PYR 41

Pricing Availability   Qty
Description: Ubiquitin-activating enzyme (E1) inhibitor
Chemical Name: 4-[4-[(5-Nitro-2-furanyl)methylene]-3,5-dioxo-1-pyrazolidinyl]benzoic acid ethyl ester
Purity: ≥98% (HPLC)
Reviews (1)
Literature (3)

Biological Activity for PYR 41

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 for PYR 41

M. Wt 371.3
Formula C17H13N3O7
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 418805-02-4
PubChem ID 2856906
Smiles CCOC(=O)C1=CC=C(C=C1)N1NC(=O)C(=CC2=CC=C(O2)[N+]([O-])=O)C1=O

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.

Solubility Data for PYR 41

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 37.13 100

Preparing Stock Solutions for PYR 41

The following data is based on the product molecular weight 371.3. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.69 mL 13.47 mL 26.93 mL
5 mM 0.54 mL 2.69 mL 5.39 mL
10 mM 0.27 mL 1.35 mL 2.69 mL
50 mM 0.05 mL 0.27 mL 0.54 mL

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Product Datasheets for PYR 41

Certificate of Analysis / Product Datasheet
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References for PYR 41

References are publications that support the biological activity of the product.

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

If you know of a relevant reference for PYR 41, please let us know.

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Keywords: PYR 41, PYR 41 supplier, PYR41, ubiquitin-activating, enzyme, E1, inhibitors, inhibits, ubiquitylation, post-translational, modifications, proteasomal, proteasome, sumoylation, sumo, ubiquitin, Ubiquitin-activating, Enzyme, Post-translational, Modifications, 2978, Tocris Bioscience

Citations for PYR 41

Citations are publications that use Tocris products.

Currently there are no citations for PYR 41. Do you know of a great paper that uses PYR 41 from Tocris? Please let us know.

Reviews for PYR 41

Average Rating: 5 (Based on 1 Review.)

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proteasomal degradation inhibitor.
By Anonymous on 03/11/2020
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: Hepg2, Huh7

This compound worked very well for our experiments in 5 uM concentration.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Autophagy Scientific Review

Autophagy Scientific Review

Written by Patricia Boya and Patrice Codogno, this review summarizes the molecular mechanisms, physiology and pathology of autophagy. The role of autophagy in cell death and its links to disease are also discussed. Compounds available from Tocris are listed.

Autophagy Poster

Autophagy Poster

Autophagy is a cellular process used by cells for degradation and recycling. Written by Patricia Boya and Patrice Codogno, this poster summarizes the molecular machinery, physiology and pathology of autophagy. Compounds available from Tocris are listed.

Parkinson's Disease Poster

Parkinson's Disease Poster

Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.