9-Hydroxyellipticin
9-hydroxyellipticine is an inhibitor of Topo II and RyR, exhibiting high affinity for DNA with a Pka value of 9.8 at pH 7.4. It has antitumor, antioxidant, and catecholamine-releasing activities, with IC50 values of 1.6 μM and 1.2 μM for Hela S-3 and 293T cells, respectively. It also demonstrates anticancer effects in L1210 leukemia mice.
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- No. CAS: 51131-85-2
- Fòrmula: C17H14N2O
- Peso molecular:262.31
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| L1210 | ED50 |
0.08 μM
Compound: 19b
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The effective dose against L1210 cell growth
The effective dose against L1210 cell growth
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[PMID: 4009597] |
| NCI-H358 | IC50 |
5.6 μM
Compound: 2 (9-OH-ellipticin)
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Cytotoxicity against H 358 human lung cancer cell line
Cytotoxicity against H 358 human lung cancer cell line
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[PMID: 1479585] |
| NCI-H417 | IC50 |
3.5 μM
Compound: 2 (9-OH-ellipticin)
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Cytotoxicity against N 417 human lung cancer cell line
Cytotoxicity against N 417 human lung cancer cell line
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[PMID: 1479585] |
| NCI-H460 | IC50 |
2.6 μM
Compound: 2 (9-OH-ellipticin)
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Cytotoxicity against H 460 human lung cancer cell line
Cytotoxicity against H 460 human lung cancer cell line
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[PMID: 1479585] |
| NCI-H69 | IC50 |
1.7 μM
Compound: 2 (9-OH-ellipticin)
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Cytotoxicity against H69 human lung cancer cell line
Cytotoxicity against H69 human lung cancer cell line
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[PMID: 1479585] |
| NIH3T3 | IC50 |
0.9 μM
Compound: 4
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Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell viability after 72 hrs by MTT assay
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[PMID: 28063783] |
| Sarcoma-180 | IC50 |
0.44 μM
Compound: 4
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Cytotoxicity against mouse Sarcoma 180 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against mouse Sarcoma 180 cells assessed as reduction in cell viability after 72 hrs by MTT assay
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[PMID: 28063783] |
Chemical Information
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No. CAS 51131-85-2
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Peso molecular 262.31
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Fòrmula C17H14N2O
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SMILES
OC1=CC2=C(NC3=C2C(C)=C(C=NC=C4)C4=C3C)C=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocolo
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Calcium Spark Assay
Calcium sparks are localized, transient increases in intracellular calcium concentration ([Ca2+]i) that occur in cardiac myocytes and represent elementary events underlying excitation-contraction coupling. These events are generated by the coordinated opening of clusters of ryanodine receptors (RyRs) on the sarcoplasmic reticulum membrane, leading to a brief release of Ca2+ into the cytosol. The detection and analysis of calcium sparks provide insights into the mechanisms of calcium handling and signaling in cardiac cells. Imaging techniques using fluorescent calcium indicators such as Fluo-3 are employed to visualize these subcellular calcium transients with high spatial and temporal resolution. The protocol is based on established methodologies described in primary literature for both experimental measurement and automated analysis of calcium sparks.
Pureza y Documentación
Referencias
[1]. Renault G, et al. In vivo exposure to four ellipticine derivatives with topoisomerase inhibitory activity results in chromosome clumping and sister chromatid exchange in murine bone marrow cells. Toxicol Appl Pharmacol. 1987 Jun 30;89(2):281-6. [Content Brief]
[2]. Saeki K, et al. Cardioprotective effects of 9-hydroxyellipticine on ischemia and reperfusion in isolated rat heart. Jpn J Pharmacol. 2002 May;89(1):21-8. [Content Brief]
[3]. G Renault, et al. In vivo exposure to four ellipticine derivatives with topoisomerase inhibitory activity results in chromosome clumping and sister chromatid exchange in murine bone marrow cells. Toxicol Appl Pharmacol. 1987 Jun 30;89(2):281-6. [Content Brief]
[4]. Le Pecq JB, et al. A new antitumoral agent: 9-hydroxyellipticine. Possibility of a rational design of anticancerous drugs in the series of DNA intercalating drugs. Proc Natl Acad Sci U S A. 1974 Dec;71(12):5078-82. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
9-Hydroxyellipticin Related Classifications
HY-101775 Related Classifications
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