Glutaminase GLS1 inhibitor / Potent and selective allosteric1 inhibitor of kidney-type glutaminase (GLS1), IC50 = 3.3 µM2. Selective for GLS1 over GLS2, g-glutamyl transpeptidase and glutamate dehydrogenase. Shuts down an alternative energy-generating glutaminolysis pathway in P493 cells under both glucose deprivation or hypoxia.3 Reduces the growth of P493 cell xenografts by 50% over a 10 day treatment.4 BPTES inhibition of glutamine utilization in cancer cells increases PD-L1 expression.5 Clears senescent cells and improves various age-related disorders in a geriatric mouse model.6
Biochemicals & reagents
314045-39-1
DeLaBarre et al. (2011), Full-length human glutaminase in complex with an allosteric inhibitor; Biochemistry 50 10764 Shukla et al. (2012), Design, synthesis, and pharmacological evaluation of bis-2-(5-phenylacetamido-1,2,4-thiadiazol-2-yl)ethyl sulfide 3 (BPTES) analogs as glutaminase inhibitors; J. Med. Chem., 55 10551 Le et al. (2012), Glucose-independent glutamine metabolism via TCA cycling for proliferation and survival in B cells; Cell Metab. 15 110 Xiang et al. (2015), Targeted inhibition of tumor-specific glutaminase diminishes cell-autonomous tumorigenesis; J. Clin. Invest. 125 2293 Byun et al. (2020), Inhibition of Glutamine Utilization Synergizes with Immune Checkpoint Inhibitor to Promote Antitumor Immunity; Mol. Cell 80 592 Pan and Locasale (2021), Targeting metabolism to influence aging; Science 371 234
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TARGET: Glutaminase; Energy production -- PATHWAY: Amino acid metabolism; Proliferation; Warburg effect; NFkappaB; Cell cycle; Senescence -- RESEARCH AREA: Cell death -- DISEASE AREA: Cancer; Ageing