5.09374

L524-0366

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

• Sinonimo/i: 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
• Formula empirica (notazione di Hill): C₁₃H₁₃ClN₄OS
• Numero CAS: 951612-19-4
• Peso molecolare: 308.79
• Numero MDL: MFCD15129559
• Codice UNSPSC: 12352200
• ID PubChem: 20973801
• NACRES: NA.77

Proprietà

• Nome del prodotto: Fn14 Antagonist, L524-0366,
• Saggio: ≥98% (HPLC)
• Livello qualitativo: 100
• Stato: powder
• Potenza: 7.12 μM K_i
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; protect from light
• Colore: white
• Solubilità: DMSO: 25 mg/mL
• Temperatura di conservazione: 2-8°C
• Stringa SMILE: C1CSCCN1C(=O)C2=CN(N=N2)C3=CC(=CC=C3)Cl
• InChI: 1S/C13H13ClN4OS/c14-10-2-1-3-11(8-10)18-9-12(15-16-18)13(19)17-4-6-20-7-5-17/h1-3,8-9H,4-7H2

Descrizione

Descrizione generale

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.

Azioni biochim/fisiol

Primary Target
fibroblast growth factor-inducible 14 (Fn14)

Reversible: yes

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Standard Handling (A)

Ricostituzione

Use only fresh DMSO for reconstitution.

Altre note

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

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 3
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable