| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
- Telomerase: TMPyP4 tosylate inhibits telomerase activity, with IC50 values of 0.8 μM (MG-63 osteosarcoma cells) [2], 1.2 μM (K562 leukemic cells) [4], and 1.0 μM (A549 lung cancer cells) [5]
- Acetylcholinesterase (AChE): It inhibits AChE with an IC50 of 3.5 μM (recombinant human AChE) [3] - SARS-CoV-2 RNA G-quadruplex: It binds to the RNA G-quadruplex structure of SARS-CoV-2 (ORF1ab region) with a dissociation constant (Kd) of 25 nM [6] - G-quadruplex structures (c-MYC promoter, telomeric DNA): It stabilizes G-quadruplexes, with a stabilization score of 0.65 (telomeric G-quadruplex) and 0.58 (c-MYC G-quadruplex) [4,5] |
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| ln Vitro |
In HOS cells, telomerase activation is inhibited by TMPyP4 tosylate (50μM, 96 hours) [2]. HOS cell proliferation is inhibited by 50μM TMPyP4 tosylate when applied over 48 or 96 hours [2]. In HOS, Saos-2, MG-63, and U2OS cell lines, TMPyP4 tosylate (50μM, 96 h) causes cell disinfection [2]. In K562 cells, TMPyP4 tosylate (100 μM, 24 or 48 hours) increases cell cycle factor proteins.
- Antitumor activity in osteosarcoma cells [2] - For MG-63 cells: TMPyP4 tosylate inhibited proliferation with an IC50 of 4.2 μM (72 h, MTT assay), reduced telomerase activity by 78% at 2 μM, and shortened telomere length by 40% after 10 passages (1 μM, continuous treatment). - For Saos-2 cells: It inhibited proliferation with an IC50 of 5.5 μM (72 h, MTT assay) and reduced telomerase activity by 65% at 2 μM. - AChE inhibitory activity [3] - It inhibited recombinant human AChE in a dose-dependent manner (IC50=3.5 μM) and rat brain AChE (IC50=4.8 μM) in vitro. It showed no significant inhibition on butyrylcholinesterase (BuChE, IC50>100 μM), indicating selectivity for AChE. - Antitumor activity in K562 leukemic cells [4] - It inhibited proliferation with an IC50 of 3.8 μM (72 h, MTT assay), induced apoptosis (35% apoptotic rate at 5 μM, Annexin V-FITC/PI staining), and downregulated c-MYC (protein level reduced by 60% at 3 μM) and hTERT (mRNA level reduced by 55% at 3 μM, qPCR). - Antitumor activity in multiple cancer cells [5] - For A549 (lung cancer) and HepG2 (liver cancer) cells: TMPyP4 tosylate inhibited proliferation with IC50 values of 4.5 μM and 5.1 μM (72 h, MTT assay), respectively. It reduced telomerase activity by 70% (A549) and 68% (HepG2) at 2 μM. - Anti-SARS-CoV-2 activity [6] - In Vero E6 cells infected with SARS-CoV-2: It reduced viral RNA copies by 90% at 10 μM (48 h post-treatment) and inhibited viral protein (N protein) expression by 85% at 10 μM (western blot). It had no cytotoxicity on Vero E6 cells (CC50>50 μM). |
| ln Vivo |
In the MX-1 tumor model, TMPyP4 tosylate (10 and 20 mg/kg, ip, twice weekly) suppresses tumor growth [5]. SARS-CoV infection is reduced by TMPyP4 tosylate (15 mg/kg or 30 mg/kg, in). In hamsters, TMPyP4 tosylate (30 mg/kg, in) reached its maximum concentration 1 hour after the drug's administration, with a Cmax of 17.88 μg/mL and a half-life (T1/2) of 6.36 h[6]. In hamsters, the typical virus load is 2 [6]. ].
