Description
Epithalon (also known as Epitalon) is a synthetic tetrapeptide research reagent (Ala-Glu-Asp-Gly) based on the analysis of amino acid sequences found in the pineal gland. It is primarily utilized in gerontological research as a potent “geroprotector” due to its ability to interact with the epigenome and induce telomerase activity.
In laboratory settings, Epithalon is a critical tool for studying the “Hayflick limit”—the number of times a normal human cell population will divide before cell division stops. Research indicates that Epithalon can overcome this division limit in human somatic cells by promoting the elongation of telomeres, the protective caps at the ends of chromosomes. Additionally, it is investigated for its role in regulating antioxidant defense systems and restoring hormonal sensitivity in aged models.
Biochemical Characteristics
Chemically, Epithalon is the tetrapeptide L-alanyl-L-glutamyl-L-aspartyl-glycine. It acts as a gene-switch modulator, initiating specific protein synthesis pathways.
- Sequence/Structure: Ala-Glu-Asp-Gly (AEDG).
- Permeability: Its small molecular size allows for rapid nuclear uptake, facilitating interaction with DNA and telomerase components.
- Stability: Supplied as a lyophilized salt to ensure structural integrity and prevent degradation of the peptide sequence during storage.
- Specificity: Highly specific for the upregulation of telomerase activity and the repression of specific oncogenes (e.g., HER-2/neu) in experimental models.
Chemical Properties
| Property |
Specification |
| Molecule Name |
Epithalon |
| Synonyms |
Epitalon; AGAG; Ala-Glu-Asp-Gly |
| Sequence |
Ala-Glu-Asp-Gly |
| CAS Number |
307297-39-8 |
| Molecular Formula |
C14H22N4O9 |
| Molecular Weight |
390.35 g/mol |
| Form |
Lyophilized Powder |
| Purity |
≥99% (Verified via HPLC) |
| Solubility |
Soluble in water and organic solvents (refer to SDS) |
| Documentation |
COA available per lot; SDS available |
Epithalon is strictly for laboratory research and is commonly employed in the following investigational areas:
Telomere Biology and Cellular Senescence
Epithalon is the gold-standard peptide for inducing telomerase activity in culture. Researchers use it to study the mechanisms of telomere elongation and the retardation of cellular senescence in human somatic cells. It is utilized to investigate the potential for extending the proliferative lifespan of cells beyond their natural division limits.
Oncology and Tumor Suppression
The peptide is used in oncology research to study its inhibitory effects on spontaneous tumor incidence and specific carcinogenesis models. Studies involve measuring the expression of oncogenes (such as HER-2/neu) and observing tumor progression in colon and breast cancer models.
Lifespan and Aging Models
Epithalon is frequently employed in longevity studies using Drosophila melanogaster and rodent models. Researchers quantify changes in biomarkers of aging, mean lifespan, and the incidence of age-related pathologies to evaluate the peptide’s geroprotective potential.
Reproductive Aging
Recent investigations utilize Epithalon to study post-ovulatory aging. In mouse oocyte models, the peptide is applied to observe its protective effects against oxidative damage and chromosomal abnormalities, providing data on the preservation of gamete quality.
Pathway / Mechanistic Context
The primary mechanism of action for Epithalon involves epigenetic regulation and enzymatic activation.
- Telomerase Activation: Epithalon induces the expression of the catalytic subunit of telomerase, leading to the synthesis of telomeric DNA repeats at the ends of chromosomes.
- Chromatin Stabilization: By maintaining telomere length, the peptide helps prevent chromosome aberrations and genomic instability often associated with aging.
- Antioxidant Regulation: Epithalon modulates the activity of antioxidant enzymes (SOD, peroxidase), enhancing the cell’s resistance to reactive oxygen species (ROS).
Preclinical Research Summary
Published preclinical literature documents investigations of Epithalon across multiple experimental models:
- Telomere Elongation: Studies in human somatic cells demonstrated that Epithalon treatment induced telomerase activity and elongated telomeres, effectively increasing the number of population doublings.
- Tumor Inhibition: Research in transgenic mice showed that Epithalon inhibited the growth of breast tumors and downregulated the expression of the HER-2/neu oncogene. Similarly, it demonstrated an inhibitory effect on colon carcinogenesis in rat models.
