pkm 2

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.

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.

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-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.

PKM2-IN-12 is an orally active PKM2 inhibitor with an IC50 of 10 nM. It effectively hinders the proliferation and migration of COLO-205 cells, induces cell cycle arrest, and triggers apoptosis (apoptosis). PKM2-IN-12 significantly reduces lactate, pyruvate, and ROS levels in cells. In mouse models, it not only directly targets cancer cells but also restores disrupted intestinal microecological balance. PKM2-IN-12 is useful for colorectal cancer 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.

PKM2 activator 11 (Compound 23) is a PKM2 activator with an AC50 value of 92.12 nM. It promotes the tetramerization of PKM2 and inhibits its nuclear translocation. Additionally, PKM2 activator 11 suppresses glycolysis and the PKM2/STAT3 signaling pathway, induces apoptosis (Apoptosis), and demonstrates potent and selective anticancer activity against colorectal cancer in vitro.

PKM2 agonist-1 (Compound D16) is a potent allosteric activator of PKM2, with an AC50 value of 77 nM. It inhibits angiotensin II-induced smooth muscle cell phenotypic transformation, effectively preventing aortic dissection and reducing mortality.

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 inhibitor G is a inhibitor of pyruvate kinase.

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).

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

(+)-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.