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Submit ReviewPYR 41
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)
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 |
| InChI Key | ARGIPZKQJGFSGQ-UHFFFAOYSA-N |
| 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 | |
|---|---|---|---|
| Solubility | |||
| 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.
| 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
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.
Literature in this Area
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