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Pyruvate kinase activators and inhibitors act on the enzyme that catalyzes the final step of glycolysis. Pyruvate kinase transfers phosphate from phosphoenolpyruvate to adenosine diphosphate (ADP), producing pyruvate and adenosine triphosphate (ATP). The M2 isoform (PKM2), expressed in proliferating cells, switches between active tetramers and less active dimers. In 2008 PKM2 was shown to support aerobic glycolysis and tumor growth in xenografts. TEPP-46 and DASA-58 activate PKM2 by promoting tetramer formation, as reported in 2012. Mitapivat is an activator of pyruvate kinase isoforms, including the red blood cell enzyme. Shikonin, listed as (Rac)-Shikonin, and PKM2-IN-1 inhibit PKM2 in studies of cancer cell glycolysis. Several other entries have no direct link to pyruvate kinase.
Shikonin, a component of chinese herbal medicine, inhibits chemokine receptor function and suppresses human immunodeficiency virus type 1.
Iminostilbene is a well-characterized inhibitor of COX2 (Cyclooxygenase-2) with additional activity against PKM2 (Pyruvate Kinase M2). This compound effectively reduces the expression of COX2 and iNOS, as well as the release of pro-inflammatory cytokines such as IL-1β, IL-6, TNF-α, and MCP-1 in macrophages. Its ability to mitigate macrophage-mediated inflammatory responses makes iminostilbene a valuable reagent for investigating mechanisms of inflammation regulation, cardiovascular disease, including myocardial ischemia/reperfusion injury, and immune-related disorders.
PKM2-IN-1 is a pyruvate kinase M2 (PKM2) inhibitor with an IC50 of 2.95 μM.
PKM2/PDK1-IN-1 is a dual inhibitor targeting pyruvate kinase M2 (PKM2) and pyruvate dehydrogenase kinase 1 (PDK1). It demonstrates significant biological activity by inhibiting the proliferation of non-small cell lung cancer (NSCLC) cells and inducing apoptosis. This compound promotes intercellular reactive oxygen species (ROS) production and modulates apoptotic proteins, engaging both mitochondrial and death receptor pathways in cancer cell death. Its unique mechanism makes it a valuable tool for research in cancer biology and therapeutic development.
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Synonyms: C.I. 75535; Isoarnebin 4
Shikonin is a potent inhibitor of the TMEM16A chloride channel, exhibiting an IC50 value of 6.5 μM. This compound functions as a specific inhibitor of pyruvate kinase M2 (PKM2) and also modulates inflammatory pathways by inhibiting TNF-α and NF-κB activation. In addition, Shikonin decreases exosome secretion by impairing glycolytic processes and effectively inhibits AIM2 inflammasome activation. Its diverse activities make it a valuable reagent for investigating cellular signaling and inflammatory responses in research applications.
PKR-IN-1 is an inhibitor of pyruvate kinase, demonstrating potent antifungal activity with an EC50 of 0.21 μg/mL against Rhizoctonia solani. Its primary mechanism involves the inhibition of glycolytic metabolism, which is crucial for fungal growth and survival. This compound is valuable for research applications focused on the development of antifungal strategies and the study of metabolic pathways in fungi.
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PKM2-IN-6 is a potent inhibitor of pyruvate kinase M2 (PKM2), exhibiting an IC50 value of 23 nM. This compound induces apoptosis and facilitates cell cycle arrest at the G2 phase, demonstrating significant anticancer activity. PKM2-IN-6 also decreases the mRNA levels of both PKM1 and PKM2, indicating its effect on metabolic regulation. This reagent is particularly relevant for research applications focused on triple-negative breast cancer.
