| Name | MTK458 |
| Description | MTK458 (EP-0035985) is an orally active and brain-permeable PINK1 activator that promotes pathological clearance of alpha-synuclein and reduces pUb in a PFF inoculation model.MTK458 induces pathological alpha-synuclein clearance by stimulating dimerization and stabilization of the PINK1/TOM complex.MTK458 may be used in Parkinson's disease research. |
| In vitro | Mitophagy activator 1 (0.1-25 µM), as a brain-penetrant small molecule, binds to PINK1 and stabilizes the active heterocomplex, thereby enhancing mitochondrial autophagy. It clears pS129 α-synuclein aggregates in a dose-dependent manner at DIV9 and DIV12[1]. |
| In vivo | In the striatum of mice injected with α-synuclein preformed fibrils (PFFs), Mitophagy activator 1 (50 mg/kg; oral gavage (p.o.), daily, for 6 months) rescued activity deficits in freely moving PFF mice and reduced the levels of inflammatory markers (TREM2, IL-6, and CXCL1)[1]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+90% Corn Oil : 3.3 mg/mL (9.93 mM), Sonication is recommended. DMSO : 80 mg/mL (240.73 mM), Sonification is recommended.
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| Keywords | PTEN-induced kinase 1 (PINK1) |
| Inhibitors Related | 1-Hexanol | Hemin | Rotenone | Curcumin | Valproic Acid | (-)-Epigallocatechin Gallate | Dexamethasone | Naringin | Sodium Molybdate | Quercetin | 4-Pentenoic acid | L-Histidine |
| Related Compound Libraries | PI3K-AKT-mTOR Compound Library | Anti-Colorectal Cancer Compound Library | Bioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | Anti-Ovarian Cancer Compound Library | Orally Active Compound Library | Immunology/Inflammation Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Anti-Liver Cancer Compound Library | Neuronal Differentiation Compound Library |