662142 DUB Inhibitor VI, P22077 - Calbiochem

662142
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₂H₇F₂NO₃S₂

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662142-25MG
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      Glass bottle 25 mg
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      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

      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 +2°C to +8°C
      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.
      Toxicity Standard Handling
      ReferencesAltun, M., et al. 2011. Chem. Biol. 18, 1401.
      Tian, X., et al. 2011. Assay Drug Dev. Technol. 9, 165.