WZB-117

WZB-117 is a small molecule experimental drug that acts as an irreversible inhibitor of glucose transporter 1 (GLUT1), also known as SLC2A1. By binding directly to GLUT1 and blocking glucose transport across the plasma membrane, it disrupts glycolysis and energy metabolism in cancer cells. This leads to reduced intracellular ATP levels, downregulation of glycolytic enzymes and GLUT1 protein itself, activation of AMP-activated protein kinase (AMPK), cell cycle arrest (notably via cyclin E2 and phosphorylated retinoblastoma reduction), senescence, necrosis in tumor cells and red blood cells, and inhibition of cancer cell proliferation. Its effects are more pronounced under hypoxic conditions typical for tumors. Preclinical studies have shown significant anti-tumor activity in lung cancer xenograft models as well as synergistic effects with other anti-cancer agents such as cisplatin or apatinib[2][3][5][6][8]. No clinical trials or approvals are reported.

Other names

Glucose Transporter Inhibitor IV3-Fluoro-1,2-phenylene bis(3-hydroxybenzoate)GLUT Inhibitor IV