2. Autophagy Apoptosis
  3. Autophagy Apoptosis
  4. PFK-158

PFK-158 is a potent and selective PFKFB3 inhibitor with an IC50 value 137 nM. PFK-158 reduces glucose uptake, ATP production, lactate release, and induces apoptosis and autophagy in cancer cells. PFK-158 has broad anti-tumor activity. PFK-158 can also enhance Colistin's resistance to bacteria.

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CAS No. : 1462249-75-7

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Customer Review

Based on 11 publication(s) in Google Scholar

PFK-158 Related Antibodies

Top Publications Citing Use of Products

    PFK-158 purchased from MedChemExpress. Usage Cited in: Cell Rep. 2023 Dec 18;43(1):113557.  [Abstract]

    Cell viability of DIPG IV and SF8628 cells treated with ERK5-IN-1, PFK-158, or combination ERK5-IN-1 and PFK-158 (dual) compared with vehicle control.

    PFK-158 purchased from MedChemExpress. Usage Cited in: Cell Rep. 2023 Dec 18;43(1):113557.  [Abstract]

    Flow cytometry plots with annexin-propidium iodide (PI) assay in SF8268 cells treated with ERK5-IN-1, PFK-158, or combination ERK5-IN-1 and PFK-158 (dual) compared with vehicle control.

    PFK-158 purchased from MedChemExpress. Usage Cited in: Cell Rep. 2023 Dec 18;43(1):113557.  [Abstract]

    Apoptosis of DIPG IV cells treated with ERK5-IN-1, PFK-158, or combination ERK5-IN-1 and PFK-158 (dual) compared with vehicle control.

    PFK-158 purchased from MedChemExpress. Usage Cited in: Cells. 2021 Jul 3;10(7):1679.

    PC9 and H522 cells were transfected with a pEGFP-LC3 plasmid and treated with erlotinib (PC9: 0.5 µM; H522: 2 µM) and/or PFK158 (PC9: 5 µM; H522: 0.75 µM) for 36 h or 24 h respectively, Whole cell lysates were immunoblotted with the indicated antibodies.

    PFK-158 purchased from MedChemExpress. Usage Cited in: Cells. 2021 Jul 3;10(7):1679.

    PC9 and H522 cells were transfected with a pEGFP-LC3 plasmid and treated with erlotinib (PC9: 0.5 µM; H522: 2 µM) and/or PFK158 (PC9: 5 µM; H522: 0.75 µM) for 36 h or 24 h, respectively. GFP-LC3 localization was evaluated by fluorescence microscopy.

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    • Purity & Documentation

    • References

    • Customer Review

    Description

    PFK-158 is a potent and selective PFKFB3 inhibitor with an IC50 value 137 nM. PFK-158 reduces glucose uptake, ATP production, lactate release, and induces apoptosis and autophagy in cancer cells. PFK-158 has broad anti-tumor activity. PFK-158 can also enhance Colistin's resistance to bacteria[1][2][3].

    IC50 & Target

    IC50 : 137 nM (PFKFB3)[1][3]
    Cellular Effect
    Cell Line Type Value Description References
    A549 IC50
    15 μM
    Compound: A13; PFK-158
    Cytotoxicity against human A549 cells
    Cytotoxicity against human A549 cells
    		[PMID: 33766773]
    In Vitro

    PFK-158 (10 μM ; 24 hours; OV2008 and C13 cells) combined with Carboplatin (CBPt; 77-453 μM) results in significant increase in apoptosis in C13 (45%) and OV2008 cells (24.6%)[1].
    PFK-158 (0-10 μM ; 24 hours; C13 and HeyA8MDR cells) treatment results in a dose-dependent decrease in p-PFKFB3, p-cPLA2 and lipid droplet (LD) levels[1].
    PFK-158 (10 μM; 24 hours) has synergistic anti-proliferative effects in vitro when combined with Cisplatin in C13 and HeyA8MDR cells compared to OV2008 and HeyA8, respectively[1].
    PFK-158 (0‐10 μM; 24 h) treatment shows a dose-dependent downregulation of p62/SQSTM1 and upregulation of LC3BII, two markers of autophagy induction, in both C13 and HeyA8MDR cells. PFK-158 treatment also reduces the numbers of LDs[1].

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

    PFK-158 Related Antibodies

    Apoptosis Analysis[1]

    Cell Line: OV2008 and C13 cells
    Concentration: 10 µM
    Incubation Time: 24 hours
    Result: Combined with Carboplatin (CBPt) treatment resulted in significant increase in apoptosis.

    Western Blot Analysis[1]

    Cell Line: C13 and HeyA8MDR cells
    Concentration: 0 µM, 5 µM, 10 µM
    Incubation Time: 24 hours
    Result: Demonstrated a dose-dependent decrease in p-PFKFB3, p-cPLA2 and lipid droplet (LD) levels.
    In Vivo

    PFK-158 (15 mg/kg; intraperitoneal injection; once a week; for 4 weeks; female athymic nude mice) plus CBPt (51 mg/kg) treatment leads to significantly enhanced antitumor activity in a gynecologic cancer mouse model[1].

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

    Animal Model: Female athymic nude mice (nu/nu) (5-6 weeks old) injected with HeyA8MDR cells[1]
    Dosage: 15 mg/kg
    Administration: Intraperitoneal injection; once a week; for 4 weeks
    Result: A marked reduction of tumor growth was observed in the combination treatment.
    Clinical Trial
    Molecular Weight

    328.29

    Formula

    C18H11F3N2O
    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    O=C(C1=CC=NC=C1)/C=C/C2=NC3=CC(C(F)(F)F)=CC=C3C=C2
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (152.30 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 3.0461 mL 15.2304 mL 30.4609 mL
    5 mM 0.6092 mL 3.0461 mL 6.0922 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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    In Vivo:

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  50% PEG300    50% Saline

      Solubility: 1.67 mg/mL (5.09 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  0.5% CMC-Na/1% Tween-80 in Saline water

      Solubility: 2.48 mg/mL (7.55 mM); Suspended solution; Need ultrasonic

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

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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    Working solution concentration: mg/mL
    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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.0461 mL 15.2304 mL 30.4609 mL 76.1522 mL
    5 mM 0.6092 mL 3.0461 mL 6.0922 mL 15.2304 mL
    10 mM 0.3046 mL 1.5230 mL 3.0461 mL 7.6152 mL
    15 mM 0.2031 mL 1.0154 mL 2.0307 mL 5.0768 mL
    20 mM 0.1523 mL 0.7615 mL 1.5230 mL 3.8076 mL
    25 mM 0.1218 mL 0.6092 mL 1.2184 mL 3.0461 mL
    30 mM 0.1015 mL 0.5077 mL 1.0154 mL 2.5384 mL
    40 mM 0.0762 mL 0.3808 mL 0.7615 mL 1.9038 mL
    50 mM 0.0609 mL 0.3046 mL 0.6092 mL 1.5230 mL
    60 mM 0.0508 mL 0.2538 mL 0.5077 mL 1.2692 mL
    80 mM 0.0381 mL 0.1904 mL 0.3808 mL 0.9519 mL
    100 mM 0.0305 mL 0.1523 mL 0.3046 mL 0.7615 mL
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    PFK-158 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      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.

    Keywords:

    PFK-1581462249-75-7PFK158PFK 158AutophagyApoptosisPFKFB3apoptosisanti-tumorglycolysislactateanti-proliferativep-cPLA2LC3BIIInhibitorinhibitorinhibit

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