509374 | Fn14 Antagonist, L524-0366 - Calbiochem

509374
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₃H₁₃ClN₄OS

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.09374.0001
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          Glass bottle 10 mg
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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
          FormWhite powder
          Hill FormulaC₁₃H₁₃ClN₄OS
          Chemical formulaC₁₃H₁₃ClN₄OS
          ReversibleY
          Structure formula ImageStructure formula Image
          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

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Dhruv, H., et al. 2013. J. Biol. Chem. 288, 32261.
          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.

          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
          Chemical formulaC₁₃H₁₃ClN₄OS
          Structure formulaStructure formula
          Purity≥98% by HPLC
          SolubilityDMSO (25 mg/ml). Use only fresh DMSO for reconstitution.
          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 6 months at -20°C.
          Toxicity Standard Handling
          ReferencesDhruv, H., et al. 2013. J. Biol. Chem. 288, 32261.