Pentamidine dimesylate
Based on 8 publication(s) in Google Scholar
Pentamidine (MP-601205) dimesylate is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine dimesylate inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine dimesylate is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine dimesylate has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities.
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- CAS. Nr.: 6823-79-6
- Formel: C21H32N4O8S2
- Molecular Weight:532.63
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Pentamidine dimesylate
More- Immunity. 2023 Feb 14;56(2):272-288.e7. [Abstract]
- Drug Des Devel Ther. 2021 Jul 1;15:2857-2868. [Abstract]
- Int J Mol Sci. 2023 Sep 7;24(18):13812. [Abstract]
- Molecules. 2020 Apr 23;25(8):1980. [Abstract]
- Cell Rep Methods. 2023 Oct 23;3(10):100599. [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]
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Cell Migration/Invasion Assay
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Biologische Aktivität
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Trypanosoma |
Leishmania |
Pentamidine (0-10 µg/mL; 6 days; WM9, DU145, C4-2, Hey, WM480, and A549 cells) dimesylate 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.
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Cell Line:WM9, DU145, C4-2, Hey, WM480, and A549 cells
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Concentration:0-10 µg/mL
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Incubation Time:6 days
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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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Athymic nude mice (6 weeks old) injected with WM9 cells[1]
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Dosage:0.25 mg/mouse
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Administration:Intramuscular injection; every 2 days; for 4 weeks
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Result:Markedly inhibited the growth of WM9 human melanoma tumors in nude mice.
Chemical Information
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CAS. Nr. 6823-79-6
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Molecular Weight 532.63
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Formel C21H32N4O8S2
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SMILES
N=C(N)C1=CC=C(C=C1)OCCCCCOC2=CC=C(C=C2)C(N)=N.OS(=O)(C)=O.OS(=O)(C)=O
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Synonyms
MP-601205 dimesylate
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (8)
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Journal Impact Factor
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Most Recent
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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 dimesylate 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 dimesylate 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 dimesylate 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 dimesylate 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.
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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 dimesylate 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.
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Cell Rep Methods
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]2023 Oct 23;3(10):100599. PMID: 37797618 -
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 dimesylate 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.
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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
Reinheit & Dokumentation
Verweise
[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]
Calculators
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