Pentamidine isethionate
Based on 9 publication(s) in Google Scholar
Pentamidine isethionate (MP-601205 isethionate) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine isethionate inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine isethionate is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine isethionate has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.95%
- No. CAS: 140-64-7
- Fòrmula: C23H36N4O10S2
- Peso molecular:592.68
-
Almacenamiento:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
-
Help & FAQs
-
HY-15142
Doxorubicin hydrochlorideTopoisomerase Inhibitor -
HY-10219
RapamycinmTOR Inhibitor -
HY-16592
Brefeldin AProtein Transport Inhibitor -
HY-B0240
DisulfiramALDH1 Inhibitor -
HY-15431
CapivasertibAkt Inhibitor -
HY-12404
Diminazene aceturateTrypanocidal Agent -
HY-108547
Alexidine dihydrochlorideAntifungal Agent -
HY-N0110
Palmatine chlorideIDO-1/NS2B-NS3 Inhibitor -
HY-B0956
Paromomycin sulfateAntibiotic -
HY-12506
NaspmCa2+-permeable AMPA Antagonist -
HY-14153A
Tegaserod maleateSerotonin Receptor 4 Agonist -
HY-B0537BR
Pentamidine isethionate (Standard)Antimicrobial Agent
Publications Citing Use of MedChemExpress (MCE) Pentamidine isethionate
More- Nature. 2026 Jul;655(8121):240-250. [Abstract]
- Immunity. 2023 Feb 14;56(2):272-288.e7. [Abstract]
- Drug Des Devel Ther. 2021 Jul 1;15:2857-2868. [Abstract]
- Cell Rep Methods. 2023 Oct 23;3(10):100599. [Abstract]
- Int J Mol Sci. 2023 Sep 7;24(18):13812. [Abstract]
- Molecules. 2020 Apr 23;25(8):1980. [Abstract]
- Microbiol Spectr. 2023 Jun 15;11(3):e0313822. [Abstract]
- BMC Womens Health. 2022 Nov 24;22(1):470. [Abstract]
- Biochem Biophys Res Commun. 2019 Sep 17;517(2):221-226. [Abstract]
Customer Validation & Images
-
IF
-
Cell Proliferation/Viability Assay
-
Cell Migration/Invasion Assay
-
WB
-
RT-PCR
Ver todos los productos específicos de isoformas Parasite
MoreVer todos los productos específicos de isoformas Antibiotic
More
Actividad biológica
Descripciòn
IC50 & Target
|
Trypanosoma |
Leishmania |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| J774 | IC50 |
41.6 μM
Compound: S1
|
Cytotoxicity against J774.1 cell line after 48 hrs
Cytotoxicity against J774.1 cell line after 48 hrs
|
[PMID: 16516467] |
| L6 | IC50 |
5100 nM
Compound: Pentamidine
|
Cytotoxicity against rat L6 cells assessed as cell viability after 70 hrs by MTT assay
Cytotoxicity against rat L6 cells assessed as cell viability after 70 hrs by MTT assay
|
[PMID: 24398295] |
In Vitro
Pentamidine (0-10 μg/mL; 6 days; WM9, DU145, C4-2, Hey, WM480, and A549 cells) treatment inhibits the growth of cancer cells in a concentration-dependent manner[1].
?
The cytotoxic properties of Pentamidine isethionate towards the promastigotes of the protozoan parasite Leishmania infantum is determined. The leishmanicidal activity of Pentamidine isethionate is 60 times higher after 72 h of incubation than that of Cisplatin. Pentamidine isethionate induces a higher amount of programmed cell death (PCD) than Cisplatin, which is associated with inhibition of DNA synthesis and cell-cycle arrest in the G2/M phase. Binding of Pentamidine isethionate to calf-thymus DNA (CT-DNA) induces conformational changes in the DNA double helix, consistent with a B-->A transition. The interaction of Pentamidine isethionate with ubiquitin leads to a 6% increase in the beta-sheet content of the protein[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
-
Cell Line:WM9, DU145, C4-2, Hey, WM480, and A549 cells
-
Concentration:0-10 µg/mL
-
Incubation Time:6 days
-
Result:The growth of all six of the cell lines in culture was inhibited in a concentration-dependent manner with complete growth inhibition of the cell lines occurring at 10 µg/mL.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Athymic nude mice (6 weeks old) injected with WM9 cells[1]
-
Dosage:0.25 mg/mouse
-
Administration:Intramuscular injection; every 2 days; for 4 weeks
-
Result:Markedly inhibited the growth of WM9 human melanoma tumors in nude mice.
