2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. Pyruvate Kinase
  5. Pyruvate Kinase Inhibitor

Pyruvate Kinase Inhibitor

Pyruvate Kinase Inhibitors (50):

Cat. No. Product Name Effect Purity
  • HY-N0822
    Shikonin
    		Inhibitor 99.80%
    Shikonin is a major component of a Chinese herbal medicine named zicao. Shikonin is a potent TMEM16A chloride channel inhibitor with an IC50 of 6.5 μM. Shikonin is a specific pyruvate kinase M2 (PKM2) inhibitor and can also inhibit TNF-α and NF-κB pathway. Shikonin decreases exosome secretion through the inhibition of glycolysis. Shikonin inhibits AIM2 inflammasome activation.
  • HY-103617
    PKM2-IN-1
    		Inhibitor 99.79%
    PKM2-IN-1 (compound 3k) is a pyruvate kinase M2 (PKM2) inhibitor with an IC50 of 2.95 μM.
  • HY-B0404A
    Benserazide hydrochloride
    		Inhibitor 99.68%
    Benserazide hydrochloride (Serazide) is an aromatic L-amino acid decarboxylase (AADC) and L-DOPA decarboxylase inhibitor. Benserazide hydrochloride is also a PKM2 inhibitor. Benserazide hydrochloride directly binds to and blocks PKM2 enzyme activity, leading to inhibition of aerobic glycolysis concurrent up-regulation of OXPHOS. Benserazide hydrochloride can be used for the study of Parkinson's disease and melanoma.
  • HY-W134163
    (E)-2-Octenal
    		Inhibitor 99.29%
    (E)-2-Octenal is an Antifungal agent. (E)-2-Octenal disrupts cell membrane integrity and causes ROS accumulation. (E)-2-Octenal decreases the activities of phosphofructokinase and pyruvate kinase. (E)-2-Octenal inhibits Neofusicoccum parvum growth by disrupting mitochondrial energy metabolism. (E)-2-Octenal suppresses the growth of a Prochloraz (HY-B0845)-resistant Penicillium italicum strain. (E)-2-octenal exerts a broad-spectrum and potent inhibitory effect on various fungi, including Sclerotium rolfsii, Metarhizium anisopliae sensu lato, and Aspergillus flavus, etc. (E)-2-Octenal can be used for the research of citrus blue mold and mango stem-end rot.
  • HY-179371
    LIQ1
    		Inhibitor
    LIQ1, a flavonoid derivative, is a potent Pyruvate kinase M2 (PKM2) allosteric inhibitor (IC50 = 0.39 μM; Kd = 4.5 μM) targeting Arg43 within the polyarginine pocket. LIQ1 exhibits efficacy in a mouse model of LPS (HY-D1056)-induced endotoxemia, preventing the nuclear translocation of PKM2 and inhibiting its binding to HIF-1α, thereby suppressing IL-1β transcription. LIQ1 can be used for the research of endotoxemia[1].
  • HY-183765
    PARP1/PKM2-IN-1
    		Inhibitor
    PARP1/PKM2-IN-1 is a dual PARP1/PKM2 inhibitor, with an IC50 of 39.5 nM against PARP1, and IC50 values of 261 nM (recombinant PKM2) and 50 nM (dimeric PKM2) against PKM2. PARP1/PKM2-IN-1 reduces the dimerization of PKM2 and decreases its nuclear accumulation level. PARP1/PKM2-IN-1 also selectively downregulates PKM2 mRNA and impairs poly (ADP-ribose)-mediated nuclear retention of PKM2. PARP1/PKM2-IN-1 exhibits antiproliferative activity and inhibits the formation of 3D cancer spheroids. PARP1/PKM2-IN-1 can be used in research related to mammary adenocarcinoma, triple-negative breast cancer, BRCA1-mutant triple-negative breast cancer, and prostate adenocarcinoma.
  • HY-162080
    METTL1-WDR4-IN-1
    		Inhibitor 99.61%
    METTL1-WDR4-IN-1 (Compound 1) is a selective competitive inhibitor of the methyltransferase complex METTL1-WDR4 (IC50 = 144 μM). METTL1-WDR4-IN-1 inhibits the m7G methyltransferase activity of the METTL1-WDR4 complex, blocking m7G modification of PKM mRNA, reducing PKM2 protein expression, disrupting the METTL1/PKM2/H3K9la positive feedback loop, and simultaneously inhibiting PKM2 nuclear translocation-mediated CD155 transcriptional activation. METTL1-WDR4-IN-1 can inhibit tumor cell proliferation, weaken glycolytic metabolism, reverse tumor immune evasion (restoring NK cell and CD8+ T cell function), and regulate RNA epigenetic modification and the tumor immune microenvironment. METTL1-WDR4-IN-1 can be used in immunotherapy research for cancers such as colorectal cancer, and is particularly suitable for use in combination with PKM2 inhibitors to enhance anti-tumor treatment efficacy.
  • HY-N7108
    7-Hydroxyflavone
    		Inhibitor 99.89%
    7-Hydroxyflavone is a flavonoid isolated from Clerodendrum phlomidis, with anti-inflammatory activity. 7-Hydroxyflavone protects renal cells from nicotine (NIC)-associated cytotoxicity via the ERK/Nrf2/HO-1 pathway. 7-Hydroxyflavone inhibits PKM2 with an IC50 of 2.12 μM. 7-Hydroxyflavone inhibits COX-2 and 5-LOX with IC50 of 27 µg/mL and 33 µg/mL. 7-Hydroxyflavone is orally active.
  • HY-157913
    PKM2-IN-6
    		Inhibitor 99.95%
