Table 1.

Overview of a selection of highly potent glucose uptake inhibitors.

Name	Class	Assay	Cell line	IC50 [nm]
cytochalasin B11	natural product	[14C]2DG uptake	erythrocytes	520
WZB11717b	small molecule	[3H]2DG uptake	A459	500
compound 155 19	small molecule	[3H]2DG uptake	HEK293, hGLUT‐1[a]	≈30
GLUT‐i120 GLUT‐i220	peptide analogue	ATP depletion[b]	CHO‐K1, hGLUT‐1[a] luciferase[c]	267±133 140±72
compound 3 21b	small molecule	ATP depletion[b,d]	DLD‐1	25
BAY‐87622a	small molecule	ATP depletion[b,d]	DLD‐1	2
example 31 26	small molecule	ATP depletion[d,e]	HT1080	10–100
chromopynone‐127	small molecule	2DG uptake[f]	HCT116	412
glutor29	small molecule	2DG uptake[f]	HCT116	11
glupin30	small molecule	2DG uptake[f]	MDA‐MB‐231	4
NV‐544031	small molecule	[3H]2DG uptake	MCF7	36

[a] Stable transfection. [b] Rotenone (mitochondrial complex I inhibitor). [c] Constitutive expression. [d] CellTiter‐Glo®. [e] Oligomycin (mitochondrial ATP synthase inhibitor). [f] Resazurin‐coupled.