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Merck KGaA
Frankfurter Str. 250
64293 Darmstadt
Germany
Telefon: +49 6151 72-0
Fax: +49 6151 72 2000
15 Februar 2012
wird geladen
A cell-permeable Streptomyces-derived antibiotic that contains two bicyclic peptide-linked quinoxalines and acts as a sequence-specific DNA bisintercalator. Echinomycin at 10 µM is shown to inhibit HIF-1 and Myc/Max DNA binding activities in U251 and MCF-7 nuclear extracts by >90%, while exhibiting little effect against the binding of AP-1 or NF-κB to their respective DNA targets that lack the 5'-ACGTG-3' core structure in cell-free EMSA assays. Reversibly inhibits hypoxia-induced HIF-1 transcription activity in an HRE promoter-based reporter assay in U215 cells (EC50 = 1.2 nM) and is of no effect against SV40 promoter-driven transcription activity. Despite echinomycin's in vitro apoptosis-inducing activity and the initial report of its in vivo antitumor effect in mice, clinical trials have not yet resulted in promising data regarding its therapeutic efficacy in cancer treatment.
| Produktinformationen | |||
|---|---|---|---|
| Form | White solid | ||
| Purity | ≥98% by HPLC | ||
| Chemische Formel | C51H64N12O12S2 | ||
| CAS-Nummer | 512-64-1 | ||
| Lager- und Versandinformationen | |||
|---|---|---|---|
| Lagerkategorie | -20°C | ||
| Ship |
Shipped with Blue Ice or with Dry Ice
Toxic |
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| Sicherheitshinweise | |||
|---|---|---|---|
| S-Satz |
S: 36-36/37/39-45-53 |
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| R-Satz |
R: 23/24/25-46 |
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