Quality Level
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
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.
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral
保管分類
11 - Combustible Solids
flash_point_f
Not applicable
flash_point_c
Not applicable
適用法令
試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。
SML4293-VAR: + SML4293-25MG: + SML4293-5MG: + SML4293-BULK:
jan
ライフサイエンス、有機合成、材料科学、クロマトグラフィー、分析など、あらゆる分野の研究に経験のあるメンバーがおります。.
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