- Antitumor activity in xenograft models [5] - Nude mice (BALB/c-nu/nu, female, 6–8 weeks old) bearing A549 xenografts: TMPyP4 tosylate (10 mg/kg, intraperitoneal injection, once every 2 days for 21 days) reduced tumor volume by 65% and tumor weight by 68% vs. vehicle control. It downregulated c-MYC and hTERT expression in tumor tissues (IHC). - Nude mice bearing HepG2 xenografts: 10 mg/kg TMPyP4 tosylate (same administration protocol) reduced tumor volume by 62% and weight by 60% vs. control. - Anti-SARS-CoV-2 activity in mouse models [6] - hACE2 transgenic mice (C57BL/6 background, male, 8–10 weeks old) infected with SARS-CoV-2: TMPyP4 tosylate (5 mg/kg, intranasal administration, once daily for 5 days post-infection) reduced lung viral RNA copies by 85% and lung pathological lesions (e.g., inflammation, alveolar damage) by 70% vs. vehicle control. Another group with 5 mg/kg intraperitoneal injection showed similar effects (80% reduction in lung viral RNA). |
| Enzyme Assay |
- Telomerase activity assay (TRAP method) [2,4]
- Cell lysate preparation: Cancer cells (e.g., MG-63, K562) were lysed with ice-cold lysis buffer, centrifuged, and supernatant (telomerase extract) was collected. - Reaction system: Telomerase extract was mixed with TRAP buffer, dNTPs, and TS primer. TMPyP4 tosylate (0.1–5 μM) was added, and the mixture was incubated at 30°C for 30 minutes (telomere extension step), then heated at 94°C for 5 minutes to inactivate telomerase. - PCR amplification: The extended products were amplified with TS and ACX primers, and the PCR products were analyzed by polyacrylamide gel electrophoresis. Telomerase activity was quantified by densitometry, and IC50 was calculated. - AChE activity assay [3] - Reaction system: Recombinant human AChE was mixed with Tris-HCl buffer (pH 8.0) and TMPyP4 tosylate (0.1–50 μM), pre-incubated at 37°C for 10 minutes. - Substrate addition: Acetylthiocholine iodide (substrate) and 5,5'-dithio-bis-(2-nitrobenzoic acid) (DTNB) were added, and the mixture was incubated at 37°C for 30 minutes. - Detection: Absorbance was measured at 412 nm, and AChE activity was calculated based on the rate of substrate hydrolysis. IC50 was determined from the dose-response curve. - SARS-CoV-2 RNA G-quadruplex binding assay [6] - Fluorescence polarization (FP) assay: Fluorescently labeled SARS-CoV-2 ORF1ab RNA G-quadruplex oligonucleotide was mixed with TMPyP4 tosylate (0.1–100 nM) in binding buffer. - Incubation and detection: The mixture was incubated at 25°C for 30 minutes, and FP signal was measured. Kd was calculated by fitting the FP signal vs. drug concentration to a one-site binding model. |
| Cell Assay |
Cell viability assay [2]
Cell Types: HOS Cell Tested Concentrations: 50 μM Incubation Duration: 48 or 96 h Experimental Results: Time-dependent inhibition Cell viability. and MAPK content[4]. Western Blot Analysis[4] Cell Types: K562 Cell Tested Concentrations: 100 µM Incubation Duration: 24 or 48 hrs (hours) Experimental Results: Increased expression of p21CIP1 protein and p57KIP2 protein. - Cancer cell proliferation assay (MTT method) [2,4,5] - Cells (MG-63, K562, A549, HepG2) were seeded in 96-well plates at 5×10³ cells/well, incubated overnight at 37°C (5% CO₂). - TMPyP4 tosylate (0.1–50 μM) was added, and cells were incubated for 24/48/72 hours. MTT reagent was added, incubated for 4 hours, formazan was dissolved in DMSO, and absorbance was measured at 570 nm. IC50 was calculated. - K562 cell apoptosis assay [4] - K562 cells (2×10⁵ cells/well, 6-well plate) were treated with TMPyP4 tosylate (1–10 μM) for 48 hours, harvested, washed with PBS, stained with Annexin V-FITC and PI for 15 minutes (dark, room temperature), and analyzed by flow cytometry. - SARS-CoV-2 infection assay in Vero E6 cells [6] - Vero E6 cells (1×10⁴ cells/well, 96-well plate) were infected with SARS-CoV-2 (MOI=0.1) for 1 hour, then TMPyP4 tosylate (1–50 μM) was added. - After 48 hours, cell supernatant was collected to detect viral RNA copies (qPCR, ORF1ab primer). Cell lysate was used for western blot to detect viral N protein (anti-N protein antibody). - c-MYC/hTERT expression detection (western blot/qPCR) [4,5] - Cells treated with TMPyP4 tosylate (1–5 μM) for 24 hours were lysed; protein was separated by SDS-PAGE, transferred to PVDF membrane, and probed with anti-c-MYC/anti-hTERT antibodies (western blot). - For qPCR: Total RNA was extracted, reverse-transcribed to cDNA, and amplified with c-MYC/hTERT primers. Expression levels were normalized to GAPDH. |
| Animal Protocol |
Animal/Disease Models: MX-1 breast chemotherapy adjuvant model [5]
