P 22077

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Cat.No. 4485 - P 22077 | C12H7F2NO3S2 | CAS No. 1247819-59-5
Description: USP7 inhibitor
Chemical Name: 1-[5-[(2,4-Difluorophenyl)thio]-4-nitro-2-thienyl]-ethanone
Purity: ≥99% (HPLC)
Datasheet
Citations (2)
Reviews
Literature

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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References

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


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View Related Products by Product Action

View all Deubiquitinating Enzyme Inhibitors

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

2 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

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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