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Biological Activity for P 22077
P 22077 is an 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 for P 22077
Technical Data for P 22077
|Storage||Store at +4°C|
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 P 22077
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for P 22077
The following data is based on the product molecular weight 315.32. 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||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|
References for P 22077
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for P 22077, please let us know.
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Keywords: P 22077, P 22077 supplier, P22077, inhibitors, inhibits, ubiquitin-specific, proteases, USP7, DUB, HDM2, claspin, ubiquitin, deubiquitination, anticancer, hausp, Deubiquitinating, Enzymes, 4485, Tocris Bioscience
3 Citations for P 22077
Citations are publications that use Tocris products. Selected citations for P 22077 include:
Lecona et al (2016) USP7 is a SUMO deubiquitinase essential for DNA replication. Nat Struct Mol Biol 23 270 PMID: 26950370
Ji et al (2019) USP7 inhibits Wnt/β-catenin signaling through promoting stabilization of Axin. Nat Commun 10 4184 PMID: 31519875
Lecona et al (2015) USP7 cooperates with SCML2 to regulate the activity of PRC1. Pharmacol Res Perspect 35 1157 PMID: 25605328
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Reviews for P 22077
Average Rating: 4 (Based on 2 Reviews.)
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P22077 was seen to induce (tumor) cell death with EC50 values in the low micromolar range. P22077 inhibition exhibited changes in ubiquitylated protein levels that are distinct from the broad specificity inhibitor.
HEK293T cells stably expressing the STF-Luc reporter were pretreated with increasing amounts of USP7 inhibitors P22077