Competitive antagonist of α-adrenoceptors in vascular smooth muscle cells. Inhibits cancer cell growth.
Inhibitor of sortase A (SrtA) IC50=23.5 µg/ml. Minimum inhibitory concentration (MIC) on S. aureus >200µg/ml.
Proteasome (chymotrypsin-like) inhibitor IC50=1,6µg/ml.
Product Specification
| Alternative Name: | 8,9-Dimethoxy-1H-benzo[de][1,6]naphtyridine |
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| Formula: | C13H12N2O2 |
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| MW: | 228.3 |
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| Purity: | ≥97% |
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| Appearance: | Oil. |
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| CAS: | 85547-22-4 |
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| Source/Host: | Isolated from the sponge Aaptos aaptos. |
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| Solubility: | Soluble in DMSO or 100% ethanol. |
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| Long Term Storage: | -20°C |
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| Hazard: | TOXIC. |
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| Handling: | Protect from light. |
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Product Literature References
Aaptamine, an alkaloid from the sponge Aaptos suberitoides, functions as a proteasome inhibitor: S. Tsukamoto, et al.; Bioorg. Med. Chem. Lett.
20, 3341 (2010),
Abstract;
Aaptamines as sortase A inhibitors from the tropical sponge Aaptos aaptos: K.H. Jang, et al.; Bioorg. Med. Chem. Lett.
17, 5366 (2007),
Abstract;
Aaptamine, a spongean alkaloid, activates p21 promoter in a p53-independent manner: S. Aoki, et al.; BBRC
342, 101 (2006),
Abstract;
Antineoplastic agents 491. Synthetic conversion of aaptamine to isoaaptamine, 9-demethylaaptamine, and 4-methylaaptamine: G.R. Pettit, et al.; J. Org. Chem.
69, 2251 (2004),
Abstract;
Alpha-adrenoceptor blocking action of aaptamine, a novel marine natural product, in vascular smooth muscle: Y. Ohizumi, et al.; J. Pharm. Pharmacol.
36, 785 (1984),
Abstract;