5.09374

L524-0366

≥98% (HPLC), powder, Fn14 antagonist, Calbiochem^®

• Synonyme(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
• Formule empirique (notation de Hill): C₁₃H₁₃ClN₄OS
• Numéro CAS: 951612-19-4
• Poids moléculaire : 308.79
• Code UNSPSC : 12352200
• ID de substance PubChem : 20973801
• Nomenclature NACRES : NA.77

Propriétés

• product name: Fn14 Antagonist, L524-0366,
• Pureté: ≥98% (HPLC)
• Niveau de qualité: 100
• Forme: powder
• Puissance: 7.12 μM K_i
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: white
• Solubilité: DMSO: 25 mg/mL
• Température de stockage: 2-8°C
• Chaîne SMILES: C1CSCCN1C(=O)C2=CN(N=N2)C3=CC(=CC=C3)Cl

Description

Description générale

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.

Actions biochimiques/physiologiques

Primary Target
fibroblast growth factor-inducible 14 (Fn14)

Reversible: yes

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

Use only fresh DMSO for reconstitution.

Autres remarques

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

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable