Biological Activity
Inhibitor of 19S regulatory particle associated deubiquitinating enzymes (DUBs), UCHL5 and USP14. Shows minimal inhibition of UCHL-1, UCHL-3, USP2, USP7, USP, BAP1 and proteasome activity. Induces apoptosis by cathepsin D-dependent caspase-cleavage (IC50 = 0.5 μM). Displays antitumor activity in vivo.
Technical Data
| M. Wt | 419.39 |
| Formula | C22H17N3O6 |
| Storage | Store at +4°C |
| Purity | ≥97% (HPLC) |
| CAS Number | 1009817-63-3 |
| PubChem ID | 5351435 |
| InChI Key | GFARQYQBWJLZMW-JYFOCSDGSA-N |
| Smiles | O=C(/C(CN(C(C=C)=O)C3)=C/C2=CC=C([N+]([O-])=O)C=C2)/C3=C/C1=CC=C([N+]([O-])=O)C=C1 |
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 | 41.94 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 419.39. 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 | 2.38 mL | 11.92 mL | 23.84 mL |
| 5 mM | 0.48 mL | 2.38 mL | 4.77 mL |
| 10 mM | 0.24 mL | 1.19 mL | 2.38 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.48 mL |
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References
References are publications that support the products' biological activity.
Berndtsson et al (2009) Induction of the lysosomal apoptosis pathway by inhibitors of the ubiquitin-proteasome system. Int.J.Cancer 124 1463 PMID: 19089926
D'Arcy et al (2011) Inhibition of proteasome deubiquitinating activity as a new cancer therapy. Nat.Med. 17 1636 PMID: 22057347
Keywords: NSC 687852, supplier, NSC687852, 19S, regulatory, particle, associated, deubiquitylating, enzymes, DUBs, apoptosis, UCHL5, USP14, cathepsin, D, dependent, caspase, cleavage, antitumor, b-AP15, Deubiquitinating, Enzymes, Apoptosis, Inducers, Deubiquitinating, Enzymes, Tocris Bioscience
