKLR genotypes and can be used in pyruvate kinase deficiency research.

$293

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DASA-58

T68161203494-49-8

DASA-58 is a specific and potent Pyruvate kinase M2 (PKM2) activator.

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PKR-IN-2

T124991628428-01-2

PKR-IN-2 is a activator of pyruvate kinase (PKR).

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PKM2 inhibitor G

T67900904457-46-1

PKM2 inhibitor G is a inhibitor of pyruvate kinase.

$195

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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.

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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.

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Disodium monofluorophosphate

T074510163-15-2

Disodium monofluorophosphate (NSC248) is a competitive inhibitor of pyruvate kinase and alkaline phosphatase, which also irreversibly inhibits phosphorylase phosphatase.

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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.

$195

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(Rac)-Etavopivat

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].

$1,670

6-8 weeks

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Benserazide

T1517L322-35-0

Benserazide is an inhibitor of dopa decarboxylase. It is often given with levodopa in the treatment of Parkinson's to prevent the conversion of levodopa to dopamine in the periphery, thereby increasing the amount that reaches the central nervous system an

$1,520

6-8 weeks

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PKM2-IN-10

T207198

PKM2-IN-10 is a PKM2 inhibitor. It effectively suppresses the proliferation of A549 and HCC1833 cell lines with IC50 values of 3.36 μM and 9.20 μM, respectively. PKM2-IN-10 demonstrates antitumor activity in human non-small cell lung cancer (NSCLC) and mouse lung adenocarcinoma models. It is applicable for research in lung cancer.

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PKM2-IN-3

T399842408841-19-8

PKM2-IN-3 is a potent PKM2 kinase inhibitor, displaying an IC 50 value of 4.1 μM. The compound effectively suppresses PKM2-mediated glycolysis and NLRP3 activation, thereby exerting an anti-neuroinflammatory effect.

$970

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Alkannin

T6058123444-65-7

Alkannin is a potent and specific inhibitor of tumor-specific pyruvate kinase-M2 (PKM2) without affecting PKM1 or pyruvate kinase-L (PKL), making it a potential anticancer agent [1].

$1,520

10-14 weeks

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PKCζ/ι pseudosubstrate inhibitor

T80071799764-07-1

PKCζ ι pseudosubstrate inhibitor demonstrates comprehensive inhibitory activity across the protein kinase C (PKC) family and is associated with the induction of memory impairment [1].

$348

35 days

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PKM2-IN-4

T79636

Compound 5C, referred to as Pkm2-in-4, is a selective PKM2 inhibitor (IC50 = 0.35 µM) that modulates pyruvate-dependent respiration and promotes mitochondrial H2O2 production rate and electron transport system coupling [1].

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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.

6-8 weeks

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PKM2 modulator 1

T205207

PKM2 modulator 1 (compound C998) is an effective PKM2 inhibitor with antiproliferative activity. It induces apoptosis and holds potential for research in glioblastoma studies.

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PKM2 activator 3

T615041346113-84-5

PKM2 activator 3 is a highly potent compound that activates PKM2, with an AC 50 value of 90 nM. It exhibits excellent Caco-2 permeability, a low efflux ratio, and remarkable microsomal stability. PKM2 activator 3 is particularly valuable for anticancer research purposes [1]. (AC 50: the concentration at which 50% enzyme activation occurs.)

$1,520

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.