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T5202 Sigma-Aldrich

TPBM

≥98% (HPLC), solid

Synonym: 8-Benzylsulfanylmethyl-1,3-dimethyl-3,7-dihydro-purine-2,6-dione, 8-[(Benzylthio)methyl]theophylline, Theophylline, 8-[(benzylthio)methyl]

  • CAS Number 6466-43-9

  • Empirical Formula (Hill Notation) C15H16N4O2S

  • Molecular Weight 316.38

  •  MDL number MFCD11114397

  •  PubChem Substance ID 329826819

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Properties

Related Categories Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology, Cell Signaling and Neuroscience, Gene Regulation,
InChI Key   FEHAMBYTUPDFJE-UHFFFAOYSA-N
assay   ≥98% (HPLC)
form   solid
color   white to off-white
solubility   DMSO: >5 mg/mL

Description

Packaging

5, 25 mg in glass bottle

Preparation Note

TPBM is soluble in DMSO at a concentration that is greater than 5 mg/ml.

Biochem/physiol Actions

TPBM is a potent inhibitor of estrogen receptor α via blocking ERα binding to consensus estrogen response element (cERE) DNA. Estrogen receptor α (ERα) plays an important role in several human cancers. Current ERα antagonists bind in the receptor ligand binding pocket and compete for binding with estrogenic ligands. TPBM instead inhibits ERα via binding to consensus estrogen response element (cERE) DNA. TPBM is not toxic to cells and does not effect estrogen-independent cell growth. TPBM does not act by chelating the zinc in ERs zinc fingers and differs from known ERα inhibitors.

Features and Benefits

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

Safety & Documentation

Safety Information

RIDADR 
NONH for all modes of transport
WGK Germany 
3

Documents

Certificate of Analysis


Milli-Q® Water Purification Solutions
Protocols & Articles

Articles

Nuclear Receptors (Steroids)

Intracellular receptors (IRs) are a class of ligand-dependent transcription factors that include receptors for both steroid and non-steroid hormones. Upon binding their cognate hormone, these recepto...
Keywords: Anti-inflammatory agents, Apoptosis, Atomic absorption spectroscopy, Cancer, Cardiovascular, Cell proliferation, Diseases, Diuretics, Gene expression, Hormones, Infrared spectroscopy, Ligands, Metabolism, Metabolites, Transcription, Transduction

Peer-Reviewed Papers
15

References

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