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MTK458

Chemical Structure : MTK458

CAS No.: 2499962-58-0

MTK458 (MTK-458)

Catalog No.: PC-49861Not For Human Use, Lab Use Only.

MTK458 (MTK-458) is a potent, selective and brain penetrant PINK1 activator, MTK-458 promotes the first step in mitophagy.

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Purity & Documentation Purity: 98.48% (HPLC) Select Batch:

Biological Activity

MTK458 (MTK-458) is a potent, selective and brain penetrant PINK1 activator, MTK-458 promotes the first step in mitophagy.
MTK458 selectively activates PINK1 by stimulating dimerization and stabilization of the PINK1/TOM complex.
MTK458 binds to PINK1 and stabilizes an active heterocomplex, thereby increasing mitophagy.
MTK458 reduces the PINK1 substrate pS65-Ubiquitin (pUb) in primary neurons and in vivo.
MTK458 drives clearance of pathologic α-synuclein in vitro and in vivo, decreases pS129 α-synuclein aggregates and normalized both brain and corresponding plasma pUb levels in both cellular and animal models of α-synuclein aggregation (PD-like pathology).

Physicochemical Properties

M.Wt 332.33
Formula C17H15F3N4
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(R)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-6-(trifluoromethyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine

References

1. Chin RM, et al. bioRxiv. 2023 Feb 15:2023.02.14.528378.

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