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Fasentin is a small molecule inhibitor of glucose uptake, acting primarily through inhibition of the glucose transporters GLUT1 and GLUT4 (IC50 = 68 μM), with preferential inhibition of GLUT4 over GLUT1. It sensitizes cells to FAS-induced cell death by modulating the extrinsic apoptotic pathway downstream of TNF receptors but upstream of effector caspases. Fasentin has been shown to block glucose uptake in cancer cell lines, exhibit anti-angiogenic activity, and rescue cardiac progenitor cell dysfunction induced by high glucose. Its effects on endothelial cells include inhibition of tube formation, proliferation, and invasion, though these effects may be independent from its modulation of glucose metabolism[1][5][6].
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