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662143 DUB Inhibitor XI

662143
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₈H₁₁Cl₂N₃O₃S₃

Products

Catalog NumberPackaging Qty/Pack
662143-10MG Glass bottle 10 mg
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
Catalog 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.