SML4293

BIO-2007817

≥98% (HPLC), powder, Parkin E3 ligase modulator

• Synonym(e): (S)-1-((R)-6-Isopropyl-3-(4-(1,2,3,4-tetrahydroquinoline-1-carbonyl)phenyl)-6,7-dihydropyrazolo[1,5-a]pyrazin-5(4H)-yl)-2-methoxy-2-(1-methyl-1H-pyrazol-4-yl)ethan-1-one, Parkin Activation Modulator BIO-2007817, BIO2007817, BIO 2007817
• Empirische Formel (Hill-System): C₃₂H₃₆N₆O₃
• Molekulargewicht: 552.67
• UNSPSC Code: 12352203
• Assay: ≥98% (HPLC)
• Form: powder

Eigenschaften

• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: -10 to -25°C

Beschreibung

General description

BIO-2007817 is a small-molecule compound identified as a positive allosteric modulator (PAM) of the Parkin E3 ubiquitin ligase. This compound belongs to the tetrahydropyrazolo-pyrazine class and has been shown to significantly enhance the activity of wildtype Parkin.

Application

BIO-2007817 has been used in ubiquitination assays and isothermal titration calorimetry to study the mechanism of activation of Parkin.

Biochem/physiol Actions

BIO-2007817 enhances Parkin activation by facilitating the interaction between the RING0 domain of Parkin and phospho-ubiquitin (pUb). It binds selectively to Parkin with an EC50 of 150 nM, acting as a molecular glue between Parkin and pUb, promoting autoubiquitination and the ubiquitination of mitochondrial proteins like mitofusin-2 (Mfn2). However, BIO-2007817 does not promote Parkin translocation to depolarized mitochondria in HeLa cells nor enhance mitophagy in MitoQC SH-SY5Y cell lines. Despite this, it shows no significant off-target effects and partially rescues the activity of disease-associated Parkin mutants.

Sicherheitshinweise

• Piktogramme: GHS07
• Signalwort: Warning
• Gefahrencodes: H302
• Sicherheitshinweise: P264 - P270 - P301 + P312 - P501
• Hazard Classifications: Acute Tox. 4 Oral
• Lagerklasse: 11 - Combustible Solids
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable