BIO-2007817

Name: BIO-2007817
Brand: SIGMA

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

Synonym(s):

(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

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About This Item

Empirical Formula (Hill Notation):

C₃₂H₃₆N₆O₃

Molecular Weight:

552.67

Assay:

≥98% (HPLC)

Form:

powder

Quality level:

100

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Properties

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

-10 to -25°C

Description

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.