A part of MilliporeSigma

662142 | DUB Inhibitor VI, P22077 - Calbiochem

662142
Price could not be retrieved
Minimum Quantity needs to be mulitiple of
Upon Order Completion More Information
You Saved ()
 
Request Pricing
Limited AvailabilityLimited Availability
Stocked 
Discontinued
Limited Quantities Available
Available
    Remaining : Will advise
      Remaining : Will advise
      Will advise
      Contact Customer Service
      View Pricing & Availability
      Click To Print This Page

      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₂H₇F₂NO₃S₂

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      662142-25MG
      Retrieving availability...
      Limited AvailabilityLimited Availability
      Stocked 
      Discontinued
      Limited Quantities Available
      Available
        Remaining : Will advise
          Remaining : Will advise
          Will advise
          Contact Customer Service

          Glass bottle 25 mg
          Retrieving price...
          Price could not be retrieved
          Minimum Quantity needs to be mulitiple of
          Upon Order Completion More Information
          You Saved ()
           
          Request Pricing
          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 Image
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          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 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.