Glutor is a selective GLUT 1/2/3 inhibitor that can suppress glucose uptake. Glutor can inhibit glycolysis and has anti-tumor activity, inducing cell apoptosis.
Glutor reduced the uptake of 2-DG with similar efficacy in different cancer cell lines, such as HCT116 (IC50 = 10.8 nM), UM-UC-3 (IC50 = 8.3 nM), UO-31 (IC50 = 3.6 nM), and MIA PaCa-2 (IC50 = 1.1 nM)[1].Glutor effectively decreases glycolysis in HCT116 cells, thereby preventing the reduction of oxidative phosphorylation rates after glucose addition[1]. Glutor inhibits the proliferation of malignant cell lines without harming the growth of non-malignant peripheral blood mononuclear cells (PBMCs) and IMR-90 embryonic lung cells[1]. Glutor (0.5μM, 24-48h) suppresses the glucose uptake-induced upregulation of GLUT-1 and GLUT-3 expression[1]. Glutor (0.0001-1μM, 24h) inhibits the number of DL cells in a time- and dose-dependent manner, with an Glutor reduced the uptake of 2-DG with similar efficacy in different cancer cell lines, such as HCT116 (IC50 = 10.8 nM), UM-UC-3 (IC50 = 8.3 nM), UO-31 (IC50 = 3.6 nM), and MIA PaCa-2 (IC50 = 1.1 nM)[1].Glutor effectively decreases glycolysis in HCT116 cells, thereby preventing the reduction of oxidative phosphorylation rates after glucose addition[1]. Glutor inhibits the proliferation of malignant cell lines without harming the growth of non-malignant peripheral blood mononuclear cells (PBMCs) and IMR-90 embryonic lung cells[1]. Glutor (0.5 μM, 24-48 h) suppresses the glucose uptake-induced upregulation of GLUT-1 and GLUT-3 expression[1]. Glutor (0.0001-1 μM, 24 h) inhibits the number of DL cells in a time- and dose-dependent manner, with an IC50 of 0.01 μM, showing no cytotoxicity to tmocytes[2].Glutor (0.01-1 μM, 24 h) induces apoptosis in DL cells[2]. Glutor (0.01-1 μM, 24 h) links tumor inhibition to the regulation of cell survival and metabolic regulatory molecules[2].Glutor (0.01-1 μM, 2 h) increases the expression of reactive oxygen species (ROS) in DL cells[2].Glutor (0.01-1 μM, 24 h) triggers depolarization of the mitochondrial membrane, disrupting the pH homeostasis of DL cells and altering their chemical sensitivity[2]. of 0.01 μM, showing no cytotoxicity to tmocytes[2].Glutor (0.01-1 μM, 24 h) induces apoptosis in DL cells[2]. Glutor (0.01-1 μM, 24 h) links tumor inhibition to the regulation of cell survival and metabolic regulatory molecules[2]. Glutor (0.01-1 μM, 2 h) increases the expression of reactive oxygen species (ROS) in DL cells[2].Glutor (0.01-1 μM, 24 h) triggers depolarization of the mitochondrial membrane, disrupting the pH homeostasis of DL cells and altering their chemical sensitivity[2].
References:
[1]. Reckzeh ES, et al. Inhibition of Glucose Transporters and Glutaminase Synergistically Impairs Tumor Cell Growth. Cell Chem Biol. 2019;26(9):1214-1228.e25.
[2]. Mithlesh Kumar Temre， et al. Glutor, a Glucose Transporter Inhibitor, Exerts Antineoplastic Action on Tumor Cells of Tmic Origin: Implication of Modulated Metabolism, Survival, Oxidative Stress, Mitochondrial Membrane Potential, pH Homeostasis, and Chemosensitivity. Front Oncol. 2022 Jun 30:12:925666.