85547-22-4
85547-22-4
Chemical Structure
Aaptamine
- CAS No.: 85547-22-4
- Formula:C13H12N2O2
- Molecular Weight:228.25
IUPAC Name: 8,9-dimethoxy-1H-benzo[de][1,6]naphthyridine
InChIKey: IVXSXOFPZFVZTM-UHFFFAOYSA-N
SMILES: COC1=C2C3=C(N=CC=C3C=C1OC)C=CN2
Biological Activity: Aaptamine is an alkaloid that can be isolated from the sponge Aaptos suberitoides. Aaptamine is a competitive antagonist of the α-adrenergic receptor, as well as an inhibitor of the proteasome and cholinesterase. Aaptamine is cytotoxic to tumor cells and can induce apoptosis, cell cycle arrest of tumor cells, and the expression of p21 through a p53-independent pathway. Aaptamine has multiple activities such as anti-tumor, antioxidant, antibacterial, and analgesic effects[1][2][3][4][5][6][7].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Aaptamine | 99.71% | Aaptamine is an alkaloid that can be isolated from the sponge Aaptos suberitoides. Aaptamine is a competitive antagonist of the α-adrenergic receptor, as well as an inhibitor of the proteasome and cholinesterase. Aaptamine is cytotoxic to tumor cells and can induce apoptosis, cell cycle arrest of tumor cells, and the expression of p21 through a p53-independent pathway. Aaptamine has multiple activities such as anti-tumor, antioxidant, antibacterial, and analgesic effects. | ||||||||||||||||||||
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Amiquinsin hydrochloride monohydrate | Amiquinsin hydrochloride monohydrate is a compound with hypotensive activity. Amiquinsin hydrochloride monohydrate is metabolized in vivo, and the major metabolite is 4-amino-6,7-dimethoxy-3-quinolinol hydrochloride hydrate. | |||||||||||||||||||||
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PDL1 degrader-3 | PDL1 degrader-3 (compound e24) is a DUBTAC-like PD-L1 degrader. PDL1 degrader-3 inhibits CSN5 enzymatic activity, increases PD-L1 ubiquitination, and induces PD-L1 degradation via the ubiquitin-proteasome pathway, reducing PD-L1 expression on tumor cell membranes. PDL1 degrader-3 blocks PD-1/PD-L1 interaction, activates the tumor immune microenvironment, enhances tumor-infiltrating T-cell immunity, and inhibits activation of immunosuppressive MDSCs and Tregs. PDL1 degrader-3 exerts antitumor effects in mouse tumor models. PDL1 degrader-3 can be used for the research of colorectal cancer, lung cancer. | |||||||||||||||||||||
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Harmine hydrochloride (Standard) | ≥98% | Harmine Hydrochloride (Telepathine Hydrochloride) is a natural DYRK inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM. | ||||||||||||||||||||
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Batatasin I | 99.0% | Batatasin I is a natural product that can be isolated from tuberous roots of Dioscorea batatas, with antifungal activity and anti-inflammatory effects. | ||||||||||||||||||||
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3,5-Dimethoxy-2,7-phenanthrenediol | 3,5-Dimethoxy-2,7-phenanthrenediol (compound 2) is a phenanthrene compound isolated from the roots of Combretum laxum. 3,5-Dimethoxy-2,7-phenanthrenediol is cytotoxic to human cancer cell lines 786-0, MCF-7 and NCI/ADR-RES, with IC50s of 73.26 μM, 118.40 μM and 83.99 μM respectively. 3,5-Dimethoxy-2,7-phenanthrenediol also has free radical scavenging activity with an IC50 of 20.4 μM. | |||||||||||||||||||||
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5,7-Dimethoxy-2,3-phenanthrenediol | 5,7-Dimethoxy-2,3-phenanthrenediol is a compound with estrogenic activity. 5,7-Dimethoxy-2,3-phenanthrenediol increases the proliferation of MCF-7 cell and the expression of ERβ in the MCF-7 cell line. | |||||||||||||||||||||
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Denthyrsinin | Denthyrsinin is a phenanthrene. | |||||||||||||||||||||
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Loddigesiinol A | Loddigesiinol A is a phenanthrene compound found in Dendrobium loddigesii. Loddigesiinol A acts as a DPPH radical scavenger with an IC50 of 26.1 μM. Loddigesiinol A also inhibits nitric oxide production. Loddigesiinol A is applicable to inflammation-related research. | |||||||||||||||||||||
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Nudol | 99.60% | Nudol is a phenanthrene compound that has anti-cancer activity. Nudol inhibits cell proliferation, induces cell apoptosis. Nudol inhibits MMP-2M and MMP-9 activity (Ki: 988.9 nM, 1.76 μM, respectively). Nudol can be used in the research of cancers, such as osteosarcoma. | ||||||||||||||||||||
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Cabozantinib impurity 8 (Standard) | ≥98% | Cabozantinib impurity 8 (Standard) is the analytical standard of Cabozantinib impurity 8 (HY-Z1053). This product is intended for research and analytical applications. | ||||||||||||||||||||
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References
- [1]. Ohizumi Y, et al. Alpha-adrenoceptor blocking action of aaptamine, a novel marine natural product, in vascular smooth muscle. J Pharm Pharmacol. 1984 Nov;36(11):785-6. [Content Brief]
- [2]. Aoki S, et al. Aaptamine, a spongean alkaloid, activates p21 promoter in a p53-independent manner. Biochem Biophys Res Commun. 2006 Mar 31;342(1):101-6. [Content Brief]
- [3]. Tsukamoto S, et al. Aaptamine, an alkaloid from the sponge Aaptos suberitoides, functions as a proteasome inhibitor. Bioorg Med Chem Lett. 2010 Jun 1;20(11):3341-3. [Content Brief]
- [4]. Dyshlovoy SA, et al. Aaptamines from the marine sponge Aaptos sp. display anticancer activities in human cancer cell lines and modulate AP-1-, NF-κB-, and p53-dependent transcriptional activity in mouse JB6 Cl41 cells. Biomed Res Int. 2014;2014:469309. [Content Brief]
- [5]. Suciati S, et al. In vitro and in silico cholinesterase inhibitory activities of aaptamine and derivatives from Aaptos suberitoides. Journal of Pharmacy and Pharmacognosy Research, 2025, 13(3): 757-773.
- [6]. Rajivgandhi G, et al. Marine sponge alkaloid aaptamine enhances the anti-bacterial and anti-cancer activity against ESBL producing Gram negative bacteria and HepG 2 human liver carcinoma cells. Biocatalysis and Agricultural Biotechnology, 2019, 17: 628-637.
- [7]. Sung CS, et al. Antinociceptive Effects of Aaptamine, a Sponge Component, on Peripheral Neuropathy in Rats. Mar Drugs. 2023 Feb 4;21(2):113. [Content Brief]
