MTK458

SKU: orb2900567

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.

Key Properties

• CAS Number: 2499962-58-0
• MW: 332.32
• Purity: >98% (HPLC)
• Formula: C₁₇H₁₅F₃N₄
• SMILES: N(C1=C2C(NC(C(F)(F)F)=C2)=NC=N1)[C@H]3C=4C(CCC3)=CC=CC4
• Target: PTEN
• Solubility: In Vitro: DMSO : 100 mg/mL (300.91 mM; Ultrasonic )

Bioactivity

• In Vivo:
  Animal model: Stratum of mice injected with α-synuclein preformed fibrils (PFFs). 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. 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.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

PTEN