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PYR 41

Cat. No. 2978

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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.

Resources

Certificate of Analysis / Safety Data Sheet

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Safety Data Sheet: View Safety Data Sheet

References

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, supplier, PYR41, ubiquitin-activating, enzyme, E1, inhibitors, ubiquitylation, post-translational, modifications, proteasomal, proteasome, sumoylation, sumo, ubiquitin