pkm2 in 3

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 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-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.

Vitamin K5 (Synkamin), a photosensitizer and antimicrobial agent, serves as a specific PKM2 inhibitor, demonstrating IC 50 values of 28, 191, and 120 μM against PKM2, PKM1, and PKL, respectively. It induces apoptosis in colon 26 cells and is utilized in infection and cancer research. Additionally, Vitamin K5 finds application as a preservative in pharmaceuticals, foods, and beverages [1] [2] [3].

MTP, a PKM2 inhibitor, promotes apoptosis in cancer cells via caspase-3 activation while also inducing autophagy and enhancing ROS generation. Further, it inhibits JAK2 signaling, rendering it useful for the study of oral squamous cell carcinoma [1].