pyruvate kinase m2

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

DL-Serine is a non-essential amino acid and a natural ligand and allosteric activator of pyruvate kinase M2.

FX-11 (LDHA Inhibitor FX11) is a highly potent, selective, and competitive inhibitor of lactate dehydrogenase A (LDHA), with a Ki value of 8 μM for LDHA. FX-11 acts as an activator of PKM2 (pyruvate kinase M2). FX-11 exerts its antitumor effects by inhibiting glycolysis, depleting ATP, and inducing oxidative stress and apoptosis. FX-11 can be used in tumor metabolism research.

SAICAR, an intermediate of de novo purine nucleotide biosynthesis, selectively activates pyruvate kinase isoform M2 (PKM2) with an EC50 of 0.3 mM.

PKM2-IN-8 (Compound 9b) is an inhibitor of pyruvate kinase M2 (PKM2) with an IC50 of 0.31 μM. It exhibits potent antiproliferative activity against U87MG glioma cells. PKM2-IN-8 induces early apoptosis and reduces lactate levels. This compound is useful for research in glioblastoma.

ML 083 is a highly specific allosteric activator of the tumor-associated M2 isoform of human pyruvate kinase that modulates phosphoenolpyruvate binding cooperativity, and it is used as a metabolic research tool to investigate tumor-specific glycolytic regulation and cancer-associated metabolic reprogramming.

PKM2-IN-11 is a PKM2 inhibitor with an IC50 value of 0.363 μM. It operates through dual mechanisms, inhibiting pyruvate kinase M2 (PKM2) and stabilizing microtubules. This compound reduces PKM2 protein levels in MCF-7 cells, slightly decreases reactive oxygen species (ROS) levels, and significantly increases early apoptosis in cells. Additionally, PKM2-IN-11 induces G2/M phase arrest and is applicable in breast cancer research.

LIQ1 is a flavonoid derivative and a potent allosteric inhibitor of pyruvate kinase M2 (PKM2) with an IC50 of 0.39 μM and a Kd of 4.5 μM, targeting the Arg43 in the poly-arginine pocket. It demonstrates efficacy in an LPS-induced mouse endotoxemia model by preventing PKM2 nuclear translocation and inhibiting its interaction with HIF-1α, thus suppressing IL-1β transcription. LIQ1 is applicable in endotoxemia research.

PKM2-IN-13 is a selective inhibitor of PKM2 with an IC50 value of 55.13 μM. This compound demonstrates broad-spectrum anticancer activity while exhibiting low toxicity to normal cells. PKM2-IN-13 induces apoptosis by elevating reactive oxygen species (ROS) levels and activating Caspase-3/7. It interacts with pyruvate kinase M2 in vitro, inhibiting its glycolytic function. Additionally, PKM2-IN-13 has shown a good safety profile, with no significant adverse effects observed in in vivo experiments. It can be utilized in research studies involving oral squamous cell carcinoma, colon cancer, breast cancer, and melanoma.

Multi-target kinase-IN-9 is a multi-target enzyme inhibitor with antiproliferative and antiangiogenic activity, showing significant selectivity for liver cancer cells. By extensively binding to active sites or ATP-binding regions of several key enzymes, such as DNA polymerase β and pyruvate kinase M2 (PKM2), it disrupts DNA repair and replication, glycolysis, chromatin dynamics, and transcriptional programs, blocking cancer stem cell self-renewal. This compound induces genomic instability, lysosomal dysfunction, and autophagic flux interruption, leading to tumor cell death. It effectively inhibits tumor proliferation, invasion, metastasis, and angiogenesis, significantly reducing tumor volume in xenograft models. Multi-target kinase-IN-9 is applicable in liver cancer research.

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].

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.

ZINC08383544 is a specific pyruvate kinase M2 activator which promotes the formation of PKM2 tetramer. ZINC08383544 effectively blocks PKM2 nuclear translocation, and inhibits the growth of tumor.

TLN-232, also known as CAP-232, is a synthetic cyclic heptapeptide with potential antineoplastic activity. Pyruvate kinase (PK) inhibitor TLN-232 targets pyruvate kinase M2 (M2PK), which may disrupt tumor cell anaerobic glycolysis. M2PK is a dimeric isoform of PK and the predominant PK isoform found in tumor cells.

PF-06284674 is a cell permeable, potent and selective M2 isoform of pyruvate kinase (PKM2) activator.

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.

ML202 is a highly specific allosteric activator of human pyruvate kinase M2 (hPK-M2), enhancing the cooperativity of phosphoenolpyruvate (PEP) binding with negligible effect on adenosine diphosphate (ADP) binding.

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).

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.

DL-Serine (Standard) is the standard substance of DL-Serine, and it is applicable for quantitative analysis, quality control, and related research in biochemical experiments. DL-Serine is a non-essential amino acid and a natural ligand and allosteric activator of pyruvate kinase M2.