Biological Activity
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
| 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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 37.13 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 371.3. Batch specific molecular weights may vary from batch to batch due to solvent 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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References
References are publications that support the products' biological activity.
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
Keywords: PYR 41, supplier, PYR41, ubiquitin-activating, enzyme, E1, inhibitors, inhibits, ubiquitylation, post-translational, modifications, proteasomal, proteasome, sumoylation, sumo, ubiquitin, Ubiquitin-activating, Enzyme, E1, Post-translational, Modifications, Ubiquitin-activating, Enzyme, E1, Tocris Bioscience
