WZB117

WZB117 is an irreversible inhibitor of glucose transporter 1 (Glut1) that blocks glucose transport in diverse cancer cells (IC₅₀ = ~0.6 µM), reducing extracellular lactate and intracellular ATP levels.¹ It inhibits cancer cell proliferation (IC₅₀s = 5-10 µM), resulting in cell cycle arrest, senescence, and necrosis or apoptosis.^1,2 These effects are enhanced by the anticancer drugs cisplatin (Item No. 13119) and paclitaxel (Item No. 10461). WZB117, given intraperitoneally at 10 mg/kg, significantly reduces tumor size in mice, with only small reductions in body weight and leukocyte count.¹ WZB117 also inhibits the self-renewal and tumor-initiating capacity of cancer stem cells, blocking tumor initiation after implantation of cancer stem cells in mice.³

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1. Liu, Y., Cao, Y., Zhang, W., et al. A small-molecule inhibitor of glucose transporter 1 downregulates glycolysis, induces cell-cycle arrest, and inhibits cancer cell growth in vitro and in vivo. Mol. Cancer Ther. 11(8), 1672-1682 (2012).

2. Xintaropoulou, C., Ward, C., Wise, A., et al. A comparative analysis of inhibitors of the glycolysis pathway in breast and ovarian cancer cell line models. Oncotarget 6(28), 25677-25695 (2015).

3. Shibuya, K., Okada, M., Suzuki, S., et al. Targeting the facilitative glucose transporter GLUT1 inhibits the self-renewal and tumor-initiating capacity of cancer stem cells. Oncotarget 6(2), 651-661 (2015).