Chemical Information
-
No. CAS 140-64-7
-
Appearance Solid
-
Peso molecular 592.68
-
Fòrmula C23H36N4O10S2
-
Color White to off-white
-
SMILES
N=C(C1=CC=C(OCCCCCOC2=CC=C(C(N)=N)C=C2)C=C1)N.OCCS(=O)(O)=O.OCCS(=O)(O)=O
-
Synonyms
MP-601205 isethionate
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (9)
-
Journal Impact Factor
-
Most Recent
-
Nature
2026 Jul;655(8121):240-250. PMID: 42236947 -
Immunity
Spermine enhances antiviral and anticancer responses by stabilizing DNA binding with the DNA sensor cGAS. [Abstract]2023 Feb 14;56(2):272-288.e7. PMID: 36724787 -
Drug Des Devel Ther
Pentamidine Inhibits Ovarian Cancer Cell Proliferation and Migration by Maintaining Stability of PTEN in vitro. [Abstract]2021 Jul 1;15:2857-2868. PMID: 34234416
Pentamidine isethionate purchased from MedChemExpress. Usage Cited in: Drug Des Devel Ther. 2021 Jul 1;15:2857-2868. [Abstract]
HO8910 cells were seeded in 96-well plates and treated with different concentrations of Pentamidine (0, 1, 2.5, 5.0, 7.5, 15, 20 μmol/L) for 24 hours, with three replicates for each concentration. Cell viability was then assessed after incubation with 20 μL of MTS for 1 hour.
Pentamidine isethionate purchased from MedChemExpress. Usage Cited in: Drug Des Devel Ther. 2021 Jul 1;15:2857-2868. [Abstract]
Scratch healing experiments were performed using DMSO control and Pentamidin-treated HO8910 cells. Representative images were obtained at specified time points at a concentration of 2.5 μmol/L.
Pentamidine isethionate purchased from MedChemExpress. Usage Cited in: Drug Des Devel Ther. 2021 Jul 1;15:2857-2868. [Abstract]
HO8910 and Caov3 cells were treated with different concentrations of Pentamidine (5/10/20 μM) for 24 hours. Cell lysates were collected and analyzed by Western blotting using anti-PTEN antibody. GAPDH was used as an internal control.
Pentamidine isethionate purchased from MedChemExpress. Usage Cited in: Drug Des Devel Ther. 2021 Jul 1;15:2857-2868. [Abstract]
HO8910 and Caov3 cells were treated with 20 μmol/L Pentamidine for 24 hours. PTEN mRNA levels were detected by RT-PCR and normalized to 18S rRNA levels.
-
Cell Rep Methods
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]2023 Oct 23;3(10):100599. PMID: 37797618 -
Int J Mol Sci
The Properties of Linezolid, Rifampicin, and Vancomycin, as Well as the Mechanism of Action of Pentamidine, Determine Their Synergy against Gram-Negative Bacteria. [Abstract]2023 Sep 7;24(18):13812. PMID: 37762115 -
Molecules
In Vitro and in Vivo Activity of mTOR Kinase and PI3K Inhibitors Against Leishmania donovani and Trypanosoma brucei. [Abstract]2020 Apr 23;25(8):1980. PMID: 32340370
Pentamidine isethionate purchased from MedChemExpress. Usage Cited in: Molecules. 2020 Apr 23;25(8):1980. [Abstract]
In vivo results for T. brucei mouse model of infection. Mouse survival after treatment with 30 mg/kg pentamidine (solid green line), 15 mg/kg Torin2 (solid black line), 5 mg/kg NVP-BGT226 (dotted black line), or the PBS control (solid blue line) for 5 days.
