Merck
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5.09374

Sigma-Aldrich

Fn14 Antagonist, L524-0366

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Synonym(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
Empirical Formula (Hill Notation):
C13H13ClN4OS
Molecular Weight:
308.79
PubChem Substance ID:
20973801

Assay

≥98% (HPLC)

Quality Level

100

form

powder

potency

7.12 μM Ki

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

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Fn14 Antagonist, L524-0366

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Fn14 Antagonist, L524-0366

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Anti-Fn14 Antibody from rabbit, purified by affinity chromatography

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344220

Formyl Peptide Receptor-Like 1 Antagonist, WRW⁴

form

powder

form

solid

form

-

form

lyophilized solid

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

-

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

-

storage condition

OK to freeze, desiccated (hygroscopic)

color

white

color

white

color

-

color

white

solubility

DMSO: 25 mg/mL

solubility

H2O: 100 mg/mL

solubility

-

solubility

DMSO: 5 mg/mL

General description

A triazolyl-thiomorpholinyl-methanone compound that acts as a fibroblast growth factor-inducible 14 (Fn14) antagonist via direct affinity interaction (KD = 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 (KD = 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

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

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Harshil Dhruv et al.
The Journal of biological chemistry, 288(45), 32261-32276 (2013-09-24)
Deregulation of the TNF-like weak inducer of apoptosis (TWEAK)-fibroblast growth factor-inducible 14 (Fn14) signaling pathway is observed in many diseases, including inflammation, autoimmune diseases, and cancer. Activation of Fn14 signaling by TWEAK binding triggers cell invasion and survival and therefore

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