MRL828
MRL828 is a heterobifunctional molecule that targets aggregated tau protein. As an autophagy-targeting chimera (ATTEC), MRL828 selectively labels aggregated tau protein for clearance via the autophagy (autophagy)-lysosome pathway. The activity of MRL828 depends on autophagosomes rather than lysosomes, and it induces autophagosome-dependent secretion. MRL828 acts as an intracellular aggregate inhibitor and a secretory autophagy inducer, reducing intracellular levels of aggregated tau protein through autophagosome-dependent secretory autophagy instead of lysosomal degradation. MRL828 can be used in the research of neurodegenerative diseases such as Alzheimer's disease.
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- CAS. Nr.: 3115333-82-6
- Formel: C46H51FN14O5S
- Molecular Weight:931.05
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
Tau aggregates 50 nM (DC50) |
In Vitro
The reduction of aggregated tau induced by MRL828 (1 μM; 24-48 h) in tau aggregation-induced CHO T-REx P301L cells depends on p62 and VPS34, components of the autophagy pathway[1].
MRL828 (1 μM, 24-48 h) still reduces tau aggregates in the presence of Bafilomycin A1 (HY-100558, 25 nM) or Hydroxychloroquine (HY-W031727, 15 μM), and does not increase the colocalization of MC1-positive tau puncta with the lysosomal marker LAMP2 at 24 h, indicating that its mechanism of action is independent of lysosomes.[1]
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:tau aggregation-induced CHO T-REx P301L cells
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Concentration:1 μM (MRL828); 100 nM (Bafilomycin A1 for LC3-II analysis); 25 nM (Bafilomycin A1 for DQ-BSA imaging)
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Incubation Time:MRL828 44 h followed by Bafilomycin A1 cotreatment for 4 h for LC3-II analysis; MRL828 or Bafilomycin A1 48 h, with DQ-BSA added 6 h before the end of treatment
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Result:Did not alter LC3-II accumulation, and showed the same Bafilomycin A1-induced LC3-II accumulation as vehicle-treated cells.
Did not impair DQ-BSA-based lysosomal proteolysis, indicating no change in lysosomal degradation capacity.
Chemical Information
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CAS. Nr. 3115333-82-6
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Molecular Weight 931.05
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Formel C46H51FN14O5S
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SMILES
O=C(NCCCOCCCCOCCCNC1=NC=C(C#CC2=CC=C(C3=CN4C=C(CO)C=CC4=N3)N=C2)C=N1)[C@@H](NC(C)=O)CSC5=NC6=C(N)N=C(N)N=C6N5CC7=CC=C(F)C=C7
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
MRL828 Related Classifications
HY-176130 Related Classifications
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