Epithalon 50mg

Compound Name: Epithalon

Synonyms: Ala-Glu-Asp-Gly; epithalone; pineal peptide tetrapeptide

CAS Number: 307297-39-8

Molecular Formula: C₁₄H₂₂N₄O₉

Molecular Weight: ~390.35 g/mol

Structure: Synthetic tetrapeptide

Peptide Sequence: H-Ala-Glu-Asp-Gly-OH

Chemical Structure:

Source: PubChem

Mechanism of Action: Epithalon functions by upregulating telomerase reverse tranceiptase (TERT) activity in somatic cells, which promotes telomere elongation and chromosomal stability. It also suppresses expression of certain oncogenes such as HER-2/neu, contributing to its antitumor effects. Additionally, Epithalon reduces oxidative stress and restores circadian melatonin secretion rhythms in aged animals^2,3.

Biological Activity: Epithalon has been shown to increase lifespan in rodent models, reduce spontaneous and induced tumor formation, stabilize the genome by reducing chromosomal aberrations, and modulate immune cell proliferation. Its actions extend to radioprotective effects on the thymus and intestinal mucosa^1,4.

Storage: −20°C or below. Protect from light and moisture.

Drug Categories: Peptides; Bioregulators; Geroprotective Compounds

Additional Notes:

• Originally synthesized at the St. Petersburg Institute of Bioregulation and Gerontology.
• Noted for unique pineal gland regulatory function and epigenetic modulation potential.
• Epithalon is a research-use-only compound. It is not FDA-approved and has not completed full clinical trials. It is supplied for laboratory investigation only and is not intended for diagnostic or therapeutic use in humans.

Summary Table:

Disclaimer: For Research Use Only. Not intended for human or veterinary use. This compound is supplied solely for laboratory and R&D purposes.

Detailed Product Description

Epithalon is a stabilized synthetic tetrapeptide analogue of the endogenous pineal peptide epithalamin. It was developed to replicate and enhance the biological functions of pineal-derived factors that regulate aging and genome integrity. Preclinical studies have demonstrated that Epithalon activates telomerase in somatic cells through activation of telomerase reverse transcriptase, which promotes telomere elongation, and delays cellular senescence. These mechanisms are believed to underpin its geroprotective effects¹. Epithalon has been extensively evaluated in aging-prone and cancer-prone rodent models, where it has been shown to reduce spontaneous tumor formation, suppress oncogene expression (notably HER-2/neu), and increase median and maximal lifespan^1,2. The peptide also restores melatonin secretion rhythms in aged animals and stabilizes genomic integrity by reducing age-associated chromosomal aberrations. While not approved for human use, epithalon is actively used in laboratory research on aging, cancer biology, and radioprotection. It is intended solely for investigational applications involving cellular senescence, telomerase modulation, and epigenetic reprogramming in experimental models of aging and age-related disease^3,4.

Research Highlights

Epithalon’s action on TERT and HER-2/neu has shown multiple clinically relevant outcomes:

• Lifespan Extension: Increased lifespan in CBA and SAMP-1 mice compared to controls¹.
• Antitumor Effects: Reduced spontaneous and induced tumor growth in multiple murine models⁴.
• HER-2/neu Suppression: Decreased oncogene expression and tumor burden in transgenic mice⁴.
• Radioprotection: Promotes regeneration in radiosensitive organs post-irradiation (e.g., thymus, spleen).
• Genomic Stability: Lower incidence of chromosomal mutations in aging models³.

• Circadian Regulation: Restores melatonin rhythmicity in aged animals¹.

Mechanism of Action

Epithalon’s geroprotective and antineoplastic effects are mediated through two principal genomic mechanisms: activation of telomerase reverse transcriptase (TERT) and transcriptional downregulation of the HER-2/neu proto-oncogene^1,2,3.

1. Activation of Telomerase Reverse Transcriptase (TERT)

Epithalon induces the expression and activity of telomerase reverse transcriptase in somatic cells, promoting elongation of telomeric DNA repeats at chromosomal termini. Telomere attrition is a hallmark of replicative senescence and genomic instability, particularly in highly mitotic tissues⁴. By sustaining telomere integrity, Epithalon enhances proliferative capacity, reduces the incidence of chromosomal aberrations, and preserves nuclear genomic architecture in aging cells. In senescence-accelerated murine models, TERT activation by Epithalon correlates with increased median and maximal lifespan, reduced incidence of cytogenetic anomalies in bone marrow metaphases, and improved resistance to oxidative and genotoxic stress^2,4.

2. Downregulation of HER-2/neu Expression

In transgenic FVB/N mice overexpressing the human HER-2/neu (erbB-2) oncogene, Epithalon administration results in a significant reduction in HER-2/neu mRNA levels, with a reported 3.7-fold decrease relative to saline controls. HER-2/neu encodes a receptor tyrosine kinase involved in mitogenic signaling via the MAPK and PI3K/AKT pathways and is implicated in the pathogenesis of multiple epithelial malignancies, including breast carcinoma. Epithalon’s suppression of HER-2/neu expression is associated with delayed tumor onset, reduced tumor multiplicity, and decreased tumor volume. These data suggest a transcriptional regulatory mechanism through which Epithalon modulates oncogenic signaling and suppresses neoplastic progression in HER-2-driven tumorigenesis⁴.

Pharmacokinetic Profile:

• Route of Administration: Subcutaneous injection
• Dosing Frequency: Once daily
• Half-Life: Not formally established in humans; estimated short plasma half-life typical of small peptides (minutes to low hours)².
• Formulation: Lyophilized powder for reconstitution

Formulation & Handling

• Lyophilized peptide powder, reconstituted in sterile PBS or water.
• Store lyophilized peptide at –20 °C; upon reconstitution, aliquot and freeze at –80 °C to avoid degradation.
• Avoid repeated freeze–thaw cycles.

Selected Clinical Trial Activity

Epithalon is a research-grade compound that has been studied in laboratory settings but has not undergone full clinical development. It is not approved for therapeutic use in humans, and no large-scale clinical trials have been conducted to evaluate its safety or efficacy as a medication. Epithalon is supplied strictly for laboratory research and investigational purposes only.

References

¹Anisimov, V. N., Khavinson, V. Kh., Alimova, I. N., Provintsiali, M., Manchini, R., & Francheski, K. Epithalon inhibits tumor growth and expression of HER-2/neu oncogene in breast tumors in transgenic mice characterized by accelerated aging. Bull Exp Biol Med. 133, 167–170 (2002).

²Rosenfeld, S.V. et al. Effect of epithalon on the incidence of chromosome aberrations in senescence-accelerated mice. Bull Exp Biol Med. 133, 274–276 (2002)

³Khavinson, V.K. et al. Immunohistochemical and morphometric analysis of effects of vilon and epithalon on functional morphology of radiosensitive organs. Bull Exp Biol Med. 131, 285–292 (2001).

⁴Anisimov, V.N. et al. Epithalon decelerates aging and suppresses development of breast adenocarcinomas in transgenic HER-2/neu mice. Bull Exp Biol Med. 134, 187–190 (2002).