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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).

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 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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Overview

Key Spec Table

CAS #Empirical Formula
916232-21-8C₂₈H₁₉FN₂O₄

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      		 Glass bottle 10 mg
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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
      Biological Information
      Primary Targetphosphorylated IκBα
      Purity≥97% by HPLC
      Physicochemical Information
      Cell permeableY
      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
      Global Trade Item Number
      Catalogue Number GTIN
      5.30588.0001 04055977260939