P 22077

Name: P 22077
Brand: Tocris Bioscience
SKU: 4485
Rating: 4 (2 reviews)

Cat. No. 4485 5 Citations 2 Reviews Submit a Review Datasheet / COA / SDS

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Description: USP7 inhibitor

Chemical Name: 1-[5-[(2,4-Difluorophenyl)thio]-4-nitro-2-thienyl]-ethanone

Purity: ≥99% (HPLC)

Datasheet

Citations (5)

Reviews (2)

Biological Activity Technical Data Solubility Calculators Datasheets References

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

P 22077 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.

Technical Data for P 22077

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.

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
Solubility
Solubility	DMSO	31.53	100

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

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Product Datasheets for P 22077

Certificate of Analysis / Product Datasheet

Safety Datasheet

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

5 Citations for P 22077

Citations are publications that use Tocris products. Selected citations for P 22077 include:

Ting-Xin et al (2021) Global feather orientations changed by electric current. iScience 24 102671 PMID: 34179734

Oscar et al (2021) USP7 and VCPFAF1 define the SUMO/Ubiquitin landscape at the DNA replication fork. Cell Rep 37 109819 PMID: 34644576

Ji et al (2019) USP7 inhibits Wnt/β-catenin signaling through promoting stabilization of Axin. Nat Commun 10 4184 PMID: 31519875

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

Do you know of a great paper that uses P 22077 from Tocris? Please let us know.

Reviews for P 22077

Average Rating: 4 (Based on 2 Reviews.)

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P22077 was seen to induce tumor cell death.

By Anonymous on 12/14/2019

Species: Human

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.

USP7 inhibitors 2 (P22077).

By Anonymous on 12/10/2019

Assay Type: In Vitro