5.09374

L524-0366

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

• 別名: 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
• 実験式（ヒル表記法）: C₁₃H₁₃ClN₄OS
• CAS番号: 951612-19-4
• 分子量: 308.79
• UNSPSCコード: 12352200
• PubChem Substance ID: 20973801
• NACRES: NA.77

特性

• product name: Fn14 Antagonist, L524-0366,
• アッセイ: ≥98% (HPLC)
• 品質水準: 100
• 形状: powder
• 有効性: 7.12 μM K_i
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: white
• 溶解性: DMSO: 25 mg/mL
• 保管温度: 2-8°C
• SMILES記法: C1CSCCN1C(=O)C2=CN(N=N2)C3=CC(=CC=C3)Cl

詳細

詳細

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.

生物化学的／生理学的作用

Primary Target
fibroblast growth factor-inducible 14 (Fn14)

Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

再構成

Use only fresh DMSO for reconstitution.

その他情報

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

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable