MTK458
Based on 6 publication(s) in Google Scholar
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.45%
- No. CAS: 2499962-58-0
- Fòrmula: C17H15F3N4
- Peso molecular:332.32
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Orally Active Compound Library
HY-L061
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Glutamine Metabolism Compound Library
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Anti-Cancer Metabolism Compound Library
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HY-L085
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Publications Citing Use of MedChemExpress (MCE) MTK458
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Customer Validation & Images
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Cell Imaging/Staining
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Cell Proliferation/Viability Assay
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WB
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WB
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WB
Actividad biológica
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 (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.
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Animal Model:Stratum of mice injected with α-synuclein preformed fibrils (PFFs)[1]
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Dosage:50 mg/kg
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Administration:Oral gavage (p.o.), daily, 6 months
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Result:Rescued an activity deficit in freely moving PFF mice.
Reduced the levels of inflammatory markers (TREM2, IL-6, and CXCL1).
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Animal Model:C57BL6J wildtype mice injected with PFF [1]
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Dosage:50 mg/kg
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Administration:Oral gavage (p.o.); 7 days, 3 weeks
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Result:Decreased pUb in the brain and plasma of PFF seeded mice.
Chemical Information
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No. CAS 2499962-58-0
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Appearance Solid
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Peso molecular 332.32
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Fòrmula C17H15F3N4
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Color White to yellow
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SMILES
FC(F)(F)C1=CC(C(N1)=NC=N2)=C2N[C@H]3C4=CC=CC=C4CCC3
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Synonyms
EP-0035985
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (6)
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Journal Impact Factor
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Most Recent
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Sci Adv
Putative PINK1/Parkin activators lower the threshold for mitophagy by sensitizing cells to mitochondrial stress. [Abstract]2025 Aug 29;11(35):eady0240. PMID: 40864725
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.
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Ecotoxicol Environ Saf
2026 May:316:120117. PMID: 41967262 -
Front Biosci (Landmark Ed)
Tectorigenin Protects Irradiation-Induced Injury of HUVECs by Inhibiting Mitophagy Through PINK1/Parkin Pathway. [Abstract]2026 May 25;31(5):48938. PMID: 42216527 -
Brain Res
PINK1 activation by MTK458 ameliorates neurological impairments and pyroptosis after intracerebral hemorrhage in mice. [Abstract]2025 Aug 15:1861:149700. PMID: 40368226 -
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bioRxiv
Visualizing PINK1 Activity Dynamics in Single Cells with a Phase Separation-Based Kinase Activity Reporter. [Abstract]2025 Oct 16:2025.10.08.681260. PMID: 41279391
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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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