| Identification | Back Directory | [Name]
bis-2-(5-PhenylacetMido-1,2,4-Thiadiazol-2-yl)Ethyl Sulfide | [CAS]
314045-39-1 | [Synonyms]
BPTES
CS-1542
Glutaminase Inhibitor II
Glutaminase Inhibitor II, BPTES
bis-2-(5-phenylaQtMido-1,2,4-Thiadiazol-2-yl)Ethylsulfide
bis-2-(5-PhenylacetMido-1,2,4-Thiadiazol-2-yl)Ethyl Sulfide
Bis-2-(5-phenylacetamido-1,3,4-thiadiazol-2-yl)ethyl sulfide
N,N'-[Thiobis(2,1-ethanediyl-1,3,4-thiadiazole-5,2-diyl)]bisbenzeneacetamide
Benzeneacetamide, N,N'-[thiobis(2,1-ethanediyl-1,3,4-thiadiazole-5,2-diyl)]bis- | [Molecular Formula]
C24H24N6O2S3 | [MDL Number]
MFCD01079848 | [MOL File]
314045-39-1.mol | [Molecular Weight]
524.68 |
| Chemical Properties | Back Directory | [density ]
1.420±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: soluble10mg/mL, clear | [form ]
powder | [pka]
9.13±0.50(Predicted) | [color ]
white to beige | [Stability:]
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months. |
| Hazard Information | Back Directory | [Description]
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 | [Uses]
Bis-2-(5-phenylacetamido-1,3,4-thiadiazol-2-yl)ethyl sulfide (BPTES) has been used as a glutaminase inhibitor. | [Biochem/physiol Actions]
Vaccinia virus (VACV) requires glutamine metabolism for its optimal replication. Inhibition of glutaminolysis by bis-2-(5-phenylacetamido-1,3,4-thiadiazol-2-yl)ethyl sulfide (BPTES) can be a potential method to treat poxvirus infections. | [in vivo]
BPTES-NPs (BPTES nanoparticles, 1.2 mg BPTES in 100 μL nanoparticles, i.v.) significantly attenuates tumor growth in the patient-derived pancreatic orthotopic tumor model[1]. | [storage]
Store at -20°C | [References]
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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