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A potent, highly selective and oral bioavailable GLUT1 inhibitor with IC50 of 2 nM; displays >100-fold selectivity against GLUT2, GLUT3, and GLUT4; exhibits good metabolic stability in vitro and high oral bioavailability in vivo.
WZB117 (WZB-117) is a small-molecule inhibitor of glucose transporter 1 (GLUT1), inhibits glucose transport and cancer cell proliferation with IC50 of 10 uM; decreases in levels of Glut1 protein, intracellular ATP, and glycolytic enzymes in treated cancer cells, inhibits cancer growth in tumor-bearing nude mice; also inhibits the self-renewal and tumor-initiating capacity of cancer stem cells (CSCs).
STF-31 is a selective GLUT1 inhibitor that does not bind to other glucose transporters; selectively kills RCCs by specifically targeting glucose uptake through GLUT1 and exploiting the unique dependence of these cells on GLUT1 for survival; also inhibits the enzymatic activity of NAMPT in a biochemical assay in vitro.
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