Chemical Name: 4-[4-[(5-Nitro-2-furanyl)methylene]-3,5-dioxo-1-pyrazolidinyl]benzoic acid ethyl ester
Biological ActivityCell-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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Inhibitors of ubiquitin-activating enzyme (E1), a new class of potential cancer therapeutics.
Yang et al.
Cancer Res., 2007;67:9472
Cancer preventative isothiocyanates induce selective degradation of cellular α- and β-tubulins by proteasomes.
Mi et al.
Homology modelling of human E1 ubiquitin activating enzyme.
Brahemi et al.
Lett.Drug Des.Discov., 2010;7:57
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This compound worked very well for our experiments in 5 uM concentration.