Potent G-Quadruplex Stabilizer & Telomerase Inhibitor

TMPyP4 tosylate is a quadruplex-specific ligand known for its ability to stabilize nucleic acid secondary structures, particularly G-quadruplex DNA. It acts as a telomerase inhibitor and has been shown to inhibit cancer cell proliferation, modulate acetylcholinesterase (AChE), and exhibit antiviral activity against SARS-CoV-2. TMPyP4 tosylate also interferes with the IGF-1 and G-quadruplex interaction, playing a critical role in oncogenic signaling pathways.

Key Features & Benefits

✅ Telomerase Inhibitor & Antitumor Agent

• Inhibits telomerase activity in telomerase-positive HOS cells (IC₅₀ = 6.5 µM).
• Suppresses cancer cell growth & induces apoptosis in various cell lines (HOS, Saos-2, MG-63, U2OS).

✅ G-Quadruplex DNA Stabilization

• Enhances quadruplex formation, which contributes to oncogene suppression.
• Disrupts telomere maintenance, making it a potential anticancer strategy.

✅ Acetylcholinesterase (AChE) Inhibitor

• Regulates cholinergic neurotransmission, with potential implications in neurodegenerative disease research.

✅ Antiviral Activity Against SARS-CoV-2

• Demonstrates in vivo efficacy by reducing viral loads in infected hamsters.
• Pharmacokinetic profile indicates a Cmax of 17.88 μg/mL at 1h and a half-life of 6.36 h (30 mg/kg, i.n.).

✅ Highly Pure & Stable

• Purity ≥98.0%, ensuring reliable experimental reproducibility.
• Available as a pale purple to purple solid for high-precision research applications.

Technical Specifications

Use Cases & Applications

1. Cancer Research & Telomerase Inhibition

Primary Use:

• Investigates telomerase-targeting anticancer therapies.
• Suppresses telomere elongation in tumor cells.

Practical Example:

A cancer research lab treats osteosarcoma (HOS) cells with TMPyP4 tosylate (50 μM, 96 h) and observes telomerase inhibition and apoptosis, identifying its therapeutic potential.

2. DNA G-Quadruplex Structural Studies

Primary Use:

• Analyzes quadruplex DNA stabilization in oncogene regulation.
• Used in high-throughput screening for G-quadruplex binding drugs.

Practical Example:

A genomics research team applies TMPyP4 tosylate in fluorescence-based DNA assays to evaluate G-quadruplex formation in MYC oncogene promoters, helping to develop novel cancer therapeutics.

3. Antiviral Research (SARS-CoV-2 & Beyond)

Primary Use:

• Investigates quadruplex-stabilizing antiviral agents.
• Reduces SARS-CoV-2 viral loads in preclinical models.

Practical Example:

A virology team administers TMPyP4 tosylate (30 mg/kg, intranasally) to SARS-CoV-2-infected hamsters, observing a significant decrease in viral loads, demonstrating its antiviral potential.

4. Acetylcholinesterase (AChE) Inhibition & Neurobiology

Primary Use:

• Explores AChE inhibition for potential applications in Alzheimer’s disease research.
• Supports cholinergic neurotransmission studies.

Practical Example:

A neurology lab examines TMPyP4 tosylate's effect on AChE in vitro, exploring its potential therapeutic role in neurodegenerative diseases.

5. Preclinical Drug Discovery & Pharmacokinetics

Primary Use:

• Supports preclinical evaluation of telomerase inhibitors.
• Pharmacokinetic studies reveal Cmax = 17.88 μg/mL at 1h, T½ = 6.36h.

Practical Example:

A pharmaceutical company includes TMPyP4 tosylate in a telomerase inhibitor screening panel, identifying promising anticancer drug candidates.

Storage & Handling Guidelines

• Store at 4°C in sealed conditions, away from moisture.
• For solvent preparation:
  • DMSO: 10 mg/mL (sonication recommended).
  • Water: 5 mg/mL (requires ultrasonic heating to 60°C).
• Long-term storage:
  • -80°C (6 months in solvent)
  • -20°C (1 month in solvent)

Why Choose MedChem TMPyP4 Tosylate?

🔬 Selective Telomerase Inhibitor – Suppresses telomerase-positive cancer cell proliferation.

💡 Stabilizes G-Quadruplex DNA – Enhances quadruplex formation, impacting gene regulation.

⚡ Antiviral Activity Against SARS-CoV-2 – Reduces viral loads in infected animal models.

🧠 Acetylcholinesterase Inhibitor – Potential implications for neurological research.

📊 High Purity & Reliable Performance – Purity ≥98%, ensuring reproducible experimental data.

MedChem TMPyP4 tosylate (≥98.0%) is a highly potent, multi-functional research compound widely used in cancer biology, genomic studies, antiviral research, and neuroscience. Its ability to stabilize G-quadruplex DNA, inhibit telomerase, and suppress tumor growth makes it a valuable tool in drug discovery and molecular research.