-
Microbiol Spectr
When Combined with Pentamidine, Originally Ineffective Linezolid Becomes Active in Carbapenem-Resistant Enterobacteriaceae. [Abstract]2023 Jun 15;11(3):e0313822. PMID: 37125928 -
BMC Womens Health
Pentamidine inhibits proliferation, migration and invasion in endometrial cancer via the PI3K/AKT signaling pathway. [Abstract]2022 Nov 24;22(1):470. PMID: 36434592
Pentamidine isethionate purchased from MedChemExpress. Usage Cited in: BMC Womens Health. 2022 Nov 24;22(1):470. [Abstract]
Pentamidine (2.5, 5 μM; 24-36 h) reduces cell migration in a dose- and time-dependent manner, in Ishikawa and HEC-1A cells.
-
Biochem Biophys Res Commun
Pentamidine protects mice from cecal ligation and puncture-induced brain damage via inhibiting S100B/RAGE/NF-κB. [Abstract]2019 Sep 17;517(2):221-226. PMID: 31331643
Solvente y solubilidad
In Vitro:
H2O : 100 mg/mL (168.73 mM; Need ultrasonic)
DMSO : 100 mg/mL (168.73 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 and light). 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 and light). 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)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.51 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (3.51 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Protocolo
-
Research Protocol for Infectious Diseases
Infectious-disease experiments test how pathogens interact with host barriers, innate immune receptors, inflammatory signaling, pathogen replication, and tissue injury; pattern-recognition receptors such as TLRs, RIG-I-like receptors, NOD-like receptors, and inflammasomes detect microbial molecules and activate NF-κB, interferon, and cytokine responses. The central hypothesis is that infection severity reflects the balance between pathogen burden and host response: protective inflammation restricts pathogen growth, whereas excessive or mislocalized inflammation contributes to tissue damage and disease phenotype. Unresolved questions include which host pathways are protective versus pathogenic, why some infection models fail to translate to human disease, and which combined readouts best predict clinically relevant infection outcomes.
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Pureza y Documentación
-
Ficha de datos (290 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Instrucciones de manejo (2659 KB)
Referencias
[1]. Pathak MK, et al. Pentamidine is an inhibitor of PRL phosphatases with anticancer activity. Mol Cancer Ther. 2002 Dec;1(14):1255-64. [Content Brief]
[2]. Nguewa, P.A., et al., Pentamidine is an antiparasitic and apoptotic drug that selectively modifies ubiquitin. Chem Biodivers, 2005. 2(10): p. 1387-400. [Content Brief]
[3]. Sands M, et al. Pentamidine: a review. Rev Infect Dis. 1985 Sep-Oct;7(5):625-34. [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 and light). 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 | 1.6873 mL | 8.4363 mL | 16.8725 mL | 42.1813 mL |
| 5 mM | 0.3375 mL | 1.6873 mL | 3.3745 mL | 8.4363 mL | |
| 10 mM | 0.1687 mL | 0.8436 mL | 1.6873 mL | 4.2181 mL | |
| 15 mM | 0.1125 mL | 0.5624 mL | 1.1248 mL | 2.8121 mL | |
| 20 mM | 0.0844 mL | 0.4218 mL | 0.8436 mL | 2.1091 mL | |
| 25 mM | 0.0675 mL | 0.3375 mL | 0.6749 mL | 1.6873 mL | |
| 30 mM | 0.0562 mL | 0.2812 mL | 0.5624 mL | 1.4060 mL | |
| 40 mM | 0.0422 mL | 0.2109 mL | 0.4218 mL | 1.0545 mL | |
| 50 mM | 0.0337 mL | 0.1687 mL | 0.3375 mL | 0.8436 mL | |
| 60 mM | 0.0281 mL | 0.1406 mL | 0.2812 mL | 0.7030 mL | |
| 80 mM | 0.0211 mL | 0.1055 mL | 0.2109 mL | 0.5273 mL | |
| 100 mM | 0.0169 mL | 0.0844 mL | 0.1687 mL | 0.4218 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.
Pentamidine isethionate Related Classifications
HY-B0537B Related Classifications
Powered by Bioz