5.09374

Fn14 Antagonist, L524-0366

• Synonym(s): Fn14 Antagonist, L524-0366, 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
• Empirical Formula (Hill Notation): C₁₃H₁₃ClN₄OS
• CAS Number: 951612-19-4
• Molecular Weight: 308.79
• UNSPSC Code: 12352200
• PubChem Substance ID: 20973801

Properties

• Assay: ≥98% (HPLC)
• Quality Level: 100
• form: powder
• potency: 7.12 μM K_i
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: white
• solubility: DMSO: 25 mg/mL
• storage temp.: 2-8°C
• SMILES string: C1CSCCN1C(=O)C2=CN(N=N2)C3=CC(=CC=C3)Cl

Description

General description

A triazolyl-thiomorpholinyl-methanone compound that acts as a fibroblast growth factor-inducible 14 (Fn14) antagonist via direct affinity interaction (K_D = 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.

A triazolyl-thiomorpholinyl-methanone compound that competes against TWEAK C-terminal/extracellular TNF homology domain (THD) for Fn14 binding (K_D = 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.

Biochem/physiol Actions

Primary Target
fibroblast growth factor-inducible 14 (Fn14)

Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Use only fresh DMSO for reconstitution.

Other Notes

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

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable