WZB117

Glucose transporter GLUT inhibitor (GLUT4 > GLUT1 = GLUT3). Fast-acting irreversible GLUT1 inhibitor. Binds directly to GLUT1 involving three hydrogen bonds, one each with Asn34, Arg126 and Trp412. Blocks glucose transport in diverse cancer cells, reducing extracellular lactate and intracellular ATP levels and consequently decreases glycolysis. Anticancer agent in vitro and in vivo. Inhibits cancer cell proliferation, resulting in cell cycle arrest, senescence and necrosis or apoptosis. Inhibits the self-renewal and tumor-initiating capacity of cancer stem cells, blocking tumor initiation after implantation of cancer stem cells in mice.