Catalog Number: 2978
Chemical Name: 4-[4-[(5-Nitro-2-furanyl)methylene]-3,5-dioxo-1-pyrazolidinyl]benzoic acid ethyl ester
Biological Activity
Cell-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.
Technical Data
  • M.Wt:
    371.3
  • Formula:
    C17H13N3O7
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at -20°C
  • CAS No:
    418805-02-4
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.
Background References
  1. Cancer preventative isothiocyanates induce selective degradation of cellular α- and β-tubulins by proteasomes.
    Mi et al.
    J.Biol.Chem., 2009;284:17039
  2. Homology modelling of human E1 ubiquitin activating enzyme.
    Brahemi et al.
    Lett.Drug Des.Discov., 2010;7:57
  3. Inhibitors of ubiquitin-activating enzyme (E1), a new class of potential cancer therapeutics.
    Yang et al.
    Cancer Res., 2007;67:9472
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