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509374 Fn14 Antagonist, L524-0366 - CAS 951612-19-4 - Calbiochem

Specifically binds to the Fn14 surface (Kd = 7.12 mM) and suppresses TWEAK-induced glioma cell migration.

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Synonymes: Fibroblast Growth Factor-inducible 14 Antagonist; L5240366, THD Receptor Antagonist; TNF-like Weak Inducer of Apoptosis Receptor Antagonist, TWEAK Receptor Antagonist; TWEAK-Fn14 Interaction Inhibitor

Primary Target: fibroblast growth factor-inducible 14 (Fn14)
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509374
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Tableau de caractéristiques principal

CAS #Empirical Formula
951612-19-4C₁₃H₁₃ClN₄OS

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      Description
      OverviewA triazolyl-thiomorpholinyl-methanone compound that competes against TWEAK C-terminal/extracellular TNF homology domain (THD) for Fn14 binding (KD = 7.12 µM). Shown to completely inhibit 100 ng/mL sTWEAK-stimulated migration of T98G glioma cells at 10 µM concentration and is more potent against sTWEAK- than TNFα-induced NF-κB activation (IC50 = 7.8 vs. 31.03 µM, respectively, in reporter assays) without any apparent cytotoxicity up to 50 µM and 72 h in T98G cultures.
      Catalogue Number509374
      Brand Family Calbiochem®
      SynonymsFibroblast Growth Factor-inducible 14 Antagonist; L5240366, THD Receptor Antagonist; TNF-like Weak Inducer of Apoptosis Receptor Antagonist, TWEAK Receptor Antagonist; TWEAK-Fn14 Interaction Inhibitor
      References
      ReferencesDhruv, H., et al. 2013. J. Biol. Chem. 288, 32261.
      Product Information
      CAS number951612-19-4
      FormWhite powder
      Hill FormulaC₁₃H₁₃ClN₄OS
      Chemical formulaC₁₃H₁₃ClN₄OS
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary Target fibroblast growth factor-inducible 14 (Fn14)
      Primary Target K<sub>i</sub>7.12 µ
      Purity≥98% 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 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 6 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
      5093740001 04055977241839

      Documentation

      Fn14 Antagonist, L524-0366 - CAS 951612-19-4 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Références bibliographiques

      Aperçu de la référence bibliographique
      Dhruv, H., et al. 2013. J. Biol. Chem. 288, 32261.
      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.

      Revision21-February-2014 JSW
      SynonymsFibroblast Growth Factor-inducible 14 Antagonist; L5240366, THD Receptor Antagonist; TNF-like Weak Inducer of Apoptosis Receptor Antagonist, TWEAK Receptor Antagonist; TWEAK-Fn14 Interaction Inhibitor
      DescriptionA triazolyl-thiomorpholinyl-methanone compound that acts as a fibroblast growth factor-inducible 14 (Fn14) antagonist via direct affinity interaction (KD = 7.12 µM) and competes against TNF-like Weak Inducer of Apoptosis (TWEAK) C-terminal/extracellular TNF homology domain (THD) for Fn14 binding (16.8% inhibition against 500 pg/mL sTWEAK; [Drug] = 25 µM). Shown to completely inhibit 100 ng/mL sTWEAK-stimulated migration of T98G glioma cells at 10 µM concentration and is more potent against sTWEAK- than TNFα-induced NF-κB activation (IC50 = 7.8 vs. 31.03 µM, respectively, in reporter assays using Fn14-NF-kB-Luc and NF-κB-Luc cells) without any apparent cytotoxicity up to 50 µM and 72 h in T98G cultures.
      FormWhite powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number951612-19-4
      Chemical formulaC₁₃H₁₃ClN₄OS
      Structure formulaStructure formula
      Purity≥98% 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 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesDhruv, H., et al. 2013. J. Biol. Chem. 288, 32261.