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.

PKM2:0.363 μM

PKM2-IN-11 (Compound 30o) exhibits potent antiproliferative activity against MCF-7 cells with an IC50 of 10.2 μM at concentrations ranging from 1-25 μM over 24 hours, while showing no cytotoxicity towards HEK-293 cells. At concentrations of 1-5 μM, it dose-dependently reduces the expression levels of PKM2 protein in MCF-7 cells. At 5 μM, PKM2-IN-11 enhances the microtubule polymerization rate (Vmax) and stabilizes microtubule growth. It also slightly reduces reactive oxygen species (ROS) levels and induces mitochondrial membrane potential (ΔΨm) depolarization in MCF-7 cells, which leads to a decrease in the red/green fluorescence ratio. Additionally, PKM2-IN-11 at 5 μM significantly increases the proportion of early apoptotic cells, has a lower proportion of late apoptosis, and causes a G2/M phase cell cycle arrest of 23% in MCF-7 cells.