1. Metabolic Enzyme/Protease
  2. Glutaminase
  3. BPTES

BPTES is an allosteric and selective glutaminase inhibitor with an IC50 of 0.16 μM.

Para uso exclusivo en investigación. No vendemos a pacientes.

No. CAS : 314045-39-1

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10 mM * 1 mL in DMSO
ready for reconstitution
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Revisión del cliente

Based on 61 publication(s) in Google Scholar

Other Forms of BPTES:

Top Publications Citing Use of Products

61 Publications Citing Use of MCE BPTES

2D/3D Cell Culture and Differentiation
WB
Flow Cytometry

    BPTES purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 May 15;16(1):4502.  [Abstract]

    BPTES (3 μM, 3 days) had no effect on ACLY expression and H3K27 and H3K9 acetylation in patient CD4+ T cells.

    BPTES purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 May 15;16(1):4502.  [Abstract]

    BPTES (3 μM, 48 h) did not reverse the increase in IFNγ, T-bet, IL-17A, and RORγt expression in Tigit−/− CD4+ T cells cultured under Th1- or Th17-polarizing conditions.

    BPTES purchased from MedChemExpress. Usage Cited in: Mater Today Bio. 2025 Feb 25:31:101608.

    BPTES (0-160μM, 24 h (left) and 48 h (right)) combined with RT (4Gy) inhibited cell growth in HepG2 cells.

    BPTES purchased from MedChemExpress. Usage Cited in: Cell Metab. 2022 Nov 1;34(11):1843-1859.e11.  [Abstract]

    BPTES treatment (3 μM, 55 min) reduced the maximal and spare respiratory capacity of Kcnj2f/f tumor-associated macrophages.

    BPTES purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2020 Aug;85:106664.  [Abstract]

    BPTES/CB839 could efficiently and specifically inhibit the NLRP1b inflammsome signaling pathway in J774A.1 cells. The cell lysate is analyzed by immunoblotting using anti-Caspase-1 and anti-GAPDH antibodies.
    • Actividad biológica

    • Protocolo

    • Pureza y Documentación

    • Referencias

    • Revisión del cliente

    Descripciòn

    BPTES is an allosteric and selective glutaminase inhibitor with an IC50 of 0.16 μM.

    IC50 & Target

    Glutaminase[1]

    Cellular Effect
    Cell Line Type Value Description References
    A549 IC50
    0.42 μM
    Compound: BPTES
    Antiproliferative activity against human A549 cells after 5 days by EZMTT reagent-based assay
    Antiproliferative activity against human A549 cells after 5 days by EZMTT reagent-based assay
    [PMID: 30543285]
    A549 IC50
    276 nM
    Compound: 2, BPTES
    Antiproliferative activity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by celltiter-fluor assay
    Antiproliferative activity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by celltiter-fluor assay
    [PMID: 33118821]
    A549 IC50
    49 μM
    Compound: BPTES
    Antiproliferative activity against human A549 cells assessed as reduction in cell viability
    Antiproliferative activity against human A549 cells assessed as reduction in cell viability
    [PMID: 36055003]
    ASPC1 IC50
    10.2 μM
    Compound: BPTES
    Growth inhibition of human Aspc-1 cells after 72 hrs by MTS assay
    Growth inhibition of human Aspc-1 cells after 72 hrs by MTS assay
    [PMID: 28609101]
    CAKI-1 IC50
    1.16 μM
    Compound: BPTES
    Antiproliferative activity against human Caki1 cells after 5 days by EZMTT reagent-based assay
    Antiproliferative activity against human Caki1 cells after 5 days by EZMTT reagent-based assay
    [PMID: 30543285]
    H22 IC50
    > 10 μM
    Compound: BPTES
    Antiproliferative activity against mouse H22 cells after 5 days by EZMTT reagent-based assay
    Antiproliferative activity against mouse H22 cells after 5 days by EZMTT reagent-based assay
    [PMID: 30543285]
    HCC827 IC50
    42.4 μM
    Compound: BPTES
    Cytotoxicity against human erlotinib-resistant HCC827 cells assessed as growth inhibition after 48 hrs by CCK8 assay
    Cytotoxicity against human erlotinib-resistant HCC827 cells assessed as growth inhibition after 48 hrs by CCK8 assay
    [PMID: 28174105]
    HCT-116 IC50
    0.54 μM
    Compound: BPTES
    Antiproliferative activity against human HCT116 cells after 5 days by EZMTT reagent-based assay
    Antiproliferative activity against human HCT116 cells after 5 days by EZMTT reagent-based assay
    [PMID: 30543285]
    HCT-116 IC50
    1.02 μM
    Compound: BPTES
    Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31603674]
    HCT-116 IC50
    3.91 μM
    Compound: BPTES; I-3
    Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 33792311]
    HCT-116 IC50
    44 μM
    Compound: BPTES
    Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability
    Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability
    [PMID: 36055003]
    HT-1080 IC50
    47.72 μM
    Compound: BPTES
    Cytotoxicity against human HT1080 cells assessed as growth inhibition after 48 hrs by CCK8 assay
    Cytotoxicity against human HT1080 cells assessed as growth inhibition after 48 hrs by CCK8 assay
    [PMID: 28174105]
    MDA-MB-231 IC50
    2610 nM
    Compound: BPTES
    Cytotoxicity against human MDA-MB-231 cells measured on 6th day by hemocytometry
    Cytotoxicity against human MDA-MB-231 cells measured on 6th day by hemocytometry
    [PMID: 26988803]
    MDA-MB-231 IC50
    6.8 μM
    Compound: BPTES
    Growth inhibition of human MDA-MB-231 cells after 72 hrs by MTS assay
    Growth inhibition of human MDA-MB-231 cells after 72 hrs by MTS assay
    [PMID: 28609101]
    MDA-MB-231 IC50
    9.08 μM
    Compound: BPTES
    Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay
    [PMID: 33176943]
    MDA-MB-436 IC50
    2.4 μM
    Compound: BPTES
    Antiproliferative activity against human MDA-MB-436 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-436 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31603674]
    MDA-MB-436 IC50
    5.08 μM
    Compound: BPTES; I-3
    Antiproliferative activity against human MDA-MB-436 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-436 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 33792311]
    NCI-H1703 GI50
    1.3 μM
    Compound: 3; BPTES
    Antiproliferative activity against human NCI-H1703 cells assessed as reduction in cell growth after 5 days by SYTOX green staining-based assay
    Antiproliferative activity against human NCI-H1703 cells assessed as reduction in cell growth after 5 days by SYTOX green staining-based assay
    [PMID: 31199640]
    SW1990 IC50
    35.33 μM
    Compound: 1; BPTES
    Antiproliferative activity against human SW1990 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 assay
    Antiproliferative activity against human SW1990 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 assay
    [PMID: 36996714]
    In Vitro

