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G5797 Sigma-Aldrich

GSK0660

≥98% (HPLC)

Synonym: 3-(((2-Methoxy-4-(phenylamino)phenyl)amino]sulfonyl)-2-thiophenecarboxylic acid methyl ester

  • CAS Number 1014691-61-2

  • Empirical Formula (Hill Notation) C19H18N2O5S2

  • Molecular Weight 418.49

  •  MDL number MFCD12828770

  •  PubChem Substance ID 329799945

  •  NACRES NA.77

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Properties

Related Categories Approved Therapeutics/Drug Candidates, Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology, Cell Signaling and Neuroscience,
assay   ≥98% (HPLC)
form   powder
color   white to beige
solubility   DMSO: 10 mg/mL, clear
originator   GlaxoSmithKline
storage temp.   2-8°C
SMILES string   COC(=O)c1sccc1S(=O)(=O)Nc2ccc(Nc3ccccc3)cc2OC
InChI   1S/C19H18N2O5S2/c1-25-16-12-14(20-13-6-4-3-5-7-13)8-9-15(16)21-28(23,24)17-10-11-27-18(17)19(22)26-2/h3-12,20-21H,1-2H3
InChI key   NDFKBGWLUHKMFY-UHFFFAOYSA-N

Description

General description

GSK0660 has antiangiogenic property in oxygen-induced retinopathy. It also regulates tumor necrosis factor-α (TNFα)-induced inflammation in human retinal microvascular endothelial cells (HRMECs).

Application

GSK0660 has been used to study the effects of bezafibrate (BZA) on hypertrophy.

Packaging

5 mg in glass bottle

Biochem/physiol Actions

GSK0660 is a potent PPARβ/δ antagonist with a pIC50 of 6.8 (160 nM). GSK0660 is nearly inactive on PPARα and PPARγ with IC50s greater than 10 μM.

Features and Benefits

This compound is a featured product for Gene Regulation research. Click here to discover more featured Gene Regulation products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

This compound is featured on the Nuclear Receptors (PPARs) page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Safety & Documentation

Safety Information

RIDADR 
NONH for all modes of transport
WGK Germany 
2

Documents

Certificate of Analysis (COA)

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Protocols & Articles

Articles

Discover Bioactive Small Molecules for Gene Regulation

The loss of regulation of gene expression is a key component to many human disease states, including neurodegenerative disorders, autoimmune conditions and, most prominently, cancers. Regulation of g...
Keywords: Acetylations, Epigenetics, Gene expression, Genomics, Methylations, PAGE, Post translational modifications, Transcription

Nuclear Receptors (PPARs)

Peroxisome proliferator activated receptors (PPARs) are members of the nuclear hormone receptor superfamily of ligand-activated transcription factors that are related to retinoid, steroid and thyroid...
Keywords: Anti-inflammatory agents, Atomic absorption spectroscopy, Cancer, Cell proliferation, Clinical, Diabetes, Diseases, Gene expression, Hormones, Inflammation, Ligands, Lipid Metabolism, Metabolic Pathways, Metabolism, Obesity, Oxidations, RNA immunoprecipitation, Transcription, Vitamins

Peer-Reviewed Papers
15

References

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