662210 USP14 Inhibitor, IU1 - Calbiochem

662210
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₈H₂₁FN₂O

Pricing & Availability

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662210-10MG
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      Glass bottle 10 mg
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      Description
      OverviewA cell-permeable pyrrolylpyrrolidinyl-ethanone that inhibits the proteasome association-dependent USP14 deubiquitinase (DUB) activity in a reversible manner (IC50 = 4.7 µM against Ub-AMC hydrolysis), exhibiting little or no activity toward 8 other DUBs. Shown to downregulate tau, TDP-43, ATXN3, GFAP, and free Ub levels in MEF cultures in a dose- (25 to 100 µM), time-, and USP14-dependent manner. USP14-catalyzed trimming of protein surface polyubiquitin chains rescues proteasome-bound proteins from proteolytic degradation and thereby prevents the depletion of free ubiquitin pool in cells. Comparing to b-AP15 (Cat. No. 662140), IU1 does not inhibit UCH37/UCH-L5 (IC50 = 700 µM).
      Catalogue Number662210
      Brand Family Calbiochem®
      Synonyms1-(1-(4-Fluorophenyl)-2,5-dimethyl-1H-pyrrol-3-yl)-2-(pyrrolidin-1-yl)ethanone, 1-(1-(4-Fluorophenyl)-2,5-dimethylpyrrol-3-yl)-2-pyrrolidin-1-ylethanone, Ubiquitin Specific Protease 14 Inhibitor, DUB Inhibitor IX
      References
      ReferencesLee, B.H., et al. 2010. Nature 467, 179.
      Product Information
      FormBeige solid
      Hill FormulaC₁₈H₂₁FN₂O
      Chemical formulaC₁₈H₂₁FN₂O
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥90% 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 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Regulatory Review
      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

      USP14 Inhibitor, IU1 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      USP14 Inhibitor, IU1 - Calbiochem Certificates of Analysis

      TitleLot Number
      662210

      References

      Reference overview
      Lee, B.H., et al. 2010. Nature 467, 179.
      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.

      Revision15-July-2019 JSW
      Synonyms1-(1-(4-Fluorophenyl)-2,5-dimethyl-1H-pyrrol-3-yl)-2-(pyrrolidin-1-yl)ethanone, 1-(1-(4-Fluorophenyl)-2,5-dimethylpyrrol-3-yl)-2-pyrrolidin-1-ylethanone, Ubiquitin Specific Protease 14 Inhibitor, DUB Inhibitor IX
      DescriptionA cell-permeable pyrrolylpyrrolidinyl-ethanone that inhibits the proteasome association-dependent USP14 deubiquitinase (DUB) activity in a reversible manner (IC50 = 4.7 µM against Ub-AMC hydrolysis), likely by targeting USP14 active site thiol, while exhibiting little or no activity toward 8 other DUBs (<10% inhibition of IsoT, UCH37/UCH-L5, BAP1, UCH-L1, UCH-L3, USP2, USP7, and USP15 at 17 µM). Shown to downregulate tau, TDP-43, ATXN3, GFAP, and free Ub levels in MEF cultures in a dose- (25 to 100 µM), time-, and USP14-dependent manner. Effectively protects HEK293 cells from menadione toxicity (90% vs. 40% viability after 4 h 100 µM menadione treatment, respectively, with or without 50 µM IU1 pretreatment) by reducing the built-up of oxidized proteins. USP14-catalyzed trimming of protein surface polyubiquitin chains rescues proteasome-bound proteins from proteolytic degradation and thereby prevents the depletion of free ubiquitin pool in cells. Comparing to b-AP15 (Cat. No. 662140), IU1 does not inhibit UCH37/UCH-L5 (IC50 = 700 µM).
      FormBeige solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₈H₂₁FN₂O
      Structure formulaStructure formula
      Purity≥90% 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 Regulatory Review
      ReferencesLee, B.H., et al. 2010. Nature 467, 179.