TMPyP4 tosylate
Based on 10 publication(s) in Google Scholar
TMPyP4 tosylate (TMP 1363) is a quadruplex-specific ligand. TMPyP4 tosylate inhibits the interaction between G-quadruplexes and IGF-1. TMPyP4 tosylate is a telomerase inhibitor and inhibits cancer cells proliferation. TMPyP4 tosylate is also a stabilizer of nucleic acid secondary structure and an acetylcholinesterase inhibitor. Besides, TMPyP4 tosylate has antiviral activity against SARS-CoV-2.
For research use only. We do not sell to patients.
- Purity: 98.0%
- CAS No.: 36951-72-1
- Formula: C72H66N8O12S4
- Molecular Weight:1363.60
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) TMPyP4 tosylate
More- Mol Cell. 2024 Jun 6;84(11):2070-2086.e20. [Abstract]
- Nat Commun. 2026 Feb 23;17(1):3076. [Abstract]
- Nat Commun. 2024 Oct 4;15(1):8602. [Abstract]
- Nucleic Acids Res. 2026 Jan 14;54(2):gkaf1481. [Abstract]
- Cell Death Dis. 2024 Nov 11;15(11):816. [Abstract]
- Int J Biol Macromol. 2025 Jan 9:139582. [Abstract]
- Anal Chem. 2025 Jun 10;97(22):11617-11626. [Abstract]
- Microbiol Spectr. 2022 Apr 21;e0046022. [Abstract]
- Biochemistry. 2024 Oct 15;63(20):2609-2620. [Abstract]
- Virology. 2024 Dec 24:603:110378. [Abstract]
Customer Validation & Images
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
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Flow Cytometry
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In Vivo Efficacy Study
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Bio/Physico-chemical Assay
Biological Activity
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AChE |
G-quadruplex |
Telomerase |
SARS-CoV-2 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
>100 μM
Compound: 71
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Cytotoxicity against human A549 cells assessed as cell growth inhibition by WST assay
Cytotoxicity against human A549 cells assessed as cell growth inhibition by WST assay
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[PMID: 35050607] |
| A549 | IC50 |
0.3 μM
Compound: 71
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Photodynamic cytotoxicity against human A549 cells assessed as cell growth inhibition upon light irradiation by WST assay
Photodynamic cytotoxicity against human A549 cells assessed as cell growth inhibition upon light irradiation by WST assay
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[PMID: 35050607] |
| Bone marrow cell | GI50 |
16.8 μM
Compound: TMPyP4
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Antiproliferative activity against human bone marrow cells after 72 hrs by WST-1 assay
Antiproliferative activity against human bone marrow cells after 72 hrs by WST-1 assay
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[PMID: 27132164] |
| HeLa | IC50 |
0.06 μM
Compound: 6, TMPyP4
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Inhibition of telomerase in human HeLa cells using 5'-AAT CCG TCG AGC AGA GTT-3' as substrate incubated for 15 mins prior to extension reaction by telomeric repeat amplification protocol
Inhibition of telomerase in human HeLa cells using 5'-AAT CCG TCG AGC AGA GTT-3' as substrate incubated for 15 mins prior to extension reaction by telomeric repeat amplification protocol
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[PMID: 22413845] |
| HeLa | IC50 |
0.147 μM
Compound: 6, TMPyP4
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Inhibition of telomerase in human HeLa cells using 5'-AAT CCG TCG AGC AGA GTT-3' as substrate incubated for 15 mins prior to extension reaction followed by compound washout by spin-telomeric repeat amplification protocol
Inhibition of telomerase in human HeLa cells using 5'-AAT CCG TCG AGC AGA GTT-3' as substrate incubated for 15 mins prior to extension reaction followed by compound washout by spin-telomeric repeat amplification protocol
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[PMID: 22413845] |
| MDA-MB-231 | GI50 |
14.3 μM
Compound: TMPyP4
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Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by WST-1 assay
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by WST-1 assay
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[PMID: 27132164] |
| MRC5 | IC50 |
>25 μM
Compound: TMPyP4
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Cytotoxicity against human MRC5 cells assessed as cell growth inhibition after 72 hrs by MTT assay
Cytotoxicity against human MRC5 cells assessed as cell growth inhibition after 72 hrs by MTT assay
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[PMID: 29323491] |
| OVCAR-3 | GI50 |
14.6 μM
Compound: TMPyP4
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Antiproliferative activity against human OVCAR3 cells after 72 hrs by WST-1 assay
Antiproliferative activity against human OVCAR3 cells after 72 hrs by WST-1 assay
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[PMID: 27132164] |
| PC-3 | GI50 |
14 μM
Compound: TMPyP4
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Antiproliferative activity against human PC3 cells after 72 hrs by WST-1 assay
Antiproliferative activity against human PC3 cells after 72 hrs by WST-1 assay
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[PMID: 27132164] |
| ScN2a | IC50 |
130 nM
Compound: TMPyP
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Inhibition of PrP-res formation in mouse ScN2a cells relative to control
Inhibition of PrP-res formation in mouse ScN2a cells relative to control
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[PMID: 16987659] |
TMPyP4 tosylate (50 µM, 96 h) inhibits telomerase activity in telomerase positive HOS cells[2].
