Biological Activity
Selective inhibitor of ubiquitin-specific protease (USP) 7 (IC50 = 4.2 μM). Displays little-to-no inhibition of other USP variants or proteases such as caspase, cathepsins and serine proteases; exhibits some activity at USP47. Induces elevated p53 and apoptosis in cancer cell lines; displays antiangiogenic activity in vivo.
Technical Data
| M. Wt | 348.22 |
| Formula | C12H7Cl2NO3S2 |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 882257-11-6 |
| PubChem ID | 2819993 |
| InChI Key | LKZLGMAAKNEGCH-UHFFFAOYSA-N |
| Smiles | CC(=O)C1=CC(=C(SC2=CC=CC(Cl)=C2Cl)S1)[N+]([O-])=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 | 3.48 | 10 |
Preparing Stock Solutions
The following data is based on the product molecular weight 348.22. 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 | 2.87 mL | 14.36 mL | 28.72 mL |
| 5 mM | 0.57 mL | 2.87 mL | 5.74 mL |
| 10 mM | 0.29 mL | 1.44 mL | 2.87 mL |
| 50 mM | 0.06 mL | 0.29 mL | 0.57 mL |
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References
References are publications that support the products' biological activity.
Weinstock et al (2012) Selective dual inhibitors of the cancer-related deubiquitylating proteases USP7 and USP47. J.Med.Chem. 3 789 PMID:
Chauhan et al (2012) A small molecule inhibitor of ubiquitin-specific protease-7 induces apoptosis in multiple myeloma cells and overcomes bortezomib resistance. Cancer Cell. 22 345 PMID: 22975377
Keywords: P005091, supplier, ubiquitin-specific, protease, USP7, inhibitors, inhibits, antiangiogenesis, antiangiogenic, apoptosis, p53, Antiangiogenics, Deubiquitinating, Enzymes, Deubiquitinating, Enzymes, Tocris Bioscience
