BPTES

Catalog No.S7753 Batch:S775306

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Technical Data

Formula

C24H24N6O2S3
Molecular Weight 524.68 CAS No. 314045-39-1
Solubility (25°C)* In vitro DMSO 50 mg/mL (95.29 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description BPTES is a potent and selective Glutaminase GLS1 (KGA) inhibitor with IC50 of 0.16 μM. It has no effect on glutamate dehydrogenase activity and causes only a very slight inhibition of γ-glutamyl transpeptidase activity.
Targets
Glutaminase GLS1 (KGA) [1]
0.16 μM
In vitro BPTES inhibits glutaminase activity expressed in human kidney cells with IC50 of 0.18 μM, and inhibits glutamate efflux by microglia with IC50 of 80-120 nM. [1] BPTES preferentially slows cell growth in D54 cells with mutant IDH1. BPTES also inhibits glutaminase activity, lowers glutamate and α-KG levels, and increases glycolytic intermediates. [2] BPTES (10 μM) inhibits cell growth of mHCC 3–4 cells derived from LAP/MYC tumors. BPTES also inhibits growth of a MYC-dependent P493 cells by blocking DNA replication, leading to cell death and fragmentation. [3]
In vivo In LAP/MYC mice, BPTES (12.5 mg/kg, i.p.) prolongs survival with no significant effects on MYC, GLS, or GLS2 levels. BPTES (200 μg/mouse, i.p.) also inhibits tumor cell growth in mice harboring P493 tumor xenografts. [3]

Protocol (from reference)

Kinase Assay:

[1]
  • Glutaminase Inhibition: Cell Free Assay

    Assay plates are prepared containing 2 μL test compound in DMSO/well. The enzyme is diluted to 1 unit (liver) or 0.8 unit (kidney)/100 μL in glutaminase assay buffer, and 100 μL diluted enzyme is added to each well of the assay plate by Multidrop. The contents are mixed by shaking at full speed for 1 min on TiterMix 100. The plates are preincubated at room temperature (RT) for 20 min to allow binding of test compounds to glutaminase, and 50 μL glutamine solution (7 mM in assay buffer) is added to each well by Multidrop. The contents are shaken at full speed for 30 sec on TiterMix 100, and the plates are then incubated at RT for 60 min (liver) or 90 min (kidney). To stop the reactions, 20 μL HCl (0.3 N) is added to each well by Multidrop and mixed immediately by shaking for 30 sec on TiterMix 100. For quantification, glutamate (formed by glutaminase-catalyzed hydrolysis of glutamine) is oxidized to 2-oxoglutarate by a second enzyme, glutamate dehydrogenase (GDH), with the concomitant production of the reduced form of nicotinamide adenine dinucleotide (NADH). Reduction of nitro blue tetrazolium (NBT) in the assay solution by NADH, catalyzed by phenazine methosulphate (PMS), results in the formation of a blue-purple formazan. The absorption of formazan at 540 nm is linearly proportional to the concentration of glutamate up to 200 μM. NBT/GDH reagent (50 μL) is added to each well by Multidrop and mixed by shaking for 30 sec on TiterMix 100, and the plates are incubated at RT for 20 min to allow color formation by the GDH reaction. Glutamate concentration is determined from formazan concentration as determined by reading OD540 nm on a SpectraMax 340.
Cell Assay:

[2]
  • Cell lines

    D54 cells

  • Concentrations

    --

  • Incubation Time

    48 h

  • Method

    Cell growth assays are carried out using alamarBlue. Cells are plated at a density of 500 cells/well in a 96-well black clear bottom plate. At 24 hrs, media is changed to the appropriate media (DMEM with 4.5 g/L, 1.5 g/L or 0.1 g/L glucose, 10% FBS, pencillin/streptomycin, and 4 mM glutamine with or without doxycyline. 48 hours after plating, compounds or DMSO are added. Media and alamarBlue is added to a volume of 200 礚 in each well. Fluorescence is measured at 48 hrs (AOA, BPTES) using a Victor3 plate-reader.
Animal Study:

[3]
  • Animal Models

    LAP/MYC mice

  • Dosages

    12.5 mg/kg

  • Administration

    i.p.

Customer Product Validation

Data from [Data independently produced by , , Journal of Cancer, 2018, 9(9):1582-1591]

Data from [Data independently produced by , , Onco Targets Ther, 2018, 11:3721-3729]

Selleck's BPTES has been cited by 55 publications

Dual Inhibition of CDK4/6 and XPO1 Induces Senescence With Acquired Vulnerability to CRBN-Based PROTAC Drugs [ Gastroenterology, 2024, S0016-5085(24)00062-3] PubMed: 38262581
Targeting metabolic adaptive responses induced by glucose starvation inhibits cell proliferation and enhances cell death in osimertinib-resistant non-small cell lung cancer (NSCLC) cell lines [ Biochem Pharmacol, 2024, S0006-2952(24)00144-8] PubMed: 38522556
Glutamine metabolic microenvironment drives M2 macrophage polarization to mediate trastuzumab resistance in HER2-positive gastric cancer [ Cancer Commun (Lond), 2023, 43(8):909-937] PubMed: 37434399
Dysregulated Gln-Glu-α-ketoglutarate axis impairs maternal decidualization and increases the risk of recurrent spontaneous miscarriage [ Cell Rep Med, 2023, 4(5):101026] PubMed: 37137303
IDH2 stabilizes HIF-1α-induced metabolic reprogramming and promotes chemoresistance in urothelial cancer [ EMBO J, 2023, e110620.] PubMed: 36637036
STAG2 inactivation reprograms glutamine metabolism of BRAF-mutant thyroid cancer cells [ Cell Death Dis, 2023, 14(7):454] PubMed: 37479689
STAG2 inactivation reprograms glutamine metabolism of BRAF-mutant thyroid cancer cells [ Cell Death Dis, 2023, 14(7):454] PubMed: 37479689
PASK links cellular energy metabolism with a mitotic self-renewal network to establish differentiation competence [ Elife, 2023, 12e81717] PubMed: 37052079
Perturbation of Copper Homeostasis Sensitizes Cancer Cells to Elevated Temperature [ Int J Mol Sci, 2023, 25(1)423] PubMed: 38203594
Deciphering the mechanism of PSORI-CM02 in suppressing keratinocyte proliferation through the mTOR/HK2/glycolysis axis [ Front Pharmacol, 2023, 14:1152347] PubMed: 37089953

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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