2. Metabolic Enzyme/Protease Apoptosis NF-κB Immunology/Inflammation
  3. Lactate Dehydrogenase Apoptosis Reactive Oxygen Species
  4. FX-11

FX-11  (Synonyms: LDHA Inhibitor FX11)

Cat. No.: HY-16214 Purity: 99.21%
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FX-11 is a potent, selective, reversible and competitive lactate dehydrogenase A (LDHA) inhibitor, with a Ki of 8 μM. FX-11 reduces ATP levels and induces oxidative stress, ROS production and cell death. FX-11 shows antitumor activity in lymphoma and pancreatic cancer xenografts.

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

FX-11 Chemical Structure

FX-11 Chemical Structure

CAS No. : 213971-34-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 132 In-stock
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Based on 19 publication(s) in Google Scholar

FX-11 Related Antibodies

Top Publications Citing Use of Products

    FX-11 purchased from MedChemExpress. Usage Cited in: Sci Rep. 2023 Feb 24;13(1):3257.  [Abstract]

    FX11 (20 μM; pretreat for 1 h) decreases bTNF-α-induced COX-2 mRNA expression and PGE2 synthesis in bovine fibroblast-like synoviocyte.

    FX-11 purchased from MedChemExpress. Usage Cited in: Nat Metab. 2022 Dec 19.  [Abstract]

    FX11(1 mg/kg/day; i.p.) in combination with NSC23766 (NSC; 1.5 mg/kg/day; i.p.) for 2-3 weeks, displays a pronounced inhibitory effect on lung metastasis of Hs578T cells (fig c) and 4T1 cells (fig d).

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    FX-11 is a potent, selective, reversible and competitive lactate dehydrogenase A (LDHA) inhibitor, with a Ki of 8 μM. FX-11 reduces ATP levels and induces oxidative stress, ROS production and cell death. FX-11 shows antitumor activity in lymphoma and pancreatic cancer xenografts[1][2][3].

    IC50 & Target

    IC50: 23.3 μM (LDHA in HeLa cell) [1].
    In Vitro

    FX-11 (9 μM, 24-48 h) shows activation of AMP kinase and phosphorylation of its substrate acetyl-CoA carboxylase[2].
    FX-11 (0-100 μM, 72 h) inhibits cell proliferation in BxPc-3 and MIA PaCa-2 cells[3].
    FX-11 inhibits glycolysis and alters cellular energy metabolism in P493 cells[2].

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

    FX-11 Related Antibodies

    Western Blot Analysis[2]

    Cell Line: P493 cells
    Concentration: 9 μM
    Incubation Time: 24 h, 48 h
    Result: Showed a decrease in ATP levels, accompanied by activation of AMP kinase and phosphorylation of its substrate acetyl-CoA carboxylase.

    Cell Proliferation Assay[3]

    Cell Line: BxPc-3 and MIA PaCa-2 cells
    Concentration: 0-100 µM
    Incubation Time: 72 h
    Result: Reduced cell metabolic activity in a concentration-dependent manner, showed a significant reduction in cell proliferation, with IC50 values of 49.27 µM and 60.54 µM for BxPc-3 and MIA PaCa-2 cells, respectively.
    In Vivo

    FX-11 (42 μg/mouse; IP, daily for 10-14 days) inhibits P493 tumor growth[2].
    FX-11 (0-2 mg/kg, IP, daily, for 3 weeks) significantly delays tumor growth[3].

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

    Animal Model: Male SCID mice and RH-Foxn1nu mice (human P493 B-cell xenografts)[2]
    Dosage: 42 µg/mouse (2.1 mg/kg)
    Administration: IP; daily for 10-14 days
    Result: Resulted in a remarkable inhibition of tumor growth, inhibited tumor xenograft progression.
    Animal Model: Immunocompromised CD-1 mice (6-8 weeks; 20-25 g, n=5 per group)[3]
    Dosage: 2 mg/kg, 1 mg/kg+15 mg/kg TEPP-46, 2 mg/kg+30 mg/kg TEPP-46
    Administration: IP (100 µL), daily, for 3 weeks
    Result: Significantly lowered LDHA activity in plasma and tumor lysates; significantly lowered the expression of the proliferation marker Ki-67; significantly decreased proliferation indices were observed in tumor sections; significantly delayed tumor growth.
    Molecular Weight

    350.41

    Formula

    C22H22O4
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(C1=C2C=C(CC3=CC=CC=C3)C(C)=CC2=C(CCC)C(O)=C1O)O
    Shipping

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

    DMSO : 250 mg/mL (713.45 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 2.8538 mL 14.2690 mL 28.5380 mL
    5 mM 0.5708 mL 2.8538 mL 5.7076 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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    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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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: ≥ 2.08 mg/mL (5.94 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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 (5.94 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.
    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 2.8538 mL 14.2690 mL 28.5380 mL 71.3450 mL
    5 mM 0.5708 mL 2.8538 mL 5.7076 mL 14.2690 mL
    10 mM 0.2854 mL 1.4269 mL 2.8538 mL 7.1345 mL
    15 mM 0.1903 mL 0.9513 mL 1.9025 mL 4.7563 mL
    20 mM 0.1427 mL 0.7134 mL 1.4269 mL 3.5672 mL
    25 mM 0.1142 mL 0.5708 mL 1.1415 mL 2.8538 mL
    30 mM 0.0951 mL 0.4756 mL 0.9513 mL 2.3782 mL
    40 mM 0.0713 mL 0.3567 mL 0.7134 mL 1.7836 mL
    50 mM 0.0571 mL 0.2854 mL 0.5708 mL 1.4269 mL
    60 mM 0.0476 mL 0.2378 mL 0.4756 mL 1.1891 mL
    80 mM 0.0357 mL 0.1784 mL 0.3567 mL 0.8918 mL
    100 mM 0.0285 mL 0.1427 mL 0.2854 mL 0.7134 mL
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    FX-11 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:

    FX-11213971-34-7LDHA Inhibitor FX11FX11FX 11LDHA Inhibitor FX 11LDHA Inhibitor FX-11Lactate DehydrogenaseApoptosisReactive Oxygen SpeciesLDHP493 cellspancreatic cancerlymphomaredox stressglycolysisreactive oxygen speciesPC-3RR cellsInhibitorinhibitorinhibit

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