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3PO is an inhibitor of PFKFB3. 3PO attenuates the proliferation of several cancer cell lines with IC50s of 1.4-24 μmol/L. 3PO suppresses glucose uptake and decreases the intracellular concentration of Fru-2,6-BP, lactate, ATP, NAD+ and NADH. 3PO can be used for the research of cancer.

For research use only. We do not sell to patients.

CAS No. : 18550-98-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Customer Review

Based on 29 publication(s) in Google Scholar

Other Forms of 3PO:

Top Publications Citing Use of Products

29 Publications Citing Use of MCE 3PO

ELISA
Cell Autophagy Assay
IHC
Flow Cytometry

    3PO purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Dec;45(12):2579-2597.  [Abstract]

    BMDMs isolated from C57BL/6J mice were incubated for 12 h with 10 μmol/L 3PO or vehicle in the presence of LPS (100 ng/mL) + IFN-γ (50 ng/mL). The supernatant levels of pro-inflammatory and anti-inflammatory cytokines measured by ELISA. n = 6 per group. The results showed that 3PO significantly reduced the supernatant levels of TNF-α and IL-6.

    3PO purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Dec;45(12):2579-2597.  [Abstract]

    BMDMs isolated from C57BL/6J mice were incubated for 12 h with 10 μmol/L 3PO or vehicle in the presence of LPS (100 ng/mL) + IFN-γ (50 ng/mL). The MFI of CD80 and CD86, and CD206 detected by flow cytometry. n = 3 per group. n = 6 per group. The results showed that 3PO significantly reduced the MFI of CD86, whereas it markedly increased the MFI of CD206.

    3PO purchased from MedChemExpress. Usage Cited in: Cancer Cell Int. 2024 Jan 6;24(1):12.  [Abstract]

    RORα deletion promotes GC proliferation induced by 3PO and DHEA in vivo The expression levels of Ki-67 and PCNA were detected through immunohistochemistry stain and MOD method in subcutaneous tumor of mice. Original 200 and 400 magnification. Scale bar = 100 μm. N = 3. The RORα-KO-MFC cells treated with 3PO (25 µM; 48 h) or DHEA (250 µM) were injected into subcutaneous flank of mice until the tumor volume reached 100 to 300 mm3.

    3PO purchased from MedChemExpress. Usage Cited in: Arch Toxicol. 2022 Nov;96(11):2913-2926.  [Abstract]

    Cells were intervened with specific inhibitors Ritonavir, 3PO (24 μM), STF-31, NSC23766, AZD3965, and 3-bromopyruvic acid for 30 min, and then incubated for 2 h with CuO-NPs (20 μg/mL). The results showed that 3PO significantly inhibited the release of HETs.

    3PO purchased from MedChemExpress. Usage Cited in: J Agric Food Chem. 2021 Nov 3;69(43):12862-12869.  [Abstract]

    T-2-triggered HET formation is dependent on PFKFB3, lactate transport, and hexokinase II. Heterophils were stimulated with T-2 (80 ng/mL) for 90 min in the inhibitors 3PO (24 μM), AZD3965, and 3-Bromopyruvic (n = 5). Zymosan (1 mg/mL) was the positive control. The results showed that 3PO significantly inhibited HET formation.
    • Biological Activity

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    Description

    3PO is an inhibitor of PFKFB3. 3PO attenuates the proliferation of several cancer cell lines with IC50s of 1.4-24 μmol/L. 3PO suppresses glucose uptake and decreases the intracellular concentration of Fru-2,6-BP, lactate, ATP, NAD+ and NADH. 3PO can be used for the research of cancer[1].

    Cellular Effect
    Cell Line Type Value Description References
    Epithelial cell IC50
    1.4 μM
    Compound: 1; 3PO
    Cytotoxicity against human Epithelial cell assessed as cell growth inhibition
    Cytotoxicity against human Epithelial cell assessed as cell growth inhibition
    [PMID: 32679452]
    In Vitro

    3PO (0-33 μM; 0-36 h) inhibits Jurkat cells proliferation by influence cell cycle[1].
    3PO (10 μM/L; 0-36 h) suppresses glycolytic flux to lactate in Jurkat cells[1].
    3PO (10 μM/L; 0-36 h) inhibits cellular proliferation of transformed tumor cell lines[1].

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

    Cell Proliferation Assay[1]

    Cell Line: Jurkat cells
    Concentration: 0.3, 1, 3, 10 and 33 μM
    Incubation Time: 0, 4, 8, 16, 24 and 36 hours
    Result: Inhibited Jurkat T cells proliferation by G2-M phase cell cycle arrest.

