pkm-2

Mitapivat (PKR-IN-1), also known as PKM2 activator 1020 is a PKM2 activator (pyruvate kinase activator) for the treatment of pyruvate kinase deficiency.

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.

(+)-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.

Cynaroside (Luteolin 7-O-Glucoside) is a flavone, a flavonoid-like chemical compound. It has an anti-oxidant effect, inhibiting lipid and protein oxidation.

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.

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.

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

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.

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.

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.

PKM2-IN-9 (compound C1) is a potent inhibitor of PKM2, demonstrating a 75% inhibition rate at 50 μM. It plays a significant role in cancer research.

PKM2 modulator 2 (compound C599) is a potent inhibitor of PKM2, displaying antiproliferative activity and inducing apoptosis. This compound holds potential for research in glioblastoma.

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

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.

PKM2 activator 7 (Compd B4) is a PKM2 activator with an AC50 value of 0.144 μM. It functions by inhibiting the growth of T cells, thereby alleviating DSS-induced colitis in mice.

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.)

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.

PKM2/PDK1-IN-1, a shikonin thioether derivative, serves as a dual inhibitor for PKM2/PDK1. This compound effectively inhibits the proliferation and induces apoptosis in NSCLC cells. It promotes intercellular ROS production and modulates apoptotic proteins, engaging in both mitochondrial and death receptor pathways [1].

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].

Compound Z10 (PKM2 activator 6) serves as both a PKM2 activator and a PDK1 inhibitor, exhibiting dissociation constants (K D ) of 121 μM and 19.6 μM, respectively. It promotes apoptosis in colorectal cells while suppressing their proliferation and migration, additionally inhibiting glycolysis. Compound Z10 demonstrates inhibitory effects on the proliferation of various cell lines, including DLD-1, HCT-8, HT-29, and MCF-10A, with half-maximal inhibitory concentrations (IC 50 ) of 10.04 μM, 2.16 μM, 3.57 μM, and 66.39 μM, as recorded in reference [1].

PKM2-IN-6 (compound 7d) is an orally active PKM2 inhibitor (IC50=23 nM) capable of inducing apoptosis and G2 cell cycle arrest. It reduces PKM1 and PKM2 expression at the mRNA level, exhibits antitumour activity, and is suitable for investigating triple-negative breast cancer (TNBC).

PKM2 inhibitor G is a inhibitor of pyruvate kinase.