TMPyP4 tosylate (50 µM, 48 or 96 h) inhibits the growth of HOS cells[2].
TMPyP4 tosylate (50 µM, 96 h) induces cell apoptosis in HOS, Saos-2, MG-63, and U2OS cell lines[2].
TMPyP4 tosylate (100 µM, 24 or 48 h) increases cell cycle regulatory proteins and MAPKs in K562 cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HOS cells
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Concentration:50 µM
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Incubation Time:48 or 96 h
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Result:Time-dependently inhibited cell viability.
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Cell Line:K562 cells
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Concentration:100 µM
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Incubation Time:24 or 48 h
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Result:Increased the expression of p21CIP1 protein and p57KIP2 protein.
TMPyP4 tosylate (15 mg/kg or 30 mg/kg, i.n.) decreases the mean viral loads in SARS-CoV-2-infected hamster[6].
TMPyP4 tosylate (30 mg/kg, i.n., hamsters) shows a Cmax of 17.88 μg/mL at 1 h, and a half-life (T1/2) of 6.36 h[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MX-1 mammary chemoadjuvant model[5]
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Dosage:10 and 20 mg/kg
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Administration:Intraperitoneal injection (i.p.), twice weekly.
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Result:Inhibited tumor growth and prolonged mice survival.
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Animal Model:SARS-CoV-2-infected hamster[6]
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Dosage:15 mg/kg or 30 mg/kg
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Administration:i.n., starting at 1 h prior to virus inoculation and continuing until 3 days post infection
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Result:Decreased the mean viral loads in the nasal wash, nasal turbinate and lung tissues.
Chemical Information
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CAS No. 36951-72-1
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Appearance Solid
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Molecular Weight 1363.60
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Formula C72H66N8O12S4
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Color Purple to dark purple
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SMILES
C[N+]1=CC=C(/C2=C3C=CC(/C(C4=CC=[N+](C)C=C4)=C5C=C/C(N/5)=C(C6=CC=[N+](C)C=C6)/C(C=C/7)=NC7=C(C8=CC=[N+](C)C=C8)/C9=CC=C2N9)=N\3)C=C1.O=S(C%10=CC=C(C)C=C%10)([O-])=O.O=S(C%11=CC=C(C)C=C%11)([O-])=O.O=S(C%12=CC=C(C)C=C%12)([O-])=O.O=S(C%13=CC=C(C)C=C%13)([O-])=O
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Synonyms
TMP 1363
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (10)
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Journal Impact Factor
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Most Recent
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Mol Cell
The MYCN oncoprotein is an RNA-binding accessory factor of the nuclear exosome targeting complex. [Abstract]2024 Jun 6;84(11):2070-2086.e20. PMID: 38703770 -
Nat Commun
2026 Feb 23;17(1):3076. PMID: 41730904 -
Nat Commun
The G4 resolvase Dhx36 modulates cardiomyocyte differentiation and ventricular conduction system development. [Abstract]2024 Oct 4;15(1):8602. PMID: 39366945
TMPyP4 tosylate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Oct 4;15(1):8602. [Abstract]
Luciferase transcriptional activation assays in HeLa cells of promoter regions of Dhx36, Kcne1, Bcl2l11, Ntn1, Ppargc1a (Pgc1a), Fhl2, and Nr4a1 cloned in pGL4.25 luciferase expressing vector. The luciferase activity, measured in Relative light units (R.L.U.) of the different constructs, are shown in the presence or absence of the G4 stabilization drug TMPyP4 tosylate (20 μM; 24 h).
