Pentamidine  (Synonyms: MP-601205)

Pentamidine (MP-601205) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine inhibits parasite Leishmania infantum with an IC₅₀ of 2.5 μM. Pentamidine is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities^[1][2][3][4].

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.

Pentamidine (0.25 mg/mouse; intramuscular injection; every 2 days; for 4 weeks; athymic nude mice) treatment markedly inhibits the growth of WM9 human melanoma tumors in nude mice^[1].

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

340.42

C₁₉H₂₄N₄O₂

100-33-4

Solid

White to off-white

N=C(C1=CC=C(OCCCCCOC2=CC=C(C(N)=N)C=C2)C=C1)N

Room temperature in continental US; may vary elsewhere.

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

* 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [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]

  [4]. David C. Bean, et al. Pentamidine: a drug to consider re-purposing in the targeted treatment of multi-drug resistant bacterial infections? J Lab Precis Med 2017;2:49.