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    CAS No. 550-24-3 Price $80 / 20mg
    Catalog No.CFN90537Purity>=98%
    Molecular Weight294.38Type of CompoundQuinones
    FormulaC17H26O4Physical DescriptionPowder
    Download     COA    MSDSSimilar structuralComparison (Web)
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    Biological Activity
    Description: Embelin is an inhibitor of X-linked inhibitor of apoptosis (XIAP) with IC50 of 4.1 μM in a cell-free assay.Embelin has antitumor, antioxidant and anti-inflammatory activities. Embelin can enhance TRAIL-induced cell apoptosis through DR4 and DR5 upregulation and decrease IL-6-induced STAT3 phosphorylation, that combination of low-toxicity Embelin and TRAIL may become as a potential antileukemia strategy.
    Targets: STAT | p53 | IL Receptor | gp120/CD4 | NF-kB | TNF-α | VEGFR | MMP(e.g.TIMP) | XIAP | DR4 | DR5
    In vitro:
    Tumour Biol. 2015 Feb;36(2):769-77.
    The XIAP inhibitor Embelin enhances TRAIL-induced apoptosis in human leukemia cells by DR4 and DR5 upregulation.[Pubmed: 25293521]
    The present study was designed to explore the effects of low-toxicity Embelin on TRAIL-induced apoptosis and its possible mechanism in human leukemia cells.
    Our study showed that low-toxicity Embelin enhanced TRAIL-induced apoptosis through DR4 and DR5 upregulation and caspase activation in HL-60 cells. Pan-caspase inhibitor Z-VAD-FMK inhibited cell apoptosis induced by TRAIL alone or combined with low-toxicity Embelin, which indicated the cytotoxic effect is mediated by caspase-dependent apoptosis. Although Embelin is an X chromosome-linked inhibitor-of-apoptosis protein (XIAP) inhibitor, an XIAP independent effect on cell death was detected in HL-60 cells exposed to low-toxicity Embelin and TRAIL. Low-toxicity Embelin upregulated DR4 and DR5 expression to enhance TRAIL-induced apoptosis. The sensitizing effects of Embelin on TRAIL-induced apoptosis were markedly attenuated when DR4/DR5 was knocked down.
    These data suggested that low-toxicity Embelin enhanced TRAIL-induced cell apoptosis through DR4 and DR5 upregulation, indicating that combination of low-toxicity Embelin and TRAIL may become as a potential antileukemia strategy.
    BMC Cancer. 2014 Oct 22;14:775.
    Embelin inhibits TNF-α converting enzyme and cancer cell metastasis: molecular dynamics and experimental evidence.[Pubmed: 25336399]
    Embelin, a quinone derivative, is found in the fruits of Embelia ribes Burm (Myrsinaceae). It has been shown to have a variety of therapeutic potentials including anthelmintic, anti-tumor, anti-diabetic, anti-bacterial and anti-inflammation. Several studies have shown that the anti-inflammatory activity of Embelin is mediated by reduction in TNF-α. The latter is synthesized as a membrane anchored protein (pro-TNF-α); the soluble component of pro-TNF-α is then released into the extracellular space by the action of a protease called TNF-α converting enzyme (TACE). TACE, hence, has been proposed as a therapeutic target for inflammation and cancer.
    We used molecular docking and experimental approaches to investigate the docking potential and molecular effects of Embelin to TACE and human cancer cell characteristics, respectively. We demonstrate that Embelin is a potential inhibitor of TACE. Furthermore, in vitro studies revealed that it inhibits malignant properties of cancer cells through inactivation of metastatic signaling molecules including MMPs, VEGF and hnRNP-K in breast cancer cells.
    Based on the molecular dynamics and experimental data, Embelin is proposed as a natural anti-inflammatory and anticancer drug.
    In vivo:
    Mol Cancer Ther. 2014 May;13(5):1206-16.
    Embelin reduces colitis-associated tumorigenesis through limiting IL-6/STAT3 signaling.[Pubmed: 24651526]
    Embelin is a small molecule inhibitor of X-linked inhibitor of apoptosis protein (XIAP), with antioxidant, anti-inflammatory, and antitumor activities. We previously showed that Embelin inhibits the growth of colon cancer cells in vitro, and effectively suppresses 1,2-dimethylhydrazine dihydrochloride-induced colon carcinogenesis in mice.
    Here, we explored the antitumor effects and mechanisms of Embelin on colitis-associated cancer (CAC) using the azoxymethane/dextran sulfate sodium (AOM/DSS) model, with a particular focus on whether Embelin exerts its effect through the IL-6/STAT3 pathway. We found that Embelin significantly reduced incidence and tumor size in CAC-bearing mice. In addition to inhibiting proliferation of tumor epithelial cells, Embelin suppressed colonic IL-6 expression and secretion, and subsequently STAT3 activation in vivo. Importantly, in vitro studies have revealed that in colon cancer cells, Embelin diminished both the constitutive and IL-6-induced STAT3 activation by stimulating Src homology domain 2-containing protein tyrosine phosphatase (SHP2) activity. Moreover, Embelin protected mice from AOM/DSS-induced colitis before tumor development. Embelin decreased IL-1β, IL-17a, and IL-23a expression as well as the number of CD4(+) T cells and macrophages infiltrating the colonic tissues.
    Thus, our findings demonstrated that Embelin suppresses CAC tumorigenesis, and its antitumor effect is partly mediated by limiting IL-6/STAT3 activation and Th17 immune response. Embelin may be a potential agent in the prevention and treatment of CAC.
    Embelin Description
    Source: The herbs of Paederia scandens (Lour.) Merr
    Solvent: Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.
    Storage: Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months(2-8C).

    Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

    Need more advice on solubility, usage and handling? Please email to: service@chemfaces.com

    After receiving: The packaging of the product may have turned upside down during transportation, resulting in the natural compounds adhering to the neck or cap of the vial. take the vial out of its packaging and gently shake to let the compounds fall to the bottom of the vial. for liquid products, centrifuge at 200-500 RPM to gather the liquid at the bottom of the vial. try to avoid loss or contamination during handling.
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    Recently, ChemFaces products have been cited in many studies from excellent and top scientific journals

    Cell. 2018 Jan 11;172(1-2):249-261.e12.
    doi: 10.1016/j.cell.2017.12.019.

    PMID: 29328914

    Mol Cell. 2017 Nov 16;68(4):673-685.e6.
    doi: 10.1016/j.molcel.2017.10.022.

    PMID: 29149595

    Scientific Reports 2017 Dec 11;7(1):17332.
    doi: 10.1038/s41598-017-17427-6.

    PMID: 29230013

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    doi: 10.3390/molecules22111829.

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    J Cell Biochem. 2018 Feb;119(2):2231-2239.
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    Phytomedicine. 2018 Feb 1;40:37-47.
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    PMID: 29496173
    Calculate Dilution Ratios(Only for Reference)
    1 mg 5 mg 10 mg 20 mg 25 mg
    1 mM 3.397 mL 16.9848 mL 33.9697 mL 67.9394 mL 84.9242 mL
    5 mM 0.6794 mL 3.397 mL 6.7939 mL 13.5879 mL 16.9848 mL
    10 mM 0.3397 mL 1.6985 mL 3.397 mL 6.7939 mL 8.4924 mL
    50 mM 0.0679 mL 0.3397 mL 0.6794 mL 1.3588 mL 1.6985 mL
    100 mM 0.034 mL 0.1698 mL 0.3397 mL 0.6794 mL 0.8492 mL
    * Note: If you are in the process of experiment, it's need to make the dilution ratios of the samples. The dilution data of the sheet for your reference. Normally, it's can get a better solubility within lower of Concentrations.
    Kinase Assay:
    Cell Biochem Biophys. 2015 Jan;71(1):291-7.
    Embelin sensitizes acute myeloid leukemia cells to TRAIL through XIAP inhibition and NF-κB inactivation.[Pubmed: 25358405]
    Embelin is a potent XIAP inhibitor which has been shown to inhibit the proliferation of tumor cells and cause cell apoptosis.
    In this study, we investigated the effects of Embelin on the TRAIL-induced apoptosis and the underlying mechanism. Here, we chose an adenovirus vector as the expression vector for TRAIL, which was named Ad-TRAIL. The results in vitro showed that the co-treatment of Embelin and Ad-TRAIL has synergistically suppressed the proliferation of AML cells. Embelin has the ability to enhance TRAIL-induced apoptosis and activate caspase pathway. More interestingly, we found that the underlying mechanism for these talent skills of Embelin is through reducing the TRAIL-mediated activation of NF-κB and decreasing its transcriptional activity. Furthermore, our results in vivo suggest that combined therapy of Embelin and Ad-TRAIL caused significant growth inhibition of HL-60 xenograft tumors.
    Our results suggested that Embelin could sensitize AML cell to TRAIL through the repression of NF-κB signal pathway in vitro and in vivo, and combined therapy of Ad-TRAIL and Embelin may be the attractive candidate for clinical application in treatment of AML.
    Cell Research:
    Cancer Lett. 2014 Nov 28;354(2):407-16.
    Embelin inhibits pancreatic cancer progression by directly inducing cancer cell apoptosis and indirectly restricting IL-6 associated inflammatory and immune suppressive cells.[Pubmed: 25128650]
    Pancreatic cancer is an aggressive malignancy and unresponsive to conventional chemotherapies. Here, the anti-inflammatory and anti-tumor effects of Embelin on pancreatic cancer were investigated.
    Embelin significantly attenuated cells invasion, proliferation and induced apoptosis through inhibition of STAT3 and activation of p53 signaling pathways. Embelin substantially reduced the tumorigenicity of pancreatic cancer cells in vivo, which was associated with reduced inflammatory cells and immune suppressive cells, IL-17A(+) Th17, GM-CSF(+) Th, MDSCs and Treg, through inhibition of IL-6 secretion. Moreover, Embelin decrease IL-6-induced STAT3 phosphorylation.
    In summary, Embelin represents a novel therapeutic drug candidate for the clinical treatment of pancreatic cancer.