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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.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 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.
|Concentration / Solvent Volume / Mass||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|
References are publications that support the biological activity of the product.
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
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Keywords: 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
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Literature in this Area
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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.