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S1697 Sigma-Aldrich

SPD304

≥98% (HPLC), solid

Synonym: 6,7-Dimethyl-3-[[methyl[2-[methyl[[1-[3-(trifluoromethyl)phenyl]-1H-indol-3-yl]methyl]amino]ethyl]amino]methyl]-(4H-1-Benzopyran-4-one dihydrochloride, SPD00000304

  • Empirical Formula (Hill Notation) C32H32F3N3O2 · 2HCl

  • Molecular Weight 620.53

  •  MDL number MFCD09265259

  •  PubChem Substance ID 24724602

  •  NACRES NA.77

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Properties

Related Categories Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology, Cell Signaling and Neuroscience, Cytokines and Growth Factors,
InChI Key   GOZMBJCYMQQACI-UHFFFAOYSA-N
assay   ≥98% (HPLC)
form   solid
color   white
solubility   H2O: >5 mg/mL
storage temp.   2-8°C
Gene Information   human ... TNF(7124)
mouse ... TNF(21926)
rat ... TNF(24835)

Description

Application

SPD304 has been used in the inhibition of tumor necrosis factor receptor 1 (TNFR1) in dorsal root ganglion neurons and tumor necrosis factor alpha in colonic epithelial cell lines.

SPD304 may be used in TNF-α-mediated cell signaling studies.

Packaging

1, 5 mg in glass bottle

Biochem/physiol Actions

SPD304 is a small molecule inhibitor of TNF-a activity with a novel mechanism of action. It interferes with protein-protein interactions on the contact surfaces of the trimeric TNF-a subunits, displacing one of the trimer units, resulting in dissociation of the trimer and loss of activity at the receptor TNFR1. SPD304 inhibits TNFR1 receptor binding to TNF-a with an IC50 of 22μM in vitro and inhibits TNF-a-mediated stimulation of IkB degradation in HeLa cells with an IC50 of 4.6 μM.

Trimerization of TNF-α is essential for its biological activity. SPD304 inhibits the trimerization by interacting with Glycine 122 residue. It also inhibits the activity of Receptor activator of nuclear factor-κB ligand (RANKL) by similar interaction.

Safety & Documentation

Safety Information

Personal Protective Equipment 
RIDADR 
NONH for all modes of transport
WGK Germany 
3

Documents

Certificate of Analysis (COA)

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Protocols & Articles

Articles

Cytokine Receptors (Tumor Necrosis Receptor Family)

The cytokines and receptors of the Tumor Necrosis Factor (TNF) superfamily serve as an intercellular communication network integrating cellular responses in vertebrates. TNF receptors activate signal...
Keywords: Angiogenesis, Anti-inflammatory agents, Apoptosis, Calcification, Cancer, Cell proliferation, Diseases, Gene expression, Growth factors, Inflammation, Ligands, Transcription, Transduction

Discover Bioactive Small Molecules for Cytokines & Growth Factors Research

Cytokines and growth factors (GF) are chemical messengers that mediate intracellular communication, thereby regulating cellular and nuclear functions. These chemical messengers bind cell surface rece...
Keywords: Biological processes, Cancer, Cell proliferation, Diseases, Growth factors, Ligands, Phosphorylations, Transcription, Transduction

Peer-Reviewed Papers
15

References

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