Catalog No.
Product Name
Application
Product Information
Citations
- Benserazid hydrochloride is an inhibitor of L-aromatic amino acid decarboxylase.
-
PTEN Inhibitor
Shikonin, a component of chinese herbal medicine, inhibits chemokine receptor function and suppresses human immunodeficiency virus type 1.- Yang J, .et al. , Biomed Pharmacother, 2017, Sep;93:1343-1357 PMID: 28753907
- 7-Hydroxyflavone is an orally active flavonoid isolated from *Clerodendrum phlomidis*, exhibiting notable anti-inflammatory activity. It protects renal cells from nicotine-induced cytotoxicity through activation of the ERK/Nrf2/HO-1 signaling pathway. Additionally, 7-Hydroxyflavone inhibits PKM2 with an IC50 of 2.12 μM, and suppresses COX-2 and 5-LOX with IC50 values of 27 μg/mL and 33 μg/mL, respectively.
-
COX2 Inhibitor
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/PDK1 Inhibitor
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. -
Stable Isotope
Iminostilbene-d10 is a deuterated derivative of Iminostilbene, functioning as a stable isotope that aids in biological tracking and analytical studies. This compound serves as a precursor for carbamazepine and acts as an orally active inhibitor of pyruvate kinase M2 (PKM2) and cyclooxygenase-2 (COX2). Iminostilbene-d10 is instrumental in research exploring inflammation regulation, cardiovascular diseases, and immune-related disorders, as it modulates cytokine release and mitigates macrophage-mediated inflammatory responses. Its unique properties make it a valuable tool for studying myocardial ischemia/reperfusion injury and related pathways. -
Chloride Channel Inhibitor
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. -
Antibiotic
Cyclamidomycin is an acrylamide antibiotic that primarily targets nucleoside diphosphate kinase and pyruvate kinase in Escherichia coli, along with impairing oxidative phosphorylation in rat liver mitochondria. It exhibits broad-spectrum antibacterial activity against various bacteria, including Staphylococcus aureus, Micrococcus flavus, Staphylococcus lutea, Bacillus subtilis, Escherichia coli, Shigella flexneri, Salmonella typhosa, Proteus vulgaris, and Klebsiella pneumoniae, with minimum inhibitory concentrations ranging from 3.12 to 25 mg/ml. This compound is valuable for research on bacterial infections and mitochondrial function. -
Pyruvate Kinase Inhibitor
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. -
PKM2 Inhibitor
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 Inhibitor
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. -
PKM2 Inhibitor
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. -
PKM2 Inhibitor
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. -
Antifungal Agent
(E)-2-Octenal is an antifungal agent that disrupts cell membrane integrity and induces reactive oxygen species (ROS) accumulation. It effectively decreases the activity of phosphofructokinase and pyruvate kinase, inhibiting the growth of Neofusicoccum parvum by impairing mitochondrial energy metabolism. Additionally, (E)-2-Octenal demonstrates broad-spectrum efficacy against various fungi, including Sclerotium rolfsii, Metarhizium anisopliae sensu lato, and Aspergillus flavus, making it valuable for research on citrus blue mold and mango stem-end rot. -
PKM2 Inhibitor
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. -
PTBP1 Inhibitor
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. -
PKM2 Inhibitor
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. -
INK Inhibitor
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). -
PKMζ Inhibitor
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. -
Purine Nucleotide Biosynthesis Intermediate
SAICAR is a key intermediate in the de novo purine nucleotide biosynthesis pathway. It selectively activates the pyruvate kinase isoform M2 (PKM2) with an EC50 of 0.3 mM, enhancing the enzymatic activity. This compound is particularly relevant for research into cancer cell metabolism, as it promotes survival under glucose-limited conditions, making it a valuable tool in the investigation of tumor biology and metabolic regulation. -
PKM2 Inhibitor
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. -
Glycolytic Enzyme
Pyruvate Kinase, Microorganism, is a glycolytic enzyme that catalyzes the conversion of phosphoenolpyruvate and ADP into pyruvate and ATP. This enzyme plays a crucial role in cellular energy metabolism and is essential for glycolysis. It is widely used in biochemical research to study metabolic pathways and enzyme kinetics in various microorganisms. -
Pyruvate Kinase-R Activator
Tebapivat is a potent activator of pyruvate kinase-R (PKR), playing a critical role in enhancing glycolytic flux and energy metabolism. Its ability to stimulate PKR makes it valuable in research on metabolic disorders and cancer, where glycolysis is often dysregulated. Tebapivat can be utilized to investigate the effects of PKR activation on cellular energy production and related biochemical pathways. -
PKM2 Activator
PKM2 activator 2 is a potent activator of pyruvate kinase M2 (PKM2) with an AC50 value of 66 nM. This compound effectively enhances PKM2 activity, facilitating the restoration of normal glycolytic metabolism in various cellular models. It is valuable for research applications focusing on cancer metabolism and cellular energy regulation, offering insights into metabolic reprogramming in tumors. -
Pyruvate Kinase Activator
Etavopivat is a selective erythrocyte pyruvate kinase (PKR) activator that enhances glycolytic flux in red blood cells. It exhibits significant antisickling effects, making it a valuable tool for investigating sickle cell disease and other hemoglobinopathies. This compound is of interest in research aimed at improving red blood cell function and mitigating the complications associated with abnormal hemoglobin disorders. -
PKM2 Kinase Inhibitor
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. -
GAPDH malonylation
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. -
PKM2 Activator
