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14 February 2012
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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.
| Product information | |||
|---|---|---|---|
| Form | White solid | ||
| Molar mass | 1101.3 | ||
| Purity | ≥98% by HPLC | ||
| Solubility | DMSO | ||
| Chemical formula | C51H64N12O12S2 | ||
| CAS number | 512-64-1 | ||
| Store and ship information | |||
|---|---|---|---|
| Storage | -20°C | ||
| Ship |
Shipped with Blue Ice or with Dry Ice
Toxic |
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| Safety information | |||
|---|---|---|---|
| S Phrase |
S: 36-36/37/39-45-53 Wear suitable protective clothing. Wear suitable protective clothing, gloves and eye/face protection. In case of accident or if you feel unwell, seek medical advice immediately (show the label where possible). Avoid exposure - obtain special instructions before use. |
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| R Phrase |
R: 23/24/25-46 Toxic by inhalation, in contact with skin and if swallowed. May cause heritable genetic damage. |
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