- 商品介绍
- 规格参数
- 包装参数
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.
| Quality Segment | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | -10 to -25°C |
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¥ 2622.09
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¥ 4173.75
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¥ 3372.68
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¥ 3290.05
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¥ 4011.97
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¥ 3404.94
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¥ 954.17
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¥ 5804.96
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