    PKM2-IN-6 (compound 7d) is a potent and orally active PKM2 inhibitor with an IC50 value of 23 nM. PKM2-IN-6 induces apoptosis and cell cycle arrest at G2 phase. PKM2-IN-6 reduces the level of PKM1 and PKM2 at the mRNA level. PKM2-IN-6 shows anticancer activity and has the potential for the research of triple-negative breast cancer.
  • HY-157395
    malonyl-NAC
    		Inhibitor 98.74%
    malonyl-NAC increases cellular propylation, resulting in reduced endogenous GAPDH activity. malonyl-NAC increases GAPDH malonylation in cells and inhibits pyruvate kinase activity. In addition, malonyl-NAC limits the metabolism and proliferation of a highly glycolytic kidney cancer cell line harboring a tricarboxylic acid cycle mutation.
  • HY-161337
    PKL-IN-1
    		Inhibitor 99.29%
    PKL-IN-1 is a potent inhibitor of pyruvate kinase (PKL) with an IC50 of 0.07 μM. PKL-IN-1 can be used in the study of non-alcoholic fatty liver disease.
  • HY-139667
    PKM2-IN-3
    		Inhibitor 99.44%
    PKM2-IN-3 is an inhibitor of PKM2 kinase with an IC50 value of 4.1 μM. PKM2-IN-3 exhibits an anti-neuroinflammatory effect by inhibiting PKM2-mediated glycolysis and NLRP3 activation.
  • HY-121275
    Benserazide
    		Inhibitor 98.43%
    Benserazide is an aromatic L-amino acid decarboxylase (AADC) and L-DOPA decarboxylase inhibitor. Benserazide is also a PKM2 inhibitor. Benserazide directly binds to and blocks PKM2 enzyme activity, leading to inhibition of aerobic glycolysis concurrent up-regulation of OXPHOS. Benserazide can be used for the study of Parkinson's disease and melanoma.
  • HY-N2552
    Vitamin K5 hydrochloride
    		Inhibitor 99.25%
    Vitamin K5 hydrochloride is a photosensitizer and a antimicrobial agent. Vitamin K5 hydrochloride is a specific PKM2 inhibitor with IC50 values of 28, 191 and 120 μM for PKM2, PKM1 and PKL. Vitamin K5 hydrochloride induces apoptosis of colon 26 cells. Vitamin K5 hydrochloride can be used for the research of infection and cancer, and it also can be used as a preservative for pharmaceuticals, foods, and beverages.
  • HY-N3011
    Iridin
    		Inhibitor 99.72%
    Iridin is an orally active natural isoflavone. Iridin inhibits the PI3K/AKT and PKM2 signaling pathways, and downregulates the JAK/STAT and NF-κB pathways. Iridin induces Fas-mediated extrinsic apoptosis, G2/M cell cycle arrest, and inhibits cell proliferation. Iridin reduces inflammation, inhibits ROS production, suppresses glycolysis, and also exhibits antioxidant and antidiabetic activities. Iridin can be used in research related to gastric cancer and acute lung injury.
  • HY-155850
    CIAC001
    		Inhibitor 99.70%
    CIAC001 is a Pyruvate Kinase PKM2 inhibitor with anti-neuroinflammatory activity. CIAC001 inhibits LPS-induced proinflammatory nitric oxide (NO) production and protects immunologically active BV-2 cells (IC50=2.5 μM). CIAC001 also has anti-neuroinflammation in mouse models and inhibits chronic morphine-induced addiction.
  • HY-148615
    NPD10084
    		Inhibitor 99.69%
    NPD10084 is a pyruvate kinase PKM2 inhibitor that inhibits non-glycolytic signaling in cancer cells. NPD10084 disrupts the interaction between PKM2 and β-catenin or STAT3 and inhibits downstream signaling. NPD10084 has antiproliferative activity against colorectal cancer cells in vitro and in vivo.
  • HY-N7064
    Iminostilbene
    		Inhibitor 99.34%
    Iminostilbene is a chemical precursor of carbamazepine. Additionally, Iminostilbene is an orally active inhibitor of PKM2 (Pyruvate Kinase M2) and COX2 (Cyclooxygenase-2). Iminostilbene exerts its effects by inhibiting PKM2 and its interaction with HIF-1α and STAT3, reducing COX2 and iNOS expression, and decreasing LPS-induced release of IL-1β, IL-6, TNF-α, and MCP-1, thereby suppressing macrophage-mediated inflammatory responses and improving myocardial ischemia/reperfusion (MI/R) injury. Iminostilbene holds promise for research in inflammation regulation, cardiovascular diseases (such as MI/R injury), and macrophage-mediated immune-related diseases.
  • HY-W319647
    GCN2 activator-1
    		Inhibitor 99.69%
    GCN2 activator-1 (Compound 20) is a GCN2 activator. GCN2 activator-1 binds within the ATP-pocket of GCN2 and activates GCN2 in a GCN1-independent manner. GCN2 activator-1 activates Integrated Stress Response (ISR) in cells. GCN2 activator-1 inhibits PKR with an IC50 of 3.75 µM. GCN2 activator-1 can be used for research of pulmonary veno-occlusive disease (PVOD).
  • HY-N15451
    Deoxytopsentin
    		Inhibitor 99.42%
    Deoxytopsentin (compound 5) is a marine bisindole alkaloid and also a MRSA pyruvate kinase inhibitor. Deoxytopsentin exists in sponges. Deoxytopsentin exhibits antibacterial activity against methicillin-resistant Staphylococcus aureus strains in vitro.