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Nucleic Acids Res
RNA G-quadruplexes promote codon repeat-associated ribosomal frameshifting in human genes. [Abstract]2026 Jan 14;54(2):gkaf1481. PMID: 41543171
TMPyP4 tosylate purchased from MedChemExpress. Usage Cited in: Nucleic Acids Res. 2026 Jan 14;54(2):gkaf1481. [Abstract]
Treatment with TMPyP4 tosylate (2 μM; 26 h) resulted in a 14.18% reduction in the HDAC1 frameshifting ratio in HEK293T cells, whereas the mut1 rG4 mutant exhibited only a minimal reduction (1.88%) compared with the control group.
TMPyP4 tosylate purchased from MedChemExpress. Usage Cited in: Nucleic Acids Res. 2026 Jan 14;54(2):gkaf1481. [Abstract]
The G4-destabilizing porphyrin TMPyP4 tosylate (1-100 μM) induced a concentration-dependent shift in the spectral peak, indicating a transition of the higher order HDAC1 RNA structure to a linear form. Moreover, the high concentration (100 μM) of TMPyP4 disrupted the standard CD spectrum of the G4 structure.
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Cell Death Dis
Targeting G-quadruplex by TMPyP4 for inhibition of colorectal cancer through cell cycle arrest and boosting anti-tumor immunity. [Abstract]2024 Nov 11;15(11):816. PMID: 39528472
TMPyP4 tosylate purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2024 Nov 11;15(11):816. [Abstract]
TMPyP4 tosylate (4-8 μM; 48 h) induced a significant increase in apoptosis in CRC cell lines.
TMPyP4 tosylate purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2024 Nov 11;15(11):816. [Abstract]
TMPyP4 tosylate (30 mg/kg; i.p.; three times a week) markedly decreased tumor weights and volumes of BALB/c nude mice bearing SW620 colorectal tumors.
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Int J Biol Macromol
2025 Jan 9:139582. PMID: 39798757 -
Anal Chem
2025 Jun 10;97(22):11617-11626. PMID: 40408126 -
Microbiol Spectr
Characterization of G-Quadruplexes in Enterovirus A71 Genome and Their Interaction with G-Quadruplex Ligands. [Abstract]2022 Apr 21;e0046022. PMID: 35446122 -
Biochemistry
G-Quadruplex-Mediated Transcriptional Regulation of SYT7: Implications for Tumor Progression and Therapeutic Strategies. [Abstract]2024 Oct 15;63(20):2609-2620. PMID: 39320967 -
Virology
The UP1 domain is essential for the facilitation effect of HnRNP A1 on PRRSV-2 replication. [Abstract]2024 Dec 24:603:110378. PMID: 39731905
Solvent & Solubility
DMSO : 10 mg/mL (7.33 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 5 mg/mL (3.67 mM; ultrasonic and warming and heat to 60°C)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1 mg/mL (0.73 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1 mg/mL (0.73 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 7.14 mg/mL (5.24 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (291 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[1]. Chen H, et al. Insuline-like growth factor type I selectively binds to G-quadruplex structures. Biochim Biophys Acta Gen Subj. 2019 Jan;1863(1):31-38. [Content Brief]
[2]. Fujimori J, et al. Antitumor effects of telomerase inhibitor TMPyP4 in osteosarcoma cell lines. J Orthop Res. 2011 Nov;29(11):1707-11. [Content Brief]
[3]. Fujiwara N, et al. a Stabilizer of Nucleic Acid Secondary Structure, Is a Novel Acetylcholinesterase Inhibitor. PLoS One. 2015 Sep 24;10(9):e0139167. [Content Brief]
[4]. Mikami-Terao Y, et al. Antitumor activity of G-quadruplex-interactive agent TMPyP4 in K562 leukemic cells. Cancer Lett. 2008 Mar 18;261(2):226-34. [Content Brief]
[5]. Grand CL, et al. The cationic porphyrin TMPyP4 down-regulates c-MYC and human telomerase reverse transcriptase expression and inhibits tumor growth in vivo. Mol Cancer Ther. 2002 Jun;1(8):565-73. Erratum in: Mol Cancer Ther.2003 Feb;2(2):208. [Content Brief]
[6]. Qin G, et al. RNA G-quadruplex formed in SARS-CoV-2 used for COVID-19 treatment in animal models. Cell Discov. 2022 Sep 6;8(1):86. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 0.7334 mL | 3.6668 mL | 7.3335 mL | 18.3338 mL |
| DMSO | 5 mM | 0.1467 mL | 0.7334 mL | 1.4667 mL | 3.6668 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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