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Merck

5.09374

L524-0366

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

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

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About This Item

Empirical Formula (Hill Notation):
C13H13ClN4OS
CAS Number:
951612-19-4
Molecular Weight:
308.79
MDL number:
MFCD15129559
UNSPSC Code:
12352200
NACRES:
NA.77
PubChem Substance ID:
20973801

Product Name

Fn14 Antagonist, L524-0366,

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

InChI key

ZOBDTKWDYMRKPF-UHFFFAOYSA-N

SMILES string

C1CSCCN1C(=O)C2=CN(N=N2)C3=CC(=CC=C3)Cl

assay

≥98% (HPLC)

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

Quality Level

100

Related Categories

Biochem/physiol Actions

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

Disclaimer

Toxicity: Standard Handling (A)

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.

Other Notes

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

Packaging

Packaged under inert gas

Preparation Note

Use only fresh DMSO for reconstitution.

Legal Information

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

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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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

Global Trade Item Number

SKUGTIN
5.09374.000104055977241839

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