TMPyP4 tosylate (Synonyms: TMP 1363)

Name: TMPyP4 tosylate
Brand: MedChemExpress
SKU: HY-108477
Rating: 5.0 (10 reviews)

Cat. No.: HY-108477 Purity: 98.0%: Data Sheet
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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.

CAS No. : 36951-72-1

Size	Stock	Quantity
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Based on 10 publication(s) in Google Scholar

10 Publications Citing Use of MCE TMPyP4 tosylate

Bio/Physico-chemical Assay

Flow Cytometry

In Vivo Efficacy Study

: 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.

: 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.

: 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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AChE BChE

Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target^[2]^[3]^[6]

AChE

G-quadruplex

Telomerase

SARS-CoV-2

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.3 μM Compound: 71	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	[PMID: 35050607]
A549	IC₅₀	> 100 μM Compound: 71	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	[PMID: 35050607]
Bone marrow cell	GI₅₀	16.8 μM Compound: TMPyP4	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	[PMID: 27132164]
HeLa	IC₅₀	0.06 μM Compound: 6, TMPyP4	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	[PMID: 22413845]
HeLa	IC₅₀	0.147 μM Compound: 6, TMPyP4	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	[PMID: 22413845]
MDA-MB-231	GI₅₀	14.3 μM Compound: TMPyP4	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	[PMID: 27132164]
MRC5	IC₅₀	> 25 μM Compound: TMPyP4	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	[PMID: 29323491]
OVCAR-3	GI₅₀	14.6 μM Compound: TMPyP4	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	[PMID: 27132164]
PC-3	GI₅₀	14 μM Compound: TMPyP4	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	[PMID: 27132164]
ScN2a	IC₅₀	130 nM Compound: TMPyP	Inhibition of PrP-res formation in mouse ScN2a cells relative to control Inhibition of PrP-res formation in mouse ScN2a cells relative to control	[PMID: 16987659]

In Vitro

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.

Cell Viability Assay^[2]

Cell Line:	HOS cells
Concentration:	50 µM
Incubation Time:	48 or 96 h
Result:	Time-dependently inhibited cell viability.

Western Blot Analysis^[4]

Cell Line:	K562 cells
Concentration:	100 µM
Incubation Time:	24 or 48 h
Result:	Increased the expression of p21^CIP1 protein and p57^KIP2 protein.

In Vivo

TMPyP4 tosylate (10 and 20 mg/kg, i.p., two times weekly) inhibits tumor growth in MX-1 tumor model^[5].
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 C_max of 17.88 μg/mL at 1 h, and a half-life (T_1/2) of 6.36 h^[6].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	MX-1 mammary chemoadjuvant model^[5]
Dosage:	10 and 20 mg/kg
Administration:	Intraperitoneal injection (i.p.), twice weekly.
Result:	Inhibited tumor growth and prolonged mice survival.

Animal Model:	SARS-CoV-2-infected hamster^[6]
Dosage:	15 mg/kg or 30 mg/kg
Administration:	i.n., starting at 1 h prior to virus inoculation and continuing until 3 days post infection
Result:	Decreased the mean viral loads in the nasal wash, nasal turbinate and lung tissues.

Molecular Weight

1363.60

Formula

C₇₂H₆₆N₈O₁₂S₄

CAS No.

36951-72-1

Appearance

Solid

Color

Purple to dark purple

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	0.7334 mL	3.6668 mL	7.3335 mL
5 mM	0.1467 mL	0.7334 mL	1.4667 mL
10 mM	---	---	---

View the 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.

* 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

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.
Protocol 2

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.

Protocol 1

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

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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

Purity: 98.0%

Select Batch:

Data Sheet (291 KB) SDS (394 KB)

COA (267 KB) HNMR (398 KB)

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

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.

TMPyP4 tosylate Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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TMPyP4 tosylate (Synonyms: TMP 1363)

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TMPyP4 tosylate Related Antibodies

10 Publications Citing Use of MCE TMPyP4 tosylate

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References

Customer Review

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Complete Stock Solution Preparation Table

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