    BPTES (10 μM) exhibits inhibition of PDAC cell proliferation[1]. BPTES preferentially slows growth of mutant IDH1 cells without inducing apoptosis. BPTES (10 μM) reduces glutaminase activity in both WT and mutant IDH1 expressing cells, diminishes glutamate and α-KG levels, and increases glycolytic intermediates while leaving total 2-HG levels unaffected[2]. BPTES (10 μM) shows a clear synergistic anti-cancer effect with 10 μM of 5-FU in A549 and EKVX cell lines, and results in a growth reduction response not only in EKVX and A549 but also in most of the NSCLC cell lines[3]. BPTES (10 μM) effectively reduces the levels of the metabolites of the TCA cycle, with no changes in the levels of metabolites in glycolysis and the pentose phosphate pathway. BPTES treatment reduces about 30% ATP production under normoxia, and an additional 10% reduction of ATP production is observed under hypoxia in EKVX[4].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Peso molecular

    524.68

    Fòrmula

    C24H24N6O2S3

    No. CAS
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(NC1=NN=C(CCSCCC2=NN=C(NC(CC3=CC=CC=C3)=O)S2)S1)CC4=CC=CC=C4

    Envío

    Room temperature in continental US; may vary elsewhere.

    Almacenamiento
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvente y solubilidad
    In Vitro: 

    DMSO : 25 mg/mL (47.65 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9059 mL 9.5296 mL 19.0592 mL
    5 mM 0.3812 mL 1.9059 mL 3.8118 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Calculadora de molaridad

    • Calculadora de dilución

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: 2.5 mg/mL (4.76 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.08 mg/mL (3.96 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Pureza y Documentación

    Purity: 98.75%

    Referencias
    Ensayo celular
    [2]

    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, and 4 mM glutamine). 48 hours after plating, compounds or DMSO are added. Media and alamarBlue is added to a volume of 200 µL in each well. Fluorescence is measured at 48 hrs or 72 hrs (EGCG) using a Victor3 plate-reader.

    MCE no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.

    Administraciòn de animales
    [1]

    Four-week-old female Foxn1nuathymic nude mice are used for the assay. Freshly resected pancreatic tumor samples obtained from patients at the time of surgery are propagated from mouse to mouse as a live tumor bank. Once a tumor volume of 50 mm3 is reached (4 wk postimplantation), mice are treated with 12.5 mg/kg BPTES by intraperitoneal injection, 200 mg/kg CB-839 twice per d by oral gavage, 54 mg/kg BPTES-NPs (1.2 mg BPTES in 100 µL nanoparticles per mouse) by intravenous injection, blank-NPs (100 µL per mouse) by intravenous injection, 25 mg/kg LY 188011 intraperitoneally, or a combination of BPTES-NPs with LY 188011. BPTES-NPs are injected once every 3 d for a total of six injections over 16 d.

    MCE no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.

    Referencias

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9059 mL 9.5296 mL 19.0592 mL 47.6481 mL
    5 mM 0.3812 mL 1.9059 mL 3.8118 mL 9.5296 mL
    10 mM 0.1906 mL 0.9530 mL 1.9059 mL 4.7648 mL
    15 mM 0.1271 mL 0.6353 mL 1.2706 mL 3.1765 mL
    20 mM 0.0953 mL 0.4765 mL 0.9530 mL 2.3824 mL
    25 mM 0.0762 mL 0.3812 mL 0.7624 mL 1.9059 mL
    30 mM 0.0635 mL 0.3177 mL 0.6353 mL 1.5883 mL
    40 mM 0.0476 mL 0.2382 mL 0.4765 mL 1.1912 mL
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    Inquiry Information

    Nombre del producto:
    BPTES
    Cat. No.:
    HY-12683
    Cantidad:
    MCE Japan Authorized Agent: