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662142 DUB Inhibitor VI, P22077 - Calbiochem

Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₂H₇F₂NO₃S₂

Products

Catalog NumberPackaging Qty/Pack
662142-25MG Glass bottle 25 mg
Description
OverviewA cell-permeable thiophenylethanone that is shown to inhibit USP7 and USP47 deubiquitinase activity (IC50 = 8.01 & 8.74 µM, respectively), while exhibiting much reduced affinity toward ATXN3, BAP1, and USP1, and displaying no inhibitory activity toward other known PR-619 (Cat. No. 662141) targets (IC50 >50 µM). Both P22077 and PR-619 are shown to increase overall protein polyubiquitination in HEK293T cells in a dose- and time-dependent manner (20 to 150 µM; 0.5 to 20 h), however PR619 treatment results in upregulation of both K48- and K63-linked, while P22077 exposure results in mainly enrichment of K48-linked polyUb chains.
Catalogue Number662142
Brand Family Calbiochem®
SynonymsUSP7 Inhibitor II, USP47 Inhibitor II, P022077, 1-(5-(2,4-Difluorophenylthio)-4-nitrothiophen-2-yl)ethanone
References
ReferencesAltun, M., et al. 2011. Chem. Biol. 18, 1401.
Tian, X., et al. 2011. Assay Drug Dev. Technol. 9, 165.
Product Information
FormOff-white solid
Hill FormulaC₁₂H₇F₂NO₃S₂
Chemical formulaC₁₂H₇F₂NO₃S₂
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥98% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Identification Number
Catalog Number GTIN
662142-25MG4055977261257

Documentation

DUB Inhibitor VI, P22077 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

DUB Inhibitor VI, P22077 - Calbiochem Certificates of Analysis

TitleLot Number
662142

References

Reference overview
Altun, M., et al. 2011. Chem. Biol. 18, 1401.
Tian, X., et al. 2011. Assay Drug Dev. Technol. 9, 165.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision27-July-2012 JSW
SynonymsUSP7 Inhibitor II, USP47 Inhibitor II, P022077, 1-(5-(2,4-Difluorophenylthio)-4-nitrothiophen-2-yl)ethanone
DescriptionA cell-permeable thiophenylethanone compound that acts a direct, reversible, and selective inhibitor of deubiquitylating enzymes (DUBs) USP7 and USP47 (IC50 = 8.01 & 8.74 µM, respectively). Exhibits only a minimal effect on other DUBs and proteases (>25 µM). Also shown to block UCH-L5 activity in HEK293T cell extracts, but not in intact cells. Stabilizes p53, HDM2, and p21 levels in HEK293T and HCT-116 cells and induces growth arrest (50% cytotoxicity concentration; CC50 = 16.6 and 7.83 µM).
Note: A pan-DUB selective inhibitor PR-619 (Cat. No. 662141) is also available.
FormOff-white solid
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₁₂H₇F₂NO₃S₂
Structure formulaStructure formula
Purity≥98% by HPLC
SolubilityDMSO (50 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity Standard Handling
ReferencesAltun, M., et al. 2011. Chem. Biol. 18, 1401.
Tian, X., et al. 2011. Assay Drug Dev. Technol. 9, 165.