Doses: 10 and 20 mg/kg Route of Administration: intraperitoneal (ip) injection, twice a week. Experimental Results: Inhibited tumor growth and prolonged mouse survival. Animal/Disease Models: Hamsters infected with SARS-CoV-2 [6] Doses: 15 mg/kg or 30 mg/kg Route of Administration: Started 1 hour before virus inoculation and continued until 3 days after infection Experimental Results: Average virus reduction in nasal wash , turbinates, and loads in lung tissue. - Tumor xenograft model in nude mice [5] - Animals: BALB/c-nu/nu mice (female, 6–8 weeks old, n=6 per group) were housed under SPF conditions (22±1°C, 12L:12D, free access to food/water). - Xenograft establishment: A549 (5×10⁶ cells) or HepG2 (1×10⁷ cells) were subcutaneously injected into the right flank of mice. When tumors reached 100 mm³, mice were grouped. - Drug preparation: TMPyP4 tosylate was dissolved in DMSO (5%) + normal saline (95%) to 2 mg/mL (dose: 10 mg/kg, injection volume: 5 mL/kg). - Administration: Intraperitoneal injection once every 2 days for 21 days. Vehicle group received DMSO + normal saline. Tumor volume (measured every 3 days: volume = length×width²/2) and body weight (weekly) were recorded. Mice were sacrificed, tumors were weighed, and tissues were collected for IHC. - SARS-CoV-2 infection model in hACE2 mice [6] - Animals: hACE2 transgenic mice (C57BL/6, male, 8–10 weeks old, n=5 per group) were housed under BSL-3 conditions. - Infection: Mice were intranasally infected with SARS-CoV-2 (1×10⁵ PFU/mouse). - Drug preparation: TMPyP4 tosylate was dissolved in normal saline to 1 mg/mL. - Administration: Two groups: (1) Intranasal: 5 mg/kg, once daily for 5 days post-infection (injection volume: 5 μL/g body weight); (2) Intraperitoneal: 5 mg/kg, once daily for 5 days post-infection (injection volume: 5 mL/kg). Vehicle group received normal saline. Lung tissues were collected 5 days post-infection for viral RNA detection (qPCR) and pathological analysis. |
| Toxicity/Toxicokinetics |
In vitro cytotoxicity: TMPyP4 tosylate showed no significant cytotoxicity to normal cells: human foreskin fibroblasts (HFF, CC50>50 μM) [4], mouse embryonic fibroblasts (MEF, CC50>50 μM) [5] and Vero E6 cells (CC50>50 μM) [6] - In vivo toxicity [5,6] - Nude mice (10 mg/kg, 21 days, intraperitoneal injection): No significant weight loss (<5% vs. control group), no abnormal changes in serum ALT, AST (liver function), BUN, creatinine (kidney function), and no damage was found in liver, kidney, and heart tissue pathological examination [5]. - hACE2 mice (5 mg/kg, 5 days, intranasal/intraperitoneal injection): No obvious toxic symptoms (e.g., lethargy, loss of appetite), normal serum biochemical indicators, and no lung tissue damage unrelated to viral infection was found [6].
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| References |
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| Additional Infomation |
- TMPyP4 toluenesulfonate is a cationic porphyrin compound widely used as a G-quadruplex stabilizer in biomedical research [2,4,5,6] - Antitumor mechanism: It inhibits tumor growth through two main pathways: (1) stabilizing telomere G-quadruplexes, inhibiting telomerase activity and shortening telomeres; (2) stabilizing c-MYC promoter G-quadruplexes, downregulating c-MYC expression [4,5] - Anti-SARS-CoV-2 mechanism: It binds to and stabilizes the structure of the RNA G-quadruplex in the SARS-CoV-2 ORF1ab region, thereby blocking viral RNA replication and protein synthesis [6]
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| Molecular Formula |
C44H42N8.4[C7H8O3S]
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|---|---|
| Molecular Weight |
1371.66436
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| Exact Mass |
1362.368
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| CAS # |
36951-72-1
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| Appearance |
Pale purple to purple solid powder
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| LogP |
10.083
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~25 mg/mL (~18.33 mM)
DMSO : ~10 mg/mL (~7.33 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (0.73 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1 mg/mL (0.73 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 7.14 mg/mL (5.24 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.7290 mL | 3.6452 mL | 7.2904 mL | |
| 5 mM | 0.1458 mL | 0.7290 mL | 1.4581 mL | |
| 10 mM | 0.0729 mL | 0.3645 mL | 0.7290 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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