Vitamin K5 hydrochloride is a specific inhibitor of pyruvate kinase M2 (PKM2), with reported IC50 values of 28, 191, and 120 μM for PKM2, PKM1, and PKL, respectively. This compound exhibits significant biological activity by inducing apoptosis in colon 26 cancer cells, making it relevant for cancer research. Additionally, Vitamin K5 hydrochloride serves as a photosensitizer and antimicrobial agent, and it is applicable in the study of infections as well as a potential preservative in pharmaceuticals, foods, and beverages.
MTP is a potent inhibitor of pyruvate kinase M2 (PKM2) that induces apoptosis in cancer cells through the modulation of caspase-3 activation. Additionally, MTP promotes autophagy and enhances reactive oxygen species (ROS) generation, while also inhibiting JAK2 signaling pathways. This compound is particularly valuable for research applications focused on oral squamous cell carcinoma and related cancer studies.
PKM2 modulator 2 (compound C599) is a potent inhibitor of pyruvate kinase M2 (PKM2), a key regulator of cellular metabolism. This compound exhibits significant antiproliferative activity and induces apoptosis in various cancer cell lines. PKM2 modulator 2 is a valuable tool for research on glioblastoma and other malignancies where PKM2 plays a critical role in tumorigenesis.
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Synonyms: Synkamin; Synkamin base
Vitamin K5 is a specific inhibitor of pyruvate kinase M2 (PKM2), exhibiting IC50 values of 28, 191, and 120 μM against PKM2, PKM1, and PKL, respectively. It demonstrates notable biological activity by inducing apoptosis in colon 26 cells, making it relevant for cancer research. Furthermore, Vitamin K5 possesses antimicrobial properties and may be employed in studies related to infection. Its applications also extend to the preservation of pharmaceuticals, foods, and beverages.
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LIQ1 is a potent allosteric inhibitor of Pyruvate kinase M2 (PKM2), targeting Arg43 within the polyarginine pocket with an IC50 of 0.39 μM and a Kd of 4.5 μM. This flavonoid derivative effectively prevents the nuclear translocation of PKM2 and its interaction with HIF-1α, leading to the suppression of IL-1β transcription. LIQ1 is valuable for research involving endotoxemic conditions, particularly in studies of inflammation and metabolic regulation.
PT109 is a potent inhibitor of the protein-targeting poly(A)-binding protein 1 (PTBP1). By promoting the conversion of the pyruvate kinase isoform from PKM2 to PKM1, PT109 effectively suppresses the proliferation and migration of glioblastoma multiforme and facilitates its reprogramming into oligodendrocytes. Additionally, PT109 interacts with key signaling pathways, including JNK, SGK1, and GSK3β, conferring neuroprotective effects that enhance neurogenesis, foster synapse formation, and mitigate neuroinflammation. In models of Alzheimer's disease, PT109 demonstrates significant improvements in spatial learning, making it a valuable tool for researching metabolic reprogramming in glioblastoma and neuroprotection in neurodegenerative disorders.
SET-171 is a selective JNK (c-Jun N-terminal kinase) inhibitor that demonstrates notable anticancer properties and regulation of lipid metabolism through the suppression of liver pyruvate kinase (PKL) expression. In vitro studies reveal IC50 values of 8.82 μM and 2.97 μM against HepG2 and Huh7 cell lines, respectively, showcasing its potent cytotoxic effects. Furthermore, SET-171 has been shown to significantly decrease triacylglycerol (TAG) levels and inhibit steatosis-related protein expression, highlighting its potential utility in the study of hepatocellular carcinoma (HCC) and non-alcoholic fatty liver disease (NAFLD).
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ZIP is a selective peptide inhibitor of Protein Kinase M zeta (PKMζ), which plays a crucial role in synaptic plasticity and memory processes. This compound effectively impairs morphine-induced conditioned place preference, making it a valuable tool for studying addiction and the molecular mechanisms underlying memory formation. Research applications include investigating the role of PKMζ in memory reinforcement and the modulation of synaptic strength.
Synonyms: 7-Desacetoxy-6,7-dehydrogedunin
7DG (7-Desacetoxy-6,7-dehydrogedunin) is a selective inhibitor of protein kinase R (PKR). It is known for its ability to shield macrophages from pyroptosis induced by lethal toxins, thereby playing a crucial role in cell survival during inflammatory responses. This compound is valuable for research focused on understanding immune pathways and studying the mechanisms of cell death.
PKM2-IN-7 is a selective inhibitor of pyruvate kinase M2 (PKM2) that disrupts the interaction between PKM2 and ALDH1A3, demonstrating minimal toxicity to normal cells. This compound is pivotal for investigations into tumor biology, making it an essential tool for research focused on cancer metabolism and tumorigenesis.
PKM2-IN-3 is a selective inhibitor of the PKM2 kinase, demonstrating an IC50 value of 4.1 μM. This compound exhibits notable anti-neuroinflammatory effects by disrupting PKM2-mediated glycolysis and inhibiting NLRP3 activation. PKM2-IN-3 is suitable for research applications focused on metabolic regulation and neuroinflammation pathways.
Malonyl-NAC is a specific inhibitor of GAPDH malonylation that leads to decreased endogenous GAPDH activity in cells. This reagent enhances GAPDH malonylation and concurrently inhibits pyruvate kinase activity. It has been shown to limit metabolism and proliferation in highly glycolytic kidney cancer cell lines possessing tricarboxylic acid cycle mutations, making it a valuable tool for investigating metabolic alterations in cancer research.
CIAC001 is a potent inhibitor of Pyruvate Kinase M2 (PKM2), demonstrating noteworthy anti-neuroinflammatory properties. It effectively suppresses LPS-induced nitric oxide (NO) production in BV-2 microglial cells, with an IC50 of 2.5 μM, and exhibits protective effects against neuroinflammation in various mouse models. Additionally, CIAC001 has shown the potential to inhibit aspects of chronic morphine-induced addiction, making it a valuable reagent for research into neuroinflammatory processes and addiction pathways.
NPD10084 is a potent inhibitor of pyruvate kinase M2 (PKM2) that targets non-glycolytic signaling in cancer cells. By disrupting the interaction between PKM2 and key regulatory proteins such as β-catenin and STAT3, NPD10084 effectively inhibits downstream signaling pathways. This compound exhibits significant antiproliferative activity against colorectal cancer cells, making it a valuable tool for cancer research and therapeutic investigations.
Deoxytopsentin is a marine bisindole alkaloid that functions as an inhibitor of pyruvate kinase in methicillin-resistant Staphylococcus aureus (MRSA). This compound demonstrates significant antibacterial activity against MRSA strains in vitro. Deoxytopsentin is derived from sponges and serves as a valuable research tool for studying bacterial metabolism and developing therapies targeting antibiotic-resistant infections.
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PKM2-IN-4 is a selective inhibitor of pyruvate kinase M2 (PKM2), exhibiting an IC50 of 0.35 μM. This compound is known to regulate pyruvate-dependent respiration and promotes mitochondrial H2O2 production, impacting the efficiency of the electron transport system. It serves as a valuable tool in research focused on metabolism, cancer biology, and oxidative stress.
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PKM2-IN-9 is a selective inhibitor of pyruvate kinase M2 (PKM2), achieving an inhibition rate of 75% at a concentration of 50 μM. This compound is of significant interest in cancer research, as it regulates metabolic pathways essential for tumor growth and survival. PKM2-IN-9 can be utilized to explore the role of PKM2 in cellular processes and as a potential therapeutic target in various types of cancer.
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Alkannin is a selective inhibitor of tumor-specific pyruvate kinase-M2 (PKM2), demonstrating potent activity without affecting PKM1 or pyruvate kinase-L (PKL). This compound has potential applications in cancer research, serving as a valuable tool for studying metabolic alterations in tumors and developing anticancer strategies. Alkannin's specificity for PKM2 highlights its utility in targeted therapeutic approaches in oncology.