PKM2 activator 5 is a selective activator of pyruvate kinase M2 (PKM2) with an AC50 value of 0.316 µM. This compound modulates the metabolic pathways of cancer cells by enhancing PKM2 activity, thereby promoting a shift from aerobic to anaerobic metabolism. PKM2 activator 5 has applications in cancer research, particularly in studies focused on metabolic reprogramming and the development of novel therapeutic strategies targeting cancer metabolism. -
PKM2 Inhibitor
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. -
PKM2 Inhibitor
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. -
MRSA Pyruvate Kinase Inhibitor
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. -
AADC/PKM2 Inhibitor
Benserazide is an inhibitor of aromatic L-amino acid decarboxylase (AADC) and L-DOPA decarboxylase, primarily targeting the PKM2 enzyme. By binding directly to PKM2, Benserazide inhibits its activity, resulting in the suppression of aerobic glycolysis and the concurrent upregulation of oxidative phosphorylation (OXPHOS). This compound is valuable for research applications related to Parkinson's disease and melanoma. -
Pyruvate Kinase-R Activator
PKR Activator 1 is a potent activator of pyruvate kinase-R (PKR), facilitating enhanced glycolytic flux and promoting overall metabolic activity. This compound is instrumental in studies exploring metabolic disorders, cancer metabolism, and the regulation of cellular energy pathways. With its ability to modulate PKR activity, PKR Activator 1 serves as a valuable tool for researchers investigating the role of PKR in various biological contexts. -
PKM2 Activator
PF-06284674 is a potent activator of PKM2, a key enzyme involved in cancer metabolism. This compound enhances the activity of PKM2, promoting metabolic switching and cellular proliferation. It is primarily utilized in cancer research, particularly studies focused on targeting metabolic pathways for therapeutic intervention. -
Pyruvate Kinase Activator
ML202 is a potent allosteric activator of human pyruvate kinase M2 (hPK-M2), designed to enhance the enzyme's activity by modulating the cooperativity of phosphoenolpyruvate (PEP) binding. It specifically influences the PEP binding site with minimal impact on adenosine diphosphate (ADP) binding. This compound is valuable for studying metabolic pathways and cellular energy regulation, making it a useful tool in cancer research and metabolic studies. -
PKR Activator
(Rac)-Etavopivat is an isomer of Etavopivat and functions as an activator of erythrocyte pyruvate kinase-R (PKR). This compound exhibits the potential to enhance glycolytic flux in erythrocytes, making it valuable for research on sickle cell disease and other hemoglobinopathies. Its oral bioavailability allows for convenient dosing in in vitro and in vivo studies, supporting investigations into erythrocyte metabolism and therapeutic strategies. -
PKR Activator
PKR Activator 5 (Compound 18) is a potent activator of pyruvate kinase R (PKR), exhibiting an AC50 of 28 nM. This compound enhances PKR activity, which plays a critical role in regulating glycolysis and energy metabolism. PKR Activator 5 is valuable for research applications aimed at understanding the metabolic pathways associated with PKR and their implications in cancer and metabolic disorders. -
PKM2 Activator
PKM2 activator 10 is a selective activator of the pyruvate kinase M2 (PKM2) enzyme, promoting its tetrameric form and enhancing glycolytic activity. This compound demonstrates significant anti-tumor activity, making it a valuable tool in cancer research. Its ability to modulate metabolic pathways provides insights into therapeutic strategies for cancer treatment and metabolic disorders. -
PKM2 Activator
PKM2 Activator 4 is a potent activator of the pyruvate kinase M2 (PKM2) enzyme, exhibiting an AC50 value in the range of 1-10 μM. This compound is primarily utilized in cancer research, where modulation of PKM2 activity may influence metabolic pathways involved in tumor growth and cell proliferation. Its role in enhancing PKM2 function makes it a valuable tool for investigating cancer metabolism and potential therapeutic strategies. -
PK Activator
Mitapivat hemisulfate is an orally active allosteric activator of pyruvate kinase (PK). This compound enhances enzymatic activity, improves protein stability, and elevates ATP levels across various PKLR genotypes, making it a potential therapeutic option for restoring function in PK-deficient glycolytic pathways. Mitapivat hemisulfate is suitable for research applications focused on PK deficiency and metabolic disorders. -
Pyruvate Kinase Activator
Mitapivat hemisulfate sesquihydrate is an orally active allosteric activator of pyruvate kinase (PK). This compound enhances enzymatic activity and protein stability while increasing ATP levels across various PKLR genotypes. Mitapivat is instrumental in studying pyruvate kinase deficiencies and has significant implications for restoring glycolytic pathway activity in affected cells. -
PK-R Activator
Mitapivat hydrochloride is a selective allosteric activator of pyruvate kinase R (PK-R). By enhancing the enzymatic activity of PK-R, it facilitates the conversion of phosphoenolpyruvate to pyruvate, promoting glycolysis and leading to increased ATP production in red blood cells while decreasing levels of 2,3-diphosphoglycerate. This compound shows potential for investigational studies related to pyruvate kinase deficiency and various anemia-related disorders. -
PKM2 Inhibitor
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. -
PKM2 Inhibitor
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. -
PKM2 Activator
PKM2 activator 3 is a potent activator of pyruvate kinase M2 (PKM2), exhibiting an AC50 value of 90 nM. This compound demonstrates favorable Caco-2 permeability, low efflux ratio, and high microsomal stability, making it an advantageous tool for in vitro studies. PKM2 activator 3 is primarily utilized in cancer research, facilitating the investigation of metabolic pathways and potential therapeutic strategies targeting PKM2.
