Art. -Nr.: HY-152943

MTK458

(Synonyms: EP-0035985)

6 Cited Publications

Kundenbewertung

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.

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Reinheit: 99.45%
CAS. Nr.: 2499962-58-0
Formel: C₁₇H₁₅F₃N₄
Molecular Weight:332.32

Speicherung:

4°C, sealed storage, away from moisture

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

MTK458 Chemical Structure

CAS. Nr.: 2499962-58-0

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Publications (6)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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.

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.

Chemical Information

CAS. Nr. 2499962-58-0
Appearance Solid
Molecular Weight 332.32
Formel C₁₇H₁₅F₃N₄
Color White to yellow
SMILES

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

EP-0035985
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

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

Publications (6)

All Cell Imaging/StainingCell Proliferation/Viability AssayWB

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Journal Impact Factor

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.
Ecotoxicol Environ Saf

PINK1-Parkin-Mediated mitophagy alleviates hepatocyte injury induced by α-amanitin. [Abstract]

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 May 12:149700. PMID: 40368226
bioRxiv

2026 Jan 8.
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

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.0091 mL

15.0457 mL

30.0915 mL

5 mM

0.6018 mL

3.0091 mL

6.0183 mL

10 mM

0.3009 mL

1.5046 mL

3.0091 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Chin RM, et al. Pharmacological PINK1 activation ameliorates Pathology in Parkinson's Disease models. bioRxiv [Preprint]. 2023 Feb 15:2023.02.14.528378. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

MTK458

6 Cited Publications

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MTK458

Metabolism/Protease Compound Library

Neuronal Signaling Compound Library

Stem Cell Signaling Compound Library

CNS-Penetrant Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Orally Active Compound Library

Glutamine Metabolism Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Mitochondria-Targeted Compound Library

Glucose Metabolism Compound Library

Cuproptosis Compound Library

Mitochondrial Protection Compound Library

Metabolic Enzyme Compound Library

Mitophagy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) MTK458

Biologische Aktivität

Chemical Information

Publications (6)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MTK458

Metabolism/Protease Compound Library

Neuronal Signaling Compound Library

Stem Cell Signaling Compound Library

CNS-Penetrant Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Orally Active Compound Library

Glutamine Metabolism Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Mitochondria-Targeted Compound Library

Glucose Metabolism Compound Library

Cuproptosis Compound Library

Mitochondrial Protection Compound Library

Metabolic Enzyme Compound Library

Mitophagy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) MTK458

Biologische Aktivität

Chemical Information

Publications (6)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MTK458 Related Classifications

HY-152943 Related Classifications