FN14 ANTAGONIST L524-0366 (C15-1304-515)

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

Molecular Weight: 308.79. Empirical Formula: C₁₃H₁₃ClN₄OS. Assay: ≥. 98% (HPLC). Quality Level: 100. form: powder. potency: 7.12 . μ. M 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. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.