BAY-876 is the first highly selective GLUT1 inhibitor with IC50 of 0.002 uM. show good metabolic stability in vitro and high oral bioavailability in vivo.

STF-31 is an inhibitor of GLUT1 (IC50 = ~1 µM) that blocks glucose uptake.

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.

Glucopiericidin A is a natural piericidin compound obtained from a marine-derived Streptomyces strain. Glucopiericidin A serves as a glucose transporter (GLUT) chemical probe and suppresses glycolysis. Glucopiericidin A inhibits ATP-dependent filopodia protrusion with Piericidin A and has no effect alone. Glucopiericidin A induces cell apoptosis through reducing the reactive oxygen species (ROS) level by increasing PRDX1 and exhibits potent antitumor efficacy in ACHN mice xenografts.

4,6-O-ethylidene-α-D-glucose (Ethylidene-glucose), a glucose derivative, is a competitive exofacial binding-site inhibitor on glucose transporter 1 (GLUT1) with a Ki of 12 mM for wild-type 2-deoxy-D-glucose transport.

SW157765 is a selective non-canonical glucose transporter GLUT8 (SLC2A8) inhibitor. KRAS/KEAP1 double mutant NSCLC cells are selectively sensitive to the SW157765, due to the convergent consequences of dual KRAS and NRF2 modulation of metabolic and xenobiotic gene regulatory programs.

KL-11743 is a potent, orally active, and glucose-competitive inhibitor of the class I glucose transporters, with IC50s of 115, 137, 90, and 68 nM for GLUT1, GLUT2, GLUT3, and GLUT4, respectively. KL-11743 specifically blocks glucose metabolism. KL-11743 can synergize with electron transport inhibitors to induce cell death.

DRB18 (DRB-18) is a potent, pan-class I glucose transporter (GLUT) inhibitor, reduces glucose uptake in HEK293 cell lines expressd single GLUT1-4 with IC50 of 0.9-8.8 uM.DRB18 reduced cell viability in a dose-dependent manner in cancer cell lines (A549 IC50=3.5 uM, HeLa IC50=1.3 uM), also exhibited IC50 values < 10 μM in all nine melanoma cell lines.DRB18 rapidly and potently inhibited glucose transport and glucose metabolism, inhibited multiple metabolic pathways associated with glucose metabolism in A549 cells.DRB18 caused G1/S phase arrest and increased oxidative stress in A549 cells.DRB18 (10mg/kg) inhibited the growth of A549 tumors xenografted in nude mice.

Glutor (Glucose uptake inhibitor Glutor) is a novel highly potent glucose uptake inhibitor (IC50=10.8 nM) that selectively targets glucose transporters GLUT-1, -2, and -3.Glutor reduced the uptake of 2-DG with similar potency in different cancer cell lines such as HCT116 (IC50 =10.8 nM), UM-UC-3 (IC50=8.3 nM), UO31 (IC50=3.6 nM), and MIA PaCa-2 (IC50=1.1 nM).Glutor did not interfere with cellular hexokinase activity and potently reduced glycolytic flux in HCT116 cells.Glutor induced upregulation of GLUT-1 and -3 in cancer cells, inhibited glycolysis and efficiently suppresseed the growth of various cancer cell lines.Glutor potently and synergistically inhibited colon cancer cell growth combined with glutaminase inhibitor CB-839.

Glutipyran is a small-molecule glucose transporter inhibitor, inhibits glycolytic activity and cell growth in human pancreatic cancer cells.