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530588 IκB Ubiquitination Inhibitor, GS143 - CAS 916232-21-8 - Calbiochem

A cell-permeable, selective inhibitor of E3 ligase complex SCFβTrCP1-mediated ubiquitination of phosphorylated IκBα (IC₅₀ = 5.2 µM).

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Synonymes: 4-(3-Benzyl-4-(5-(2-fluoro-phenyl)-furan-2-ylmethylene)-5-oxo-4,5-dihydropyrazol-1-yl)-benzoic acid, 4-(3-Benzyl-4-((5-(2-fluorophenyl)furan-2-yl)methylene)-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid, GS 143

Primary Target: phosphorylated IκBα
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530588
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Tableau de caractéristiques principal

CAS #Empirical Formula
916232-21-8C₂₈H₁₉FN₂O₄

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      Description
      OverviewA cell-permeable trisubstituted oxo-dihydropyrazolyl-benzoic acid that selectively inhibits the E3 ligase complex SCFβTrCP1-mediated ubiquitination of phosphorylated IκBα (IC50 = 5.2 µM), displaying little inhibitory potency against IKKβ-catalyzed IκBα phosphorylation, MDM2-mediated p53 ubiquitination, or the protease activities of cathepsin B, chymotrypsin, 20S & 26S proteasome (IC50 >100 µM). Effectively inhibits TNFα- and LPS-stimulated NF-κB transcription in HEK293, HT-29, and THP-1 cultures (IC50 from 2.1 to 10.5 µM). Intranasal administration (32 µg/20 µL/mouse) among OVA-sensitized mice 2 h prior to OVA challenge via inhalation greatly suppress NF-κB activation in lung tissue and airway inflammation in vivo. GS143 most likely prevents SCFβTrCP1 from interacting with phosphorylated IκBα without inhibiting SCFβTrCP1 E3 ligase activity directly.
      Catalogue Number530588
      Brand Family Calbiochem®
      Synonyms4-(3-Benzyl-4-(5-(2-fluoro-phenyl)-furan-2-ylmethylene)-5-oxo-4,5-dihydropyrazol-1-yl)-benzoic acid, 4-(3-Benzyl-4-((5-(2-fluorophenyl)furan-2-yl)methylene)-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid, GS 143
      References
      ReferencesHirose, K., et al. 2008. Biochem. Biophys. Res. Commun. 374, 507.
      Nakajima, H., et al. 2008. Biochem. Biophys. Res. Commun. 368, 1007.
      Product Information
      CAS number916232-21-8
      FormDark red powder
      Hill FormulaC₂₈H₁₉FN₂O₄
      Chemical formulaC₂₈H₁₉FN₂O₄
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary Targetphosphorylated IκBα
      Purity≥97% 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
      Référence GTIN
      5.30588.0001 04055977260939

      Documentation

      IκB Ubiquitination Inhibitor, GS143 - CAS 916232-21-8 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Références bibliographiques

      Aperçu de la référence bibliographique
      Hirose, K., et al. 2008. Biochem. Biophys. Res. Commun. 374, 507.
      Nakajima, H., et al. 2008. Biochem. Biophys. Res. Commun. 368, 1007.
      Fiche technique

      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.

      Revision13-June-2014 JSW
      Synonyms4-(3-Benzyl-4-(5-(2-fluoro-phenyl)-furan-2-ylmethylene)-5-oxo-4,5-dihydropyrazol-1-yl)-benzoic acid, 4-(3-Benzyl-4-((5-(2-fluorophenyl)furan-2-yl)methylene)-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid, GS 143
      DescriptionA cell-permeable trisubstituted oxo-dihydropyrazolyl-benzoic acid that selectively inhibits the E3 ligase complex SCFβTrCP1-mediated ubiquitination of phosphorylated IκBα (IC50 = 5.2 µM), displaying little inhibitory potency against IKKβ-catalyzed IκBα phosphorylation, MDM2-mediated p53 ubiquitination, or the protease activities of cathepsin B, chymotrypsin, 20S & 26S proteasome (IC50 >100 µM). Cellular IκBα degradation blockage by GS143 treatment (complete inhibition against TNFα-induced degradation with 30 min 20 µM drug pretreatment in in HeLa S3 and HT29 cultures) effectively inhibits TNFα- and LPS-stimulated NF-κB transcription in HEK293, HT-29, and THP-1 cultures (IC50 from 2.1 to 10.5 µM). Intranasal administration (32 µg/20 µL/mouse) among OVA-sensitized mice 2 h prior to OVA challenge via inhalation greatly suppress OVA challenge-induced NF-κB activation in lung tissue (> 90% inhibition of nuclear NF-κB p65 DNA-binding activity 2 h post challenge) and airway inflammation (>80% reduction in eosinophils & lymphocytes in BALF 48 h post challenge) in vivo. GS143 most likely prevents SCFβTrCP1 from interacting with phosphorylated IκBα without inhibiting SCFβTrCP1 E3 ligase activity directly, as no apparent accumulation of another known SCFβTrCP1 substrate β-catenin is seen in HeLa S3 cells upon GS143 treatment (up to 20 µM for 3 h).
      FormDark red powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number916232-21-8
      Chemical formulaC₂₈H₁₉FN₂O₄
      Structure formulaStructure formula
      Purity≥97% by HPLC
      SolubilityDMSO (25 mg/ml). 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
      ReferencesHirose, K., et al. 2008. Biochem. Biophys. Res. Commun. 374, 507.
      Nakajima, H., et al. 2008. Biochem. Biophys. Res. Commun. 368, 1007.