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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
Assay:
≥98% (HPLC)
Form:
powder
Storage condition:
OK to freeze, protect from light
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Product Name

Fn14 Antagonist, L524-0366,

assay

≥98% (HPLC)

Quality Segment

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

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

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.

Biochem/physiol Actions

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

Packaging

Packaged under inert gas

Preparation Note

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

Disclaimer

Toxicity: Standard Handling (A)

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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