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.

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

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.

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.

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

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.

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.

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.

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.

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.