Cat. No. 2978
Chemical Name: 4-[4-[(5-Nitro-2-furanyl)methylene]
Biological ActivityCell-permeable, irreversible ubiquitin-activating enzyme (E1) inhibitor (IC50 < 10 μM). Blocks ubiquitylation 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.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
Brahemi et al (2010) Homology modelling of human E1 ubiquitin activating enzyme. Lett.Drug Des.Discov. 7 57. PMID: 20396627.
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.
Yang et al (2007) Inhibitors of ubiquitin-activating enzyme (E1), a new class of potential cancer therapeutics. Cancer Res. 67 9472. PMID: 17909057.
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Keywords: PYR 41, supplier, PYR41, ubiquitin-activating, enzyme, E1, inhibitors, inhibits, ubiquitylation, post-translational, modifications, proteasomal, proteasome, sumoylation, sumo, ubiquitin, Tocris Bioscience, Ubiquitin-activating Enzyme E1 Inhibitor products
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