PYR 41

• Supplier: Tocris Bioscience
• Catalog: 2954
• Prices: $205.00, $845.00
• Sizes: 10 mg, 50 mg
• Function Type: Inhibitor
• Cas Number: 418805-02-4
• Chemical Name: 4-[4-[(5-Nitro-2-furanyl)methylene]-3,5-dioxo-1-pyrazolidinyl]benzoicacidethylester
• Formula: C17H13N3O7
• Molecular Weight: 371.3
• Purity: >98 %
• Description: Cell-permeable, irreversible ubiquitin-activating enzyme (E1) inhibitor (IC 50 < 10 μ M). Blocks ubiquitylation and prevents ubiquitin-mediated proteasomal degradation. Inhibits NF- κ B activation, blocks degradation of p53, increases p21 levels and induces apoptosis in vitro . Also causes an increase in sumoylation of proteins.

Product References

Inhibitors of ubiquitin-activating enzyme (E1), a new class of potential cancer - Inhibitors of ubiquitin-activating enzyme (E1), a new class of potential cancer

Yang Y, Kitagaki J, Dai RM, Tsai YC, Lorick KL, Ludwig RL, Pierre SA, Jensen JP, Davydov IV, Oberoi P, Li CC, Kenten JH, Beutler JA, Vousden KH, Weissman AM. Cancer Res. 2007 Oct 1;67(19):9472-81.

Cancer preventive isothiocyanates induce selective degradation of cellular alpha- - Cancer preventive isothiocyanates induce selective degradation of cellular alpha-

Mi L, Gan N, Cheema A, Dakshanamurthy S, Wang X, Yang DC, Chung FL. J Biol Chem. 2009 Jun 19;284(25):17039-51.

Homology Modelling of Human E1 Ubiquitin Activating Enzyme. - Homology Modelling of Human E1 Ubiquitin Activating Enzyme.

Brahemi G, Burger AM, Westwell AD, Brancale A. Lett Drug Des Discov. 2010 Jan 1;7(1):57-62.