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Formula | C26H30O7 |
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Molecular Weight | 454.51 | CAS No. | 751-03-1 | |
Solubility (25°C)* | In vitro | DMSO | 91 mg/mL (200.21 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | Obacunone (AI3-37934, CCRIS 8657), a natural compound present in citrus fruits, has been demonstrated for various biological activities including anti-cancer and anti-inflammatory properties. It significantly inhibits aromatase activity in an in vitro enzyme assay with an IC50 value of 28.04 μM; also a novel activator of Nrf2. | ||||
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Targets |
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In vitro | Obacunone is strongly inhibited MCF-7 cell proliferation without affecting non-malignant breast cells. Treatment with obacunone increases apoptosis by upregulating expression of the pro-apoptotic protein Bax and down-regulating the anti-apoptotic protein Bcl2, as well as inducing G1 cell cycle arrest. In addition, obacunone significantly inhibits aromatase activity in an in vitro enzyme assay. Exposure of MCF-7 breast cancer cells to obacunone down-regulates expression of inflammatory molecules including nuclear factor-kappa B (NF-kB) and cyclooxygenase-2 (COX-2). Obacunone inhibits COX-2 and NF-kB by activation of the p38 mitogen-activated protein kinase (MAPK). Obacunone is reported as a glutathione S-transferase (GST) enzyme inducer as well as a neuroprotective agent acting by induction of heme oxygenase-1 via the p38 MAPK pathway[1]. Obacunone is a novel activator of Nrf2 by decreasing Nrf2 ubiquitination and increasing its stability. It can effectively protect cells from oxidative stress by activating the Nrf2 pathway. Obacunone could induce the expression of the ARE-dependent luciferase gene in a dose-dependent manner[2]. | ||||
In vivo | The systemic administration of obacunone strongly inhibits bleomycin-induced lung fibrosis in mice. Obacunone can inhibit cancer proliferation and has some therapeutic effects on cardiovascular diseases[2]. In vitro and animal studies suggests that obacunone and a few other limonoids may have potential anticarcinogenic activity against certain types of cancers. A 500-mg/kg (of body weight) dose of obacunone per day is well tolerated and does not have adverse effects in rats, indicating a low toxicity[3]. |
Cell Assay:[1] |
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Animal Study:[2] |
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Obacunone Photoprotective Effects against Solar-Simulated Radiation-Induced Molecular Modifications in Primary Keratinocytes and Full-Thickness Human Skin [ Int J Mol Sci, 2023, 24(14)11484] | PubMed: 37511243 |
Obacunone alleviates ferroptosis during lipopolysaccharide-induced acute lung injury by upregulating Nrf2-dependent antioxidant responses [ Cell Mol Biol Lett, 2022, 27(1):29] | PubMed: 35305560 |
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
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