2. Metabolic Enzyme/Protease Apoptosis
  3. PDHK Apoptosis
  4. JX06

JX06 is a potent, selective and covalent inhibitor of PDK. JX06 inhibits PDK1, PDK2 and PDK3 with IC50s of 49 nM, 101 nM, and 313 nM, respectively. JX06 inhibits PDK1 activity via covalently binding to a cysteine residue in an irreversible manner. JX06 shows significant antitumor activity.

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

CAS No. : 729-46-4

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Customer Review

Based on 6 publication(s) in Google Scholar

JX06 Related Antibodies

Top Publications Citing Use of Products

    JX06 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 Mar 6;16(1):158.  [Abstract]

    Huh7 cells were infected with Lenti-PRMT3 or Lenti-Ctrl and then treated with JX06 (200 nM) or DMSO. The representative images of stained transwell chamber were shown at the right.

    JX06 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 Mar 6;16(1):158.  [Abstract]

    In Huh7 xenograft mouse model, JX06 (30 mg/kg, i.p.) treatment diminished the tumor-promoting effects of PRMT3.

    JX06 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 Mar 6;16(1):158.  [Abstract]

    Immunoblot analysis of PRMT3, PDHK1, and p-PDHA (phosphorylated PDHA) levels in Huh7 xenografts derived from nude mice treated with JX06 (30 mg/kg, i.p.)

    JX06 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 Mar 6;16(1):158.  [Abstract]

    PD-L1 mRNA levels were measured in Huh7 and Hepa1-6 cells with the indicated treatments. Hepatoma cells were infected with Lenti-PRMT3 or Lenti-Ctrl and then treated with JX06 (200 nM).

    JX06 purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2025 Apr 2;26(7):3321.  [Abstract]

    JX06 (10 μM) significantly reduced the levels of total ROS and mitochondrial ROS in force-loaded macrophages.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    JX06 is a potent, selective and covalent inhibitor of PDK. JX06 inhibits PDK1, PDK2 and PDK3 with IC50s of 49 nM, 101 nM, and 313 nM, respectively. JX06 inhibits PDK1 activity via covalently binding to a cysteine residue in an irreversible manner. JX06 shows significant antitumor activity[1].

    IC50 & Target

    IC50: 49 nM (PDK1), 101 nM (PDK2), 313 nM (PDK3)[1]
    Cellular Effect
    Cell Line Type Value Description References
    A549 IC50
    0.48 μM
    Compound: 16; JX06
    Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay
    Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay
    		[PMID: 28230989]
    A549 IC50
    < 0.5 μM
    Compound: JX06
    Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
    Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
    		[PMID: 38056298]
    Kelly IC50
    0.289 μM
    Compound: 16; JX06
    Antiproliferative activity against human Kelly cells after 72 hrs by CCK8 assay
    Antiproliferative activity against human Kelly cells after 72 hrs by CCK8 assay
    		[PMID: 28230989]
    L02 IC50
    > 10 μM
    Compound: 16; JX06
    Antiproliferative activity against human LO2 cells after 72 hrs by CCK8 assay
    Antiproliferative activity against human LO2 cells after 72 hrs by CCK8 assay
    		[PMID: 28230989]
    In Vitro

    JX06 barely shows inhibitory activity against PDK4 at a concentration of 10 μM[1].
    ? JX06 (1-10 μM; 48 hours) induces cell apoptosis in cancer cells with high ECAR/OCR[1].
    ? JX06 (0-0.6 μM; 72 hours) dose-dependently suppresses the growth of A549 cells[1].
    ? JX06 (0.1-10 μM; 6-24 hours) inhibits PDHA1 phosphorylation in A549 cells in a time- and dose-dependent manner[1].
    ? JX06 (1-10 μM) increases glucose uptake and intracellular ATP level and reduces aerobic glycolysis determined by the lactate production in A549 cells[1].
    ? JX06 (1-10 μM; 24 hours) induces ROS generation in cancer cells with high extracellular acidification rate (ECAR)/ oxygen consumption rate (OCR) [1].

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

    JX06 Related Antibodies

    Apoptosis Analysis[1]

    Cell Line: A549, EBC-1, HT-29 and H460 cells
    Concentration: 0, 1, 3, 10 μM
    Incubation Time: 48 hours
    Result: Induces cell apoptosis in A549 and EBC-1 cells.

    Cell Viability Assay[1]

    Cell Line: A549 cells
    Concentration: 0, 0.2, 0.4, 0.6 μM
    Incubation Time: 72 hours
    Result: Inhibits the viability of A549 cells in a dose dependent manner.

    Western Blot Analysis[1]

    Cell Line: A549 cells
    Concentration: 0, 0.1, 0.3, 1, 3, 10 μM
    Incubation Time: 0, 6, 12, 24 hours
    Result: Decreased PDHA1 phosphorylation at both serine 293 and serine 232 (S293 and S232) in a time- and dose-dependent manner.
    In Vivo

    JX06 (40-80?mg/kg; i.p. for 21 days) inhibits tumor growth in vivo[1].

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

    Animal Model: A549 subcutaneous xenograft mice[1]
    Dosage: 40, 80 mg/kg
    Administration: I.p. injections for 21 days
    Result: Reduced tumor weights and 67.5% tumor volume at the dose of 80 mg/kg compared with the vehicle control.
    Well tolerated at the administration dose.
    Molecular Weight

    324.51

    Formula

    C10H16N2O2S4
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    S=C(N1CCOCC1)SSC(N2CCOCC2)=S
    Shipping

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

    DMSO : 50 mg/mL (154.08 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 3.0816 mL 15.4078 mL 30.8157 mL
    5 mM 0.6163 mL 3.0816 mL 6.1631 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
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    Concentration
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    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

    ×
    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 (7.70 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% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (7.70 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 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
    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: 99.78%

    SDS (538 KB)

    COA (246 KB) LCMS (95 KB)

    Handling Instructions (2659 KB)
    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 3.0816 mL 15.4078 mL 30.8157 mL 77.0392 mL
    5 mM 0.6163 mL 3.0816 mL 6.1631 mL 15.4078 mL
    10 mM 0.3082 mL 1.5408 mL 3.0816 mL 7.7039 mL
    15 mM 0.2054 mL 1.0272 mL 2.0544 mL 5.1359 mL
    20 mM 0.1541 mL 0.7704 mL 1.5408 mL 3.8520 mL
    25 mM 0.1233 mL 0.6163 mL 1.2326 mL 3.0816 mL
    30 mM 0.1027 mL 0.5136 mL 1.0272 mL 2.5680 mL
    40 mM 0.0770 mL 0.3852 mL 0.7704 mL 1.9260 mL
    50 mM 0.0616 mL 0.3082 mL 0.6163 mL 1.5408 mL
    60 mM 0.0514 mL 0.2568 mL 0.5136 mL 1.2840 mL
    80 mM 0.0385 mL 0.1926 mL 0.3852 mL 0.9630 mL
    100 mM 0.0308 mL 0.1541 mL 0.3082 mL 0.7704 mL
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    JX06 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:

    JX06729-46-4JX 06JX-06PDHKApoptosisPyruvate dehydrogenase kinasePDH kinaseInhibitorinhibitorinhibit

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