PYR 41
Chemical Name: 4-[4-[(5-Nitro-2-furanyl)methylene]-3,5-dioxo-1-pyrazolidinyl]benzoic acid ethyl ester
Purity: ≥98%
Biological Activity
PYR 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.Technical Data
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.
Background References
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Lipid-regulated degradation of HMG-CoA reductase and Insig-1 through distinct mechanisms in insect cells.
Faulkner, Rebecca, Nguyen, Andrew D, Jo, Youngah, DeBose-Boyd, Russell
J Lipid Res, 2013;54(4):1011-22. -
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.
J.Biol.Chem., 2009;284:17039 -
Homology modelling of human E1 ubiquitin activating enzyme.
Brahemi et al.
Lett.Drug Des.Discov., 2010;7:57
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