    Cell Viability Assay[1]

    Cell Line: Jurkat cells
    Concentration: 0.3, 1, 3, 10 and 33 μM
    Incubation Time: 0, 4, 8, 16, 24 and 36 hours
    Result: Decreased lactate secretion, NADH, NAD+ and ATP in Jurkat cells.

    Cell Proliferation Assay[1]

    Cell Line: Jurkat, K562, HL-60, MDA-MB231, HL-60, HeLa, Melanoma and Lewis Lung
    Concentration: 0-20 μM
    Incubation Time: 0, 4, 8, 16, 24 and 36 hours
    Result: Inhibited solid tumor and hematologic cell lines with IC50s of 1.4-24 μM/L.
    In Vivo

    3PO (0.07 mg/g; i.p. once per day for 14 days) inhibits the growth of Lewis lung carcinoma xenografts in C57Bl/6 mice[1].
    3PO (0.07 mg/g; i.p. three sequential daily injections followed by 3 off days for 14 days) inhibits the tumor growth in BALB/c athymic mice[1].
    3PO (0.07 mg/g; i.p. two daily injections followed a 7-day rest for 14 days) inhibits the tumor growth in BALB/c athymic mice[1].
    3PO (0.07 mg/g; i.p. once) inhibits Fru-2,6-BP and glucose uptake in C57Bl/6 mice[1].

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

    Animal Model: Female C57Bl/6 mice with Lewis lung carcinoma xenografts[1]
    Dosage: 0.07 mg/g
    Administration: Intraperitoneal injection; 0.07 mg/g once a day; for 14 days
    Result: Suppressed the growth of Lewis lung carcinoma xenografts in C57Bl/6 mice compared to the control group.
    Animal Model: Female BALB/c athymic mice with MDA-MB231 human breast adenocarcinoma xenografts[1]
    Dosage: 0.07 mg/g
    Administration: Intraperitoneal injection; 0.07 mg/g three sequential daily injections of either DMSO or 3PO followed by 3 off days; for 14 days
    Result: Suppressed xenograft tumorigenic growth of MDA-MB231 cells compared with the controls.
    Animal Model: Female BALB/c athymic mice with HL-60 leukemia xenografts[1]
    Dosage: 0.07 mg/g
    Administration: Intraperitoneal injection; 0.07 mg/g two daily injections followed a 7-day rest; for 14 days
    Result: Suppressed xenograft tumorigenic growth of HL-60 leukemia compared with the controls, especially from the second administration cycle.
    Animal Model: Female C57Bl/6 mice with Lewis lung carcinoma xenografts[1]
    Dosage: 0.07 mg/g
    Administration: Intraperitoneal injection; once
    Result: Decreased Fru-2,6-BP and glucose uptake in C57Bl/6 mice compared to control group.
    Molecular Weight

    210.23

    Formula

    C13H10N2O

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C(C1=CC=NC=C1)/C=C/C2=CC=CN=C2

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 60 mg/mL (285.40 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 4.7567 mL 23.7835 mL 47.5670 mL
    5 mM 0.9513 mL 4.7567 mL 9.5134 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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    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: ≥ 3 mg/mL (14.27 mM); Clear solution

      This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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% (20% SBE-β-CD in Saline)

      Solubility: ≥ 3 mg/mL (14.27 mM); Clear solution

      This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
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    Please enter your animal formula composition:
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    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.
    Purity & Documentation
    References

    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 4.7567 mL 23.7835 mL 47.5670 mL 118.9174 mL
    5 mM 0.9513 mL 4.7567 mL 9.5134 mL 23.7835 mL
    10 mM 0.4757 mL 2.3783 mL 4.7567 mL 11.8917 mL
    15 mM 0.3171 mL 1.5856 mL 3.1711 mL 7.9278 mL
    20 mM 0.2378 mL 1.1892 mL 2.3783 mL 5.9459 mL
    25 mM 0.1903 mL 0.9513 mL 1.9027 mL 4.7567 mL
    30 mM 0.1586 mL 0.7928 mL 1.5856 mL 3.9639 mL
    40 mM 0.1189 mL 0.5946 mL 1.1892 mL 2.9729 mL
    50 mM 0.0951 mL 0.4757 mL 0.9513 mL 2.3783 mL
    60 mM 0.0793 mL 0.3964 mL 0.7928 mL 1.9820 mL
    80 mM 0.0595 mL 0.2973 mL 0.5946 mL 1.4865 mL
    100 mM 0.0476 mL 0.2378 mL 0.4757 mL 1.1892 mL
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      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
    3PO
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