BPTES | Glutaminase GLS1 inhibitor
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $55.00 | ||
| 25 mg | $220.00 |
BPTES (314045-39-1) is a 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
References/Citations:
- 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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Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
BPTES (314045-39-1) is a 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
References/Citations:
- 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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1-855-FOCUS21
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