Fn14 Antagonist, L524-0366-Calbiochem

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一般描述

A triazolyl-thiomorpholinyl-methanone compound that acts as a fibroblast growth factor-inducible 14 (Fn14) antagonist via direct affinity interaction (K_D= 7.12 ?M) 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 ?M). Shown to completely inhibit 100 ng/mL sTWEAK-stimulated migration of T98G glioma cells at 10 ?M concentration and is more potent against sTWEAK- than TNFα-induced NF-κB activation (IC₅₀= 7.8 vs. 31.03 ?M, respectively, in reporter assays using Fn14-NF-kB-Luc and NF-κB-Luc cells) without any apparent cytotoxicity up to 50 ?M 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 ?M). Shown to completely inhibit 100 ng/mL sTWEAK-stimulated migration of T98G glioma cells at 10 ?M concentration and is more potent against sTWEAK- than TNFα-induced NF-κB activation (IC₅₀= 7.8 vs. 31.03 ?M, respectively, in reporter assays) without any apparent cytotoxicity up to 50 ?M and 72 h in T98G cultures.

生化/生理作用

Reversible: yes
Primary Target
fibroblast growth factor-inducible 14 (Fn14)

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

Use only fresh DMSO for reconstitution.

其他说明

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

法律信息

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

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