CAS 314045-39-1: bis-2-(5-Phenylacetmido-1,2,4-Thiadiazol-2-yl)Ethyl Sulfide

BPTES

BPTES

Applications BPTES-d10 is the isotope labelled analog of BPTES (B676675); a potent and selective glutaminase inhibitor. Used in the treatment of renal cell carcinomas resulting from overexpression of the MYC oncogene. References Shroff, E. et al.: PNAS. U.S.A., 112, 6539 (2015); Thomas, A. et al.: Biochem. Biophys. Res. Comm., 443, 32 (2014)

Applications BPTES is a potent and selective Glutaminase inhibitor. Used in the treatment of renal cell carcinomas resulting from overexpression of the MYC oncogene. References Shroff, E. et al.: PNAS. U.S.A., 112, 6539 (2015); Thomas, A. et al.: Biochem. Biophys. Res. Comm., 443, 32 (2014);

BPTES(IC50 of 0.16 μM) is an effective and specific GlutamiN/Ase GLS1 (KGA) inhibitor.

The Glutaminase Inhibitor II, BPTES is a glutaminase inhibitor that is used to treat cancer. It binds to the active site of glutaminase and inhibits the enzyme from catalyzing the conversion of glutamine to glutamate. This results in reduced production of ATP, which leads to cell death. The minimal toxicity of this drug has been shown in animal models using a dinucleotide phosphate-based assay. BPTES has also been shown to inhibit mitochondrial membrane potential and induce apoptosis by decreasing levels of reactive oxygen species (ROS) and increasing mitochondrial membrane potential in a model system. BPTES can also synergize with other drugs such as anticancer agents or radiation therapy, resulting in increased efficacy against tumor cells.