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Specifications:
| Application | molecular biology | ||
| Storage Temperature | 2-8°C | ||
| Product Type | Proteins & Peptides | Forms | Solid |
| Product Brand | Selleckchem | ||
| Product Grade | Analytical grade | Formula | C₄₄H₃₈N₈ · C₂₈H₂₈O₁₂S₄ |
Potent Quadruplex-Specific Ligand & Telomerase Inhibitor
TMPyP4 tosylate (TMP 1363) is a high-purity, cationic porphyrin compound known for its quadruplex DNA-binding properties and telomerase inhibition (IC₅₀ = 6.5 µM). This compound effectively disrupts G-quadruplex and IGF-1 interactions, inhibits cancer cell proliferation, and exhibits antiviral activity against SARS-CoV-2. TMPyP4 tosylate also functions as an acetylcholinesterase (AChE) inhibitor, further expanding its potential applications in neurobiology and drug discovery.
Key Features & Benefits
✅ Telomerase Inhibition & G-Quadruplex Stabilization
- Binds & stabilizes G-quadruplex DNA, leading to telomerase inhibition.
- IC₅₀ = 6.5 µM, preventing telomere elongation in cancer cells.
✅ Anti-Cancer & Apoptotic Effects
- Inhibits proliferation of telomerase-positive HOS cells at 50 µM (96h incubation).
- Induces apoptosis in HOS, Saos-2, MG-63, and U2OS cell lines.
- Enhances cell cycle regulatory proteins & MAPKs in K562 cells (100 µM, 24–48h).
✅ Antiviral Activity Against SARS-CoV-2
- Intranasal administration (15–30 mg/kg) significantly reduces viral load in infected hamsters.
- Pharmacokinetics in hamsters: Cmax = 17.88 μg/mL at 1h, T1/2 = 6.36h.
✅ Acetylcholinesterase (AChE) Inhibition
- Potential role in neurodegenerative research targeting AChE-related pathways.
✅ High Purity & Stability
- Purity ≥98.73%, ensuring high-quality and reproducible results.
- Stable at 4°C, with extended storage at -20°C or -80°C in solvents.
Technical Specifications
| Feature | Details |
|---|---|
| Molecular Formula | C72H66N8O12S4 |
| Molecular Weight | 1363.6 g/mol |
| CAS Number | 36951-72-1 |
| Appearance | Solid, pale purple to purple powder |
| Peptide Content (by %N) | ≥80% |
| Purity (by HPLC) | ≥98.73% |
| Single Impurity (by HPLC) | ≤1.0% |
| Assay (By Anhydrous, Acetic Acid-free) | 95.0~105.0% |
| Solubility (In Vitro) | DMSO: 10 mg/mL (7.33 mM, ultrasonic needed) H2O: 5 mg/mL (3.67 mM, requires heat to 60°C & ultrasonic) |
| Storage Conditions | 4°C sealed (solid), -80°C (solvent, 6 months), -20°C (solvent, 1 month) |
| Shipping Conditions | Ambient (room temperature) in continental US; varies elsewhere |
Use Cases & Applications
1. Cancer Research & Telomerase Inhibition Studies
Primary Use:
- Investigates telomerase-dependent tumor proliferation.
- Studies quadruplex-targeting anticancer compounds.
Practical Example:
A cancer research lab uses TMPyP4 tosylate to study telomerase inhibition in glioblastoma cells, identifying potential therapeutic approaches for targeting telomerase-dependent tumors.
2. G-Quadruplex & DNA Structural Research
Primary Use:
- Stabilizes G-quadruplex DNA structures, disrupting oncogene regulation.
- Enables fluorescence-based quadruplex detection assays.
Practical Example:
A molecular biology team applies TMPyP4 in fluorescence-based assays to investigate quadruplex formation in MYC and KRAS promoters, leading to new drug targets for cancer therapy.
3. Antiviral Research (SARS-CoV-2 & Emerging Viruses)
Primary Use:
- Evaluates TMPyP4 as an antiviral agent against coronaviruses.
- Assesses G-quadruplex stabilization in viral RNA structures.
Practical Example:
A virology lab studying SARS-CoV-2 tests TMPyP4 tosylate (30 mg/kg, i.n.) in infected hamsters, observing reduced viral loads and improved survival outcomes.
4. Acetylcholinesterase (AChE) Inhibition & Neurodegenerative Research
Primary Use:
- Investigates AChE inhibition as a potential Alzheimer's treatment.
- Explores quadruplex-targeted gene regulation in neuronal pathways.
Practical Example:
A neuroscience lab tests TMPyP4 in AChE activity assays, identifying potential neuroprotective properties for Alzheimer’s disease research.
5. Preclinical Drug Development & Pharmacokinetics
Primary Use:
- Supports preclinical drug screening for telomerase-targeted cancer therapies.
- Assesses TMPyP4 pharmacokinetics in animal models.
Practical Example:
A pharmaceutical company conducting telomerase inhibitor trials uses TMPyP4 tosylate in xenograft mouse models, studying tumor inhibition and bioavailability.
Why Choose Selleckchem TMPyP4 Tosylate?
🔬 Selective Telomerase & Quadruplex Inhibition – Blocks telomerase function & disrupts oncogene regulation.
💡 Quadruplex Fluorescent Probe – Enables visualization of G-quadruplex DNA interactions.
⚡ Anticancer & Antiviral Applications – Targets tumor cells and SARS-CoV-2 replication pathways.
📈 High Purity & Reproducibility – ≥98.73% purity ensures consistent experimental results.
🛡 Stable & Easy to Handle – Long shelf life, with multiple storage options for extended usability.
TMPyP4 tosylate is a highly potent telomerase inhibitor and G-quadruplex stabilizer, making it a valuable tool in cancer research, drug discovery, virology, and neurobiology. With its fluorescent binding to quadruplex DNA, anticancer activity, and antiviral potential, TMPyP4 is a powerful compound for preclinical drug development and molecular biology research.
- Pack Size: 100mg 25mg