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Submit ReviewPYR 41 is a cell-permeable, irreversible ubiquitin-activating enzyme (E1) inhibitor (IC50 < 10 μM). Blocks ubiquitination and prevents ubiquitin-mediated proteasomal degradation. Inhibits NF-κB activation, blocks degradation of p53, increases p21 levels and induces apoptosis in vitro. Also causes an increase in sumoylation of proteins.
分子量 | 371.3 |
公式 | C17H13N3O7 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 418805-02-4 |
PubChem ID | 2856906 |
InChI Key | ARGIPZKQJGFSGQ-UHFFFAOYSA-N |
Smiles | CCOC(=O)C1=CC=C(C=C1)N1NC(=O)C(=CC2=CC=C(O2)[N+]([O-])=O)C1=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 37.13 | 100 |
以下数据基于产品分子量 371.3。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.69 mL | 13.47 mL | 26.93 mL |
5 mM | 0.54 mL | 2.69 mL | 5.39 mL |
10 mM | 0.27 mL | 1.35 mL | 2.69 mL |
50 mM | 0.05 mL | 0.27 mL | 0.54 mL |
参考文献是支持产品生物活性的出版物。
Yang et al (2007) Inhibitors of ubiquitin-activating enzyme (E1), a new class of potential cancer therapeutics. Cancer Res. 67 9472 PMID: 17909057
Mi et al (2009) Cancer preventative isothiocyanates induce selective degradation of cellular α- and β-tubulins by proteasomes. J.Biol.Chem. 284 17039 PMID: 19339240
Brahemi et al (2010) Homology modelling of human E1 ubiquitin activating enzyme. Lett.Drug Des.Discov. 7 57 PMID: 20396627
If you know of a relevant reference for PYR 41, please let us know.
关键词: PYR 41, PYR 41 supplier, PYR41, ubiquitin-activating, enzyme, E1, inhibitors, inhibits, ubiquitylation, post-translational, modifications, proteasomal, proteasome, sumoylation, sumo, ubiquitin, Ubiquitin-activating, Enzyme, Post-translational, Modifications, 2978, Tocris Bioscience
平均评分: 5 (Based on 1 Review.)
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Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.