- Lifespan Extension: Experiments with Drosophila melanogaster and Swiss-derived SHR mice indicated that Epithalon administration significantly increased mean lifespan and reduced the frequency of spontaneous tumors.
Form & Analytical Testing
This material is produced via robust chemical synthesis and supplied as a lyophilized (freeze-dried) powder.
- Lyophilization: Removes water content under vacuum to maintain compound integrity and extend shelf-life.
- Identity Verification: Each lot undergoes Mass Spectrometry (MS) to confirm molecular weight and sequence identity.
- Purity Verification: High-Performance Liquid Chromatography (HPLC) is performed to ensure the product meets the ≥99% purity standard required for reproducible research data.
Referenced Citations
References are provided for informational purposes only and are not clinical claims.
- Khavinson, V., Bondarev, I., & Butyugov, A. (2003). Epithalon Peptide Induces Telomerase Activity and Telomere Elongation in Human Somatic Cells. Bulletin of Experimental Biology and Medicine, 135, 590-592. https://doi.org/10.1023/A:1025493705728
- Shi-Liang, T. (2007). Retarding the cellular senescence by Epithalon and changes of telomere length and telomerase activity in the retarding process. Journal of Chongqing College of Education.
- Anisimov, V., et al. (2004). Effect of Epitalon on biomarkers of aging, life span and spontaneous tumor incidence in female Swiss-derived SHR mice. Biogerontology, 4, 193-202. https://doi.org/10.1023/A:1025114230714
- Khavinson, V., Izmaylov, D., Obukhova, L., & Malinin, V. (2000). Effect of epitalon on the lifespan increase in Drosophila melanogaster. Mechanisms of Ageing and Development, 120, 141-149. https://doi.org/10.1016/S0047-6374(00)00217-7
- Khavinson, V., Bondarev, I., Butyugov, A., & Smirnova, T. (2004). Peptide Promotes Overcoming of the Division Limit in Human Somatic Cell. Bulletin of Experimental Biology and Medicine, 137, 503-506. https://doi.org/10.1023/B:BEBM.0000038164.49947.8c
- Rosenfeld, S., et al. (2002). Effect of Epithalon on the Incidence of Chromosome Aberrations in Senescence-Accelerated Mice. Bulletin of Experimental Biology and Medicine, 133, 274-276. https://doi.org/10.1023/A:1015899003974
- Yue, X., et al. (2022). Epitalon protects against post-ovulatory aging-related damage of mouse oocytes in vitro. Aging (Albany NY), 14, 3191 – 3202. https://doi.org/10.18632/aging.204007
- Goncharova, N., Vengerin, A., Khavinson, V., & Lapin, B. (2005). Pineal peptides restore the age-related disturbances in hormonal functions of the pineal gland and the pancreas. Experimental Gerontology, 40, 51-57. https://doi.org/10.1016/j.exger.2004.10.004
- Khavinson, V., & Malinin, V. (2005). Gerontological Aspects of Genome Peptide Regulation. https://doi.org/10.1159/isbn.978-3-318-01193-7
- Kozina, L., Arutjunyan, A., & Khavinson, V. (2007). Antioxidant properties of geroprotective peptides of the pineal gland. Archives of Gerontology and Geriatrics, 44 Suppl 1, 213-6. https://doi.org/10.1016/J.ARCHGER.2007.01.029
- Anisimov, V., et al. (2002). Epithalon Inhibits Tumor Growth and Expression of HER-2/neu Oncogene in Breast Tumors in Transgenic Mice Characterized by Accelerated Aging. Bulletin of Experimental Biology and Medicine, 133, 167-170. https://doi.org/10.1023/A:1015555023692
- Anisimov, V., Khavinson, V., Popovich, I., & Zabezhinski, M. (2002). Inhibitory effect of peptide Epitalon on colon carcinogenesis induced by 1,2-dimethylhydrazine in rats. Cancer Letters, 183 1, 1-8. https://doi.org/10.1016/S0304-3835(02)00090-3
RESEARCH USE ONLY
This product is intended strictly for laboratory research use only. It is not for human or veterinary use. It is not intended for diagnosis, treatment, cure, or prevention of any disease. All purchases are subject to our Terms of Service and Purity Guarantee.
No COAs available for this product.
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