662143 DUB Inhibitor XI

662143
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₈H₁₁Cl₂N₃O₃S₃

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      662143-10MG
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          Glass bottle 10 mg
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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®
          Synonyms4-Cyano-5-((3,5-dichloropyridin-4-yl)thio)-N-(4-(methylsulfonyl)phenyl)thiophene-2-carboxamide, USP7 Inhibitor III, 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
          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

          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
          Synonyms4-Cyano-5-((3,5-dichloropyridin-4-yl)thio)-N-(4-(methylsulfonyl)phenyl)thiophene-2-carboxamide, USP7 Inhibitor III, 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 +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 3 months at -20°C.
          Toxicity Standard Handling
          ReferencesWeinstock, J., et al. 2012. ACS Med. Chem. Lett. 3, 789.