GLPBio

BPTES

Catalog No.: GC13958Purity:>98.00%
COASDSData Sheet
BPTES is a potent and selective allosteric inhibitor of kidney-type glutaminase (GLS) that has served as a molecular probe to determine the therapeutic potential of GLS inhibition.

Products are for research use only. Not for human use. We do not sell to patients.

BPTES
Cas No.: 314045-39-1
10mM (in 1mL DMSO)In Stock
$58.00
1
1mgIn Stock
$20.00
1
5mgIn Stock
$50.00
1
10mgIn Stock
$67.00
1
25mgIn Stock
$110.00
1
50mgIn Stock
$171.00
1
100mgIn Stock
$255.00
1
200mgIn Stock
$370.00
1
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Description

BPTES is a potent and selective allosteric inhibitor of kidney-type glutaminase (GLS) that has served as a molecular probe to determine the therapeutic potential of GLS inhibition[1].

In vitro, BPTES (2, 5 and 10μM) could effectively and specifically suppress NLRP1b inflammasome activation in macrophages[2]. BPTES (10μM; 6h) pretreatments increased the toxic effects of cisplatin and etoposide on HCC1937 and BT-549 cells[3]. BPTES (0, 0.05, 0.5, 1, 2.5 and 5μM; 72h) selectively eliminates human skin senescent fibroblasts[4]. BPTES (10μM; 24h) reduces Extracellular vesicle (EV) release in HIV-1-infected macrophages and immune-activated microglia[5].

In vivo, BPTES (1mg/kg; 1h; i.p.) can block the anthrax lethal toxin-induced mortality and tissue injury in mice by preventing injury to lungs, adrenal glands and intestine[2]. BPTES (0.25mg/20g/200μL; 2-3 times a week for 1 month; i.p.) can eliminate SA-β-Gal-positive cells in a human skin graft chimera model in mice[4].

References:
[1] Shukla K, Ferraris DV, Thomas AG, et al. 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. 2012 Dec 13;55(23):10551-63.
[2] Wang J, Yang D, Shen X, et al. BPTES inhibits anthrax lethal toxin-induced inflammatory response. Int Immunopharmacol. 2020 Aug;85:106664.
[3] Chen L, Cui H, Fang J, et al. Glutamine deprivation plus BPTES alters etoposide- and cisplatin-induced apoptosis in triple negative breast cancer cells. Oncotarget. 2016 Aug 23;7(34):54691-54701.
[4] Takaya K, Ishii T, Asou T, et al. Glutaminase inhibitors rejuvenate human skin via clearance of senescent cells: a study using a mouse/human chimeric model. Aging (Albany NY). 2022 Nov 21;14(22):8914-8926.
[5] Wu B, Liu J, Zhao R, et al. Glutaminase 1 regulates the release of extracellular vesicles during neuroinflammation through key metabolic intermediate alpha-ketoglutarate. J Neuroinflammation. 2018 Mar 14;15(1):79.

Protocol

Cell experiment [1]:

Cell lines

HCC1937 and BT-549 cells

Preparation Method

HCC1937 and BT-549 cells were pretreated with 10μM BPTES for 6h and then treated with 5μM etoposide or cisplatin for 48h. The expressions of cleaved-PARP, cleaved-caspase 3, cleaved-caspase 9, Bcl-2, and BAX in HCC1937 and BT-549 cells were measured by immunoblotting. Cell apoptosis was measured by flow cytometry in BT-549 and HCC1937 cells.

Reaction Conditions

10μM; 6h

Applications

BPTES pretreatments increased the toxic effects of cisplatin and etoposide on HCC1937 and BT-549 cells.
Animal experiment [2]:

Animal models

4-week-old female Balb/c mice

Preparation Method

Four-week-old female Balb/c mice were pretreated with vehicle or 1mg/kg BPTES via intraperitoneal injection for 1h, and then subjected to intravenous injection of 500mg/kg lethal factor (LF) and protective antigen (PA). Mouse survival was measured up to 150h.
The lungs were removed from mice that had undergone the respective treatments, and the wet-to-dry weight ratio of the lungs was calculated by dividing the wet weight by the dry weight. Pleural effusions from mice that had undergone the respective treatments were drained and quantified from the thoracic cavities.

Tissue sections of the lungs, adrenal glands and intestines were stained with hematoxylin and eosin (H&E).

Dosage form

1mg/kg; 1h; i.p.

Applications

BPTES can block the anthrax lethal toxin-induced mortality and tissue injury in mice by preventing injury to lungs, adrenal glands and intestine.

References:
[1] Chen L, Cui H, Fang J, et al. Glutamine deprivation plus BPTES alters etoposide- and cisplatin-induced apoptosis in triple negative breast cancer cells. Oncotarget. 2016 Aug 23;7(34):54691-54701.
[2] Wang J, Yang D, Shen X, et al. BPTES inhibits anthrax lethal toxin-induced inflammatory response. Int Immunopharmacol. 2020 Aug;85:106664.

Product Documents

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
314045-39-1
Chemical Name
(1Z,1'Z)-N',N''-(5,5'-(thiobis(ethane-2,1-diyl))bis(1,3,4-thiadiazole-5,2-diyl))bis(2-phenylacetimidic acid)
SMILES
O/C(CC1=CC=CC=C1)=N\C2=NN=C(S2)CCSCCC(S3)=NN=C3/N=C(O)/CC4=CC=CC=C4
Molecular Formula
C24H24N6O2S3
Molecular Weight
524.68
Solubility
≥ 18 mg/mL in DMSO
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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