MTK458 free base · Synonyms: EP-0035985

MTK458 is an orally active brain penetrant PINK1 activator.

For research use only. Not for human or veterinary use.

Target PINK1/Parkin Mitophagy Mitochondrial Metabolism

Research area Neurological Disease Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

MTK458 structure

CAS No.: 2499962-58-0

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 450.00	BP-02025-100mg	In stock	Get quote
250 mg	USD 850.00	BP-02025-250mg	In stock	Get quote
500 mg	USD 1,360.00	BP-02025-500mg	In stock	Get quote
1 g	USD 2,180.00	BP-02025-1g	In stock	Get quote

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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.

Biological activity

In Vitro MTK458 (25 µM) increases PINK1-mediated mitophagy to enhance clearance of intramitochondrial aggregates in Hela cells induced ΔOTC and YFP-Parkin. MTK458 (0.1-25 µM) clears pS129 α-synuclein aggregates (12-250 kDa) in a dose-dependent manner in DIV9 and DIV12. MTK458 (0-13 µM, 10 days) reduces α-synuclein pathology and the mitochondrial stress marker pUb in iPSC neurons. 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). MTK458 (50 mg/kg, p.o., 6 doses, 5 days) decreases plasma pS65-Ubiquitin (pUb) in wild-type Sprague-Dawley rats.

Identifiers

SMILES: FC(F)(F)C(N1)=CC2=C1N=CN=C2N[C@H]3C(C=CC=C4)=C4CCC3
InChIKey: JOIONRWKOGDQOG-CYBMUJFWSA-N

Specifications

MW (average): 332.3230
Formula: C₁₇H₁₅F₃N₄
CAS No.: 2499962-58-0
Physical state: Solid
Color: White to yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder 4℃ 2 years, sealed storage, away from moisture; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO : 100 mg/mL

Documents

References

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

Same target

Search PINK1/Parkin

Same research area

Search Neurological Disease