Description
BAY-876 is a potent, highly selective, cell-permeable inhibitor of glucose transporter GLUT1. It had an IC50 value of 2 nM in vitro and inhibited glucose uptake by Hela-MaTu cells with an IC50 value of 3.2 nM. BAY-876 was at least 130-fold selective for GLUT1 relative to GLUT2, GLUT3, GLUT4 and a panel of 18 kinases and 68 proteins.BAY-588 is used as a negative control and is available from Sigma.
Uses
BAY-876 is a potent and selective inhibitor of glucose transporter 1 (Glut1) with IC50 values of 2, 10,800, 1,670, and 290 nM for Glut1, Glut2, Glut3, and Glut4, respectively, in CHO cells expressing human recombinant receptors.1 It shows low metabolic clearance and has high permeability in vitro. In vivo, BAY-876 displays low plasma clearance and high oral bioavailability in rats and dogs.
Biological Activity
Potent and selective GLUT1 inhibitor (IC50 = 2 nM). Displays selectivity for GLUT1 over GLUT2/3/4 (IC50 values are 10.8, 1.67 and 0.29 μM, respectively). Induces cell death in hypoxic conditions in vitro. Inhibits glucose uptake by Hela-MaTu cells. Cell permeable and orally bioavailable.
Biochem/physiol Actions
BAY-876 is a potent, highly selective, cell-permeable inhibitor of glucose transporter GLUT1. It had an IC50 value of 2 nM in vitro and inhibited glucose uptake by Hela-MaTu cells with an IC50 value of 3.2 nM. BAY-876 was at least 130-fold selective for GLUT1 relative to GLUT2, GLUT3, GLUT4 and a panel of 18 kinases and 68 proteins. For full characterization details, please visit the BAY-876 probe summary on the Structural Genomics Consortium (SGC) website.BAY-588 is the negative control for the active probe, BAY-876. BAY-588 is available from Sigma. To learn more about and purchase BAY-588, click here.To learn about other SGC chemical probes for protein targets, visit sigma.com/sgc
