2. Metabolic Enzyme/Protease
  3. Mitochondrial Metabolism
  4. UK-5099

UK-5099 (PF-1005023) is a potent inhibitor of the mitochondrial pyruvate carrier (MPC). UK-5099 (PF-1005023) inhibits pyruvate-dependent O2 consumption with an IC50 of 50 nM.

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

CAS No. : 56396-35-1

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Customer Review

Based on 53 publication(s) in Google Scholar

UK-5099 Related Antibodies

Top Publications Citing Use of Products

53 Publications Citing Use of MCE UK-5099

Cell Proliferation/Viability Assay
Flow Cytometry
WB

    UK-5099 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 May 15;16(1):4502.  [Abstract]

    Naive Tigit−/− or Tigit+/+ CD4+ T cells were cultured under Th1- or Th17- polarizing condition for 5 d. UK5099 (20 μM), MSDC-0602 (10 μM), Etomoxir (ETO, 1 μM), or bis-2-(5-phenylacetamido-1, 2, 4-thiadiazol-2-yl) ethyl sulfide (BPTES, 3 μM) was included for the last 48 h of culture. IFNγ, T-bet, IL-17A, and RORγt expression in CD4+ T cells were measured by flow cytometry.

    UK-5099 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 May 15;16(1):4502.  [Abstract]

    Naive Tigit−/− or Tigit+/+ CD4+ T cells were cultured under Th1- or Th17- polarizing condition for 5 d. UK5099 (20 μM), MSDC-0602 (10 μM), Etomoxir (ETO,1 μM), or bis-2-(5-phenylacetamido-1, 2,4-thiadiazol-2-yl) ethyl sulfide (BPTES, 3 μM) was included for the last 48 h of culture. IFNγ, T-bet, IL-17A, and RORγt expression in CD4+ T cells were measured by flow cytometry.

    UK-5099 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 May 15;16(1):4502.  [Abstract]

    CD4+ T cells from HC or PM patients were stimulated with αCD3/CD28 in the presence of UK5099 (20 μM), recombinant human CD155-Fc (10 μg/ml), or control IgG1 for 3 d.

    UK-5099 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 May 15;16(1):4502.  [Abstract]

    Immunoblot analysis of acetylated H3K9 and H3K27 in mouse CD4+ T cells and representative bands.Cells were stimulated with αCD3/CD28 for 3 days in the presence of UK5099 (20 μM), ETO, or BPTES.

    UK-5099 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Aug 3;15(1):6587.  [Abstract]

    NIC cells were treated with 10μM UK5099, or DMSO as a control. Proliferation was assessed by Incucyte® to measure cell confluency in real time.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    UK-5099 (PF-1005023) is a potent inhibitor of the mitochondrial pyruvate carrier (MPC). UK-5099 (PF-1005023) inhibits pyruvate-dependent O2 consumption with an IC50 of 50 nM.

    IC50 & Target

    IC50: 50 nM (MPC)[1]
    In Vitro

    The trypanosomal pyruvate carrier is found to be rather insensitive to inhibition by alpha-cyano-4-hydroxycinnamate (Ki=17 mM) but can be completely blocked by UK-5099 (Ki=49 microM)[2]. UK-5099 also inhibits the monocarboxylate transporter (MCT) [3]. UK5099 significantly inhibits the glucose-stimulated rise in oxygen consumption in a dose-dependent manner and at 150 μM reduced oxygen consumption below basal levels. UK5099 reduces ATP levels and increases ADP and AMP levels in 832/13 cells[4]. The UK5099 treated cells show significantly higher proportion of side population fraction and express higher levels of stemness markers Oct3/4 and Nanog. UK5099 application may be an ideal model for Warburg effect studies[5].

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

    UK-5099 Related Antibodies
    In Vivo

    The MPC inhibitor UK5099 increases the glucose excursion seen during an intraperitoneal glucose tolerance test in C57BLK mice[4].

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

    288.30

    Formula

    C18H12N2O2
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C(O)/C(C#N)=C/C1=CN(C2=CC=CC=C2)C3=C1C=CC=C3
    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 (173.43 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.4686 mL 17.3430 mL 34.6861 mL
    5 mM 0.6937 mL 3.4686 mL 6.9372 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.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
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    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

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    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 (8.67 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      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: ≥ 2.5 mg/mL (8.67 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 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 (25.0 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)

    μL

    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

    Purity: 99.95%

    SDS (393 KB)

    COA (258 KB) RP-HPLC (244 KB) MS (177 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [4]

    The 832/13 cell line is used for experiments. Cell viability is measured using CellTiter Blue. The assay is based on cellular reduction of resazurin to resorufin. Appearance of resorufin is monitored by fluorescence emission at 585 nm using a Spectramax M5 microplate reader with excitation at 555 nm. For UK5099-treated cells, cells are allowed to recover for 1 h before measuring cell viability. Data are expressed as -fold relative to no treatment or siCtrl[4].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [4]

    C57BLK mice are fasted for 16 h prior to glucose challenge. UK5099 (32 μmol/kg of body weight) or DMSO in PBS is injected into the intraperitoneal cavity 30 min before injecting glucose (1.5 mg of glucose/g of body weight). Blood glucose levels are measured at 0, 10, 20, 30, 60, and 120 min after glucose injection[4].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    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 3.4686 mL 17.3430 mL 34.6861 mL 86.7152 mL
    5 mM 0.6937 mL 3.4686 mL 6.9372 mL 17.3430 mL
    10 mM 0.3469 mL 1.7343 mL 3.4686 mL 8.6715 mL
    15 mM 0.2312 mL 1.1562 mL 2.3124 mL 5.7810 mL
    20 mM 0.1734 mL 0.8672 mL 1.7343 mL 4.3358 mL
    25 mM 0.1387 mL 0.6937 mL 1.3874 mL 3.4686 mL
    30 mM 0.1156 mL 0.5781 mL 1.1562 mL 2.8905 mL
    40 mM 0.0867 mL 0.4336 mL 0.8672 mL 2.1679 mL
    50 mM 0.0694 mL 0.3469 mL 0.6937 mL 1.7343 mL
    60 mM 0.0578 mL 0.2891 mL 0.5781 mL 1.4453 mL
    80 mM 0.0434 mL 0.2168 mL 0.4336 mL 1.0839 mL
    100 mM 0.0347 mL 0.1734 mL 0.3469 mL 0.8672 mL
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    UK-5099 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:

    UK-509956396-35-1PF-1005023UK5099UK 5099PF1005023PF 1005023Mitochondrial MetabolismInhibitorinhibitorinhibit

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