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662143 DUB Inhibitor XI

662143
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₁₈H₁₁Cl₂N₃O₃S₃

Pricing & Availability

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662143-10MG
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      Description
      OverviewA cell-permeable dichloropyridinylthio-thiophenecarboxamide that is more potent than DUB Inhibitor VI, P22077 (Cat. No. 662142) as a dual inhibitor against USP7 (IC50 = 0.42 vs. 8.0 µM with respective inhibitor) and USP47 (IC50 = 1.0 vs. 8.7 µM with respective inhibitor), while exhibiting comparable cytotoxicity toward HCT-116 (CC50 = 7.6 vs. 7.8 µM with respective inhibitor) by upregulating cellular p21 and p53 protein levels in a time-dependent manner. Displays little potency against USP2, USP5, USP8, USP21 USP28, cathepsin B, caspase-3, calpain-1, or 20S proteasome chymotrypsin-like activity (IC50 >31.6 µM).
      Catalogue Number662143
      Brand Family Calbiochem®
      SynonymsUSP7 Inhibitor III, 4-Cyano-5-((3,5-dichloropyridin-4-yl)thio)-N-(4-(methylsulfonyl)phenyl)thiophene-2-carboxamide, USP47 Inhibitor III
      References
      ReferencesWeinstock, J., et al. 2012. ACS Med. Chem. Lett. 3, 789.
      Product Information
      FormPale yellow solid
      Hill FormulaC₁₈H₁₁Cl₂N₃O₃S₃
      Chemical formulaC₁₈H₁₁Cl₂N₃O₃S₃
      ReversibleN
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetUSP7/47
      Primary Target IC<sub>50</sub>0.42 and 1.0 µ
      Purity≥95% by HPLC
      Physicochemical Information
      Cell permeableY
      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 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Catalogue Number GTIN
      662143-10MG 04055977261264

      Documentation

      DUB Inhibitor XI Certificates of Analysis

      TitleLot Number
      662143

      References

      Reference overview
      Weinstock, J., et al. 2012. ACS Med. Chem. Lett. 3, 789.
      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.

      Revision21-March-2014 JSW
      SynonymsUSP7 Inhibitor III, 4-Cyano-5-((3,5-dichloropyridin-4-yl)thio)-N-(4-(methylsulfonyl)phenyl)thiophene-2-carboxamide, USP47 Inhibitor III
      DescriptionA cell-permeable dichloropyridinylthio-thiophenecarboxamide that is more potent than DUB Inhibitor VI, P22077 (Cat. No. 662142) as a dual inhibitor against USP7 (IC50 = 0.42 vs. 8.0 µM with respective inhibitor) and USP47 (IC50 = 1.0 vs. 8.7 µM with respective inhibitor), while exhibiting comparable cytotoxicity toward HCT-116 (CC50 = 7.6 vs. 7.8 µM with respective inhibitor) by upregulating cellular p21 and p53 protein levels in a time-dependent manner. Displays little potency against USP2, USP5, USP8, USP21 USP28, cathepsin B, caspase-3, calpain-1, or 20S proteasome chymotrypsin-like activity (IC50 >31.6 µM).
      FormPale yellow solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₈H₁₁Cl₂N₃O₃S₃
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO. Use only fresh DMSO for reconstitution.
      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 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesWeinstock, J., et al. 2012. ACS Med. Chem. Lett. 3, 789.