GLUT3 Inhibitor

BAY-876, a chemical probe, is an orally active and selective glucose transporter 1 (GLUT1) inhibitor with an IC₅₀ of 2 nM. BAY-876 is >130-fold more selective for GLUT1 than GLUT2, GLUT3, and GLUT4. BAY-876 is also a potent blocker of glycolytic metabolism and ovarian cancer growth. In addition, BAY-876 can induce the formation of disulfide bonds in actin cytoskeletal proteins, leading to the occurrence of cellular disulfidptosis.

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. In addition, KL-11743 can induce the formation of disulfide bonds in actin cytoskeletal proteins, leading to the occurrence of cellular disulfidptosis.

GLUT inhibitor-1 is a potent and orally active inhibitor of glucose transporters, targeting both GLUT1 and GLUT3, with IC₅₀s of 242 nM and 179 nM, respectively. GLUT inhibitor-1 has the potential for the reaesrch of cancers and autoimmune diseases.

NV-5440 (Compound I-120) is an mTORC1 inhibitor and glucose transporter inhibitor. NV-5440 targets GLUT-1, -2, -3, and -4, and shows no activity against GLUT-5. NV-5440 inhibits glucose uptake.

(Rac)-Glutipyran is a broad-spectrum GLUT inhibitor that targets both GLUT1 and GLUT3. (Rac)-Glutipyran inhibits glucose uptake and suppresses the growth of multiple cancer cells, significantly inhibiting PANC-1 cell growth (IC₅₀=1.8 μM) and glucose uptake (IC₅₀=0.13 μM).