Pentamidine dimesylate
Based on 9 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 番号: 6823-79-6
- 分子式: C21H32N4O8S2
- 分子量:532.63
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 Pentamidine dimesylate
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
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IF
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Cell Proliferation/Viability Assay
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Cell Migration/Invasion Assay
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WB
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RT-PCR
Antibiotic アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
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Trypanosoma |
Leishmania |
体外実験
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. Further protocols information, click here.
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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.
体内実験
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.
化学情報
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CAS 番号 6823-79-6
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分子量 532.63
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分子式 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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別名
MP-601205 dimesylate
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (9)
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Journal Impact Factor
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Most Recent
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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 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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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 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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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
プロトコル
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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.
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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.
純度とドキュメンテーション
参考文献
[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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Pentamidine dimesylate 関連分類
HY-B0537C 関連分類
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