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662210 USP14 Inhibitor, IU1 - Calbiochem

The USP14 Inhibitor, IU1 controls the biological activity of USP14. This small molecule/inhibitor is primarily used for Cell Structure applications.

USP14 Inhibitor, IU1 - Calbiochem: SDB (Sicherheitsdatenblätter), Analysenzertifikate und Qualitätszertifikate, Dossiers, Broschüren und andere verfügbare Dokumente.

Synonyme: 1-(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

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      Übersicht

      Replacement Information

      Key Spec Table

      Empirical Formula
      C₁₈H₂₁FN₂O
      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
      Global Trade Item Number
      Bestellnummer GTIN
      662210 0

      Documentation

      USP14 Inhibitor, IU1 - Calbiochem SDB

      Titel

      Sicherheitsdatenblatt (SDB) 

      USP14 Inhibitor, IU1 - Calbiochem Analysenzertifikate

      TitelChargennummer
      662210

      Literatur

      Übersicht
      Lee, B.H., et al. 2010. Nature 467, 179.

      Broschüre

      Titel
      New Products: Volume 3, 2012
      Datenblatt

      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 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 6 months at -20°C.
      Toxicity Regulatory Review
      ReferencesLee, B.H., et al. 2010. Nature 467, 179.