2. Neuronal Signaling Autophagy Metabolic Enzyme/Protease
  3. PINK1/Parkin Mitophagy Mitochondrial Metabolism
  4. MTK458

MTK458 is an orally active brain penetrant PINK1 activator. MTK458 binds to PINK1 and stabilizes an active heterocomplex, thereby increasing mitophagy. MTK458 can be used for research on Parkinson's disease.

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

CAS No. : 2499962-58-0

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10 mM * 1 mL in DMSO
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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of MTK458:

MTK458 Related Antibodies

Top Publications Citing Use of Products

    MTK458 purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Aug 29;11(35):eady0240.  [Abstract]

    Confocal imaging of mt-Keima–expressing HeLa cells after treatment with 7.8 nM O/A alone, 7.8 nM O/A and 1.25 μM FB231, or 7.8 nM O/A and 2.5 μM MTK458 for 6 hours.

    MTK458 purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Aug 29;11(35):eady0240.  [Abstract]

    After treating YFP-Parkin mt-Keima HeLa cells with different doses of O/A and MTK458 for 6 hours, mt-Keima activity was detected, and each treatment was labeled with a different color.

    MTK458 purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Aug 29;11(35):eady0240.  [Abstract]

    Western blot analysis was performed on HeLa cells expressing YFP-Parkin/mt-Keima to detect the expression of mitophagy biomarkers pUb, YFP-Parkin, and COX4I2. These cells were treated with different doses of FB231 or MTK458, with or without 10 nM O/A, for 6 hours.

    MTK458 purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Aug 29;11(35):eady0240.  [Abstract]

    COX4I2 immunoblotting analysis was performed on SH-SY5Y cells. Cells were treated alone or in combination with 10 nM O/A for 16 hours, or in combination with 10 μM FB231 or 5 μM MTK458.

    MTK458 purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Aug 29;11(35):eady0240.  [Abstract]

    After treating WT SH-SY5Y cells with 10 nM O/A, 10 μM FB231 and 5 μM MTK458 for 16 hours, Western blot analysis of IFRD1, ATF3, ATF4 and FECH was performed.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    MTK458 is an orally active brain penetrant PINK1 activator. MTK458 binds to PINK1 and stabilizes an active heterocomplex, thereby increasing mitophagy. MTK458 can be used for research on Parkinson's disease[1].

    In Vitro

    MTK458 (25 µM) increases PINK1-mediated mitophagy to enhance clearance of intramitochondrial aggregates in Hela cells induced ΔOTC and YFP-Parkin[1].
    MTK458 (0.1-25 µM) clears pS129 α-synuclein aggregates (12-250 kDa) in a dose-dependent manner in DIV9 and DIV12[1].
    MTK458 (0-13 µM, 10 days) reduces α-synuclein pathology and the mitochondrial stress marker pUb in iPSC neurons[1].

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

    MTK458 Related Antibodies
    In Vivo

    MTK458 (50 mg/kg, p.o., daily, 6 months) drives clearance of pathologic α-synuclein in a dose-dependent manner in the stratum of mice injected with α-synuclein preformed fibrils (PFFs)[1].
    MTK458 (50 mg/kg, p.o., 6 doses, 5 days) decreases plasma pS65-Ubiquitin (pUb) in wild-type Sprague-Dawley rats[1].

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

    Animal Model: Stratum of mice injected with α-synuclein preformed fibrils (PFFs)[1]
    Dosage: 50 mg/kg
    Administration: Oral gavage (p.o.), daily, 6 months
    Result: Rescued an activity deficit in freely moving PFF mice.
    Reduced the levels of inflammatory markers (TREM2, IL-6, and CXCL1).
    Animal Model: C57BL6J wildtype mice injected with PFF [1]
    Dosage: 50 mg/kg
    Administration: Oral gavage (p.o.); 7 days, 3 weeks
    Result: Decreased pUb in the brain and plasma of PFF seeded mice.
    Molecular Weight

    332.32

    Formula

    C17H15F3N4
    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    FC(F)(F)C1=CC(C(N1)=NC=N2)=C2N[C@H]3C4=CC=CC=C4CCC3
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (300.91 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 3.0091 mL 15.0457 mL 30.0915 mL
    5 mM 0.6018 mL 3.0091 mL 6.0183 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 (sealed storage, away from moisture). 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)

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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    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (7.52 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).

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    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: 99.45%

    SDS (252 KB)

    COA (252 KB) HNMR (136 KB) RP-HPLC (174 KB) LCMS (101 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 (sealed storage, away from moisture). 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 3.0091 mL 15.0457 mL 30.0915 mL 75.2287 mL
    5 mM 0.6018 mL 3.0091 mL 6.0183 mL 15.0457 mL
    10 mM 0.3009 mL 1.5046 mL 3.0091 mL 7.5229 mL
    15 mM 0.2006 mL 1.0030 mL 2.0061 mL 5.0152 mL
    20 mM 0.1505 mL 0.7523 mL 1.5046 mL 3.7614 mL
    25 mM 0.1204 mL 0.6018 mL 1.2037 mL 3.0091 mL
    30 mM 0.1003 mL 0.5015 mL 1.0030 mL 2.5076 mL
    40 mM 0.0752 mL 0.3761 mL 0.7523 mL 1.8807 mL
    50 mM 0.0602 mL 0.3009 mL 0.6018 mL 1.5046 mL
    60 mM 0.0502 mL 0.2508 mL 0.5015 mL 1.2538 mL
    80 mM 0.0376 mL 0.1881 mL 0.3761 mL 0.9404 mL
    100 mM 0.0301 mL 0.1505 mL 0.3009 mL 0.7523 mL
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    MTK458 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:

    MTK4582499962-58-0EP-0035985MTK 458MTK-458EP0035985EP 0035985PINK1/ParkinMitophagyMitochondrial MetabolismPTEN-induced kinase 1/ParkinMitochondrial AutophagyPINK1 activatorbrain penetrantorally activemitophagyα-synucleinpS65-UbiquitinParkinson's diseaseInhibitorinhibitorinhibit

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