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    Ellagic acid
    Ellagic acid

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1403
    CAS #: 476-66-4Purity ≥98%

    Description: Ellagic acid (Elagostasine, Gallogen; Alizarine Yellow; Benzoaric acid; CCRIS-774; HSDB-7574; Lagistase), the dilactone of hexahydroxydiphenic acid, is a naturally occuring phenol and an antioxidant found in numerous fruits and vegetables. It has antiproliferative and antioxidant properties in a number of in vitro and small-animal models. The antiproliferative and antioxidant properties of ellagic acid have prompted research into its potential health benefits. The antiproliferative properties of ellagic acid may be due to its ability to directly inhibit the DNA binding of certain carcinogens, including nitrosamines and polycyclic aromatic hydrocarbons.

    References: J Nutr Biochem. 2005;16(6):360-7; Cancer Lett. 1999;136(2):215-21; Carcinogenesis. 1988;9(7):1313-6.

    Related CAS: 314041-08-2 (hydrate)

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    Molecular Weight (MW)302.19 
    CAS No.476-66-4 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 3 mg/mL (9.9 mM) 
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Other info

    Chemical Name: 2,3,7,8-tetrahydroxychromeno[5,4,3-cde]chromene-5,10-dione


    InChi Code: InChI=1S/C14H6O8/c15-5-1-3-7-8-4(14(20)22-11(7)9(5)17)2-6(16)10(18)12(8)21-13(3)19/h1-2,15-18H

    SMILES Code: O=C1C2=CC(O)=C(O)C(O3)=C2C4=C(C3=O)C=C(O)C(O)=C4O1           

    SynonymsElagostasine, Gallogen; Alizarine Yellow; Benzoaric acid; CCRIS 774; HSDB 7574; CCRIS774; HSDB7574; CCRIS-774; HSDB-7574; Lagistase;

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    In Vitro

    In vitro activity: Ellagic acid is a potent and natural CK2 inhibitor, with an IC50 of 40 nM and a Ki of 20 nM. Ellagic acid also blocks other kinases such as LYN, PKA, SYK, GSK3, FGR and CK1, with IC50s of 2.9, 3.5, 4.3, 7.5, 9.4 and 13.0 μM, respectively, and shows no obvious effects on DYRK1a, CSK, NPM-ALK, RET and FLT3 (IC50s > 40 μM). Ellagic acid (5-100 μM) shows inhibitory activities against Karpas299, SUDHL1, SR786, and FE-PD cell lines[1]. Ellagic acid (10 μM) exhibits cytotoxic effects on MCF-7 cells after treatment of radiation. Ellagic acid (10 μM) in combination with Irradiation (IR) significantly abridges the capacity of MCF-7 cells to form colonies equated with individual treatments. Ellagic acid with IR also induces cell apoptosis, and facilitates the upregulation of pro-apopttotic Bax and downregulation of Bcl-2 in MCF-7 cells

    Kinase Assay: CK2 and CK1 phosphorylation assays are carried out at 37°C in the presence of increasing amounts of each inhibitor (Ellagic acid) in a final volume of 25 µL containing 50 mM, Tris-HCl pH 7.5, 100 mM NaCl, 12 mM MgCl2, 0.02 mM [33P-ATP] (500-1000 cpm/pmol), unless otherwise indicated. The phosphorylatable substrates are the synthetic peptide substrate RRRADDSDDDDD (100 µM) and RRKHAAIGDDDDAYSITA (200 µM) for CK2 and CK1, respectively. Reaction started with the addition of the kinase and is stopped after 10 min. by addition of 5 µL of 0.5 M orthophosphoric acid before spotting aliquots onto phosphocellulose filters. Filters are washed in 75 mM phosphoric acid substrate following SDS-PAGE of the radiolabeled samples. DYRK1A, assayed on the peptide RRRFRPASPLRGPPK, and tyrosine kinase activities are determined

    Cell Assay: ALCL cell viability is measured by MTT assay. Briefly, 0.1 × 105 cells are seeded onto 96-well microculture plates 12 hrs before adding ellagic acid. The cells are grown in 200 µL of complete RPMI-1640 medium, under standard tissue-culture conditions, in the presence or absence of the drug (Ellagic acid) for 48 hours. Twenty µL of MTT solution (5 mg/mL) are then added to the cell suspension for 4h. The intracellular formazan crystals are dissolved with 150 µL of DMSO and optical density, measured on a spectrophotometer at 540 nm, represents the mean (± SD) of triplicate cultures.

    In VivoEllagic acid (EA; 10 mg/kg/day; p.o., 14 days) strongly decreases MDA brain content by 17%, and reduces the levels of brain TNF-α by 42% in rats. Ellagic acid markedly increases the reduced brain contents of 5-HT (39%), dopamine (DA, 71%), and norepinephrine (NE, 77%). Ellagic acid (10 mg/kg, p.o., 14 days) causes decreased histopathological changes induced by Doxorubicin in rats.
    Animal modelRats
    Formulation & Dosage10 mg/kg/day; p.o.
    References[1]. Cozza G, et al. Identification of ellagic acid as potent inhibitor of protein kinase CK2: a successful example of a virtual screening application. J Med Chem. 2006 Apr 20;49(8):2363-6.

    These protocols are for reference only. InvivoChem does not independently validate these methods.


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