1799753-84-6 Usage
Description
BAY-876 is a potent, highly selective, cell-permeable inhibitor of glucose transporter GLUT1. It has an IC50 value of 2 nM in vitro and inhibits glucose uptake by Hela-MaTu cells with an IC50 value of 3.2 nM. BAY-876 is at least 130-fold selective for GLUT1 relative to GLUT2, GLUT3, GLUT4, and a panel of 18 kinases and 68 proteins.
Uses
Used in Pharmaceutical Industry:
BAY-876 is used as a potent and selective inhibitor of glucose transporter 1 (Glut1) for targeting cancer cells that rely on increased glucose uptake for their energy needs. Its high selectivity and cell permeability make it a promising candidate for the development of anti-cancer therapies.
Used in Drug Development:
BAY-876 is used as a research tool in drug development to study the role of glucose transporters in various diseases, particularly cancer. Its high selectivity and potency allow researchers to investigate the effects of inhibiting GLUT1 on cellular processes and the potential for therapeutic intervention.
Used in Metabolic Research:
BAY-876 is used as a research compound in metabolic studies to understand the role of glucose transporters in glucose uptake and metabolism. Its ability to selectively inhibit GLUT1 provides insights into the regulation of glucose transport and its implications in metabolic disorders.
Used in Preclinical Models:
BAY-876 is used in preclinical models to evaluate its efficacy and safety as a potential anti-cancer agent. Its low metabolic clearance, high permeability, low plasma clearance, and high oral bioavailability in rats and dogs make it a suitable candidate for further investigation in animal models of cancer.
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
Check Digit Verification of cas no
The CAS Registry Mumber 1799753-84-6 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,7,9,9,7,5 and 3 respectively; the second part has 2 digits, 8 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 1799753-84:
(9*1)+(8*7)+(7*9)+(6*9)+(5*7)+(4*5)+(3*3)+(2*8)+(1*4)=266
266 % 10 = 6
So 1799753-84-6 is a valid CAS Registry Number.
1799753-84-6Relevant articles and documents
Identification and Optimization of the First Highly Selective GLUT1 Inhibitor BAY-876
Siebeneicher, Holger,Cleve, Arwed,Rehwinkel, Hartmut,Neuhaus, Roland,Heisler, Iring,Müller, Thomas,Bauser, Marcus,Buchmann, Bernd
, p. 2261 - 2271 (2016/10/24)
Despite the long-known fact that the facilitative glucose transporter GLUT1 is one of the key players safeguarding the increase in glucose consumption of many tumor entities even under conditions of normal oxygen supply (known as the Warburg effect), only
