Biological Activity
Inhibitor of ubiquitin-specific protease (USP) 7 (EC50 = 8.6 μM); also inhibits the closely related deubiquitinase (DUB) USP47. Demonstrates downstream inhibition of HDM2 and claspin in vitro. Inhibits USP7-mediated p53 deubiquitination. Blocks deubiquitination of Tip60 (KAT5) histone lysine acetyltransferase.
Compound Libraries
P 22077 is also offered as part of the Tocriscreen Plus and Tocriscreen Epigenetics Toolbox. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 315.32 |
| Formula | C12H7F2NO3S2 |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 1247819-59-5 |
| PubChem ID | 46931953 |
| InChI Key | RMAMGGNACJHXHO-UHFFFAOYSA-N |
| Smiles | CC(C1=CC([N+]([O-])=O)=C(SC2=CC=C(F)C=C2F)S1)=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 | 31.53 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 315.32. 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 | 3.17 mL | 15.86 mL | 31.71 mL |
| 5 mM | 0.63 mL | 3.17 mL | 6.34 mL |
| 10 mM | 0.32 mL | 1.59 mL | 3.17 mL |
| 50 mM | 0.06 mL | 0.32 mL | 0.63 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Loch et al (2011) Deubiquitylase, deSUMOylase, and deISGylase activity microarrays for assay of substrate preference and functional modifiers. Mol.Cell.Proteomics 10 M100.002402 PMID: 20956615
Tian et al (2011) Characterization of selective ubiquitin and ubiquitin-like protease inhibitors using a fluorescence-based multiplex assay format. Assay Drug Dev.Technol. 9 165 PMID: 21133675
Altun et al (2011) Activity-based chemical proteomics accelerates inhibitor development for deubiquitylating enzymes. Chem.Biol. 18 1401 PMID: 22118674
Dar et al (2013) Deubiquitination of Tip60 by USP7 determines the activity of the p53-dependent apoptotic pathway. Mol.Cell Biol. 33 3309 PMID: 23775119
Keywords: P 22077, supplier, P22077, inhibitors, inhibits, ubiquitin-specific, proteases, USP7, DUB, HDM2, claspin, ubiquitin, deubiquitination, anticancer, hausp, Deubiquitinating, Enzymes, Deubiquitinating, Enzymes, Tocris Bioscience
