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Pentamidine isethionate

Catalog No. T1654 CAS 140-64-7

Synonyms: Pentamidine isethionate salt, Pentamidine diisethionate

Pentamidine isethionate (Pentamidine diisethionate) is a synthetic amidine derivative, Pentamidine Isethionate is an antiprotozoal and antifungal agent.

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Pentamidine isethionate Chemical Structure

Pentamidine isethionate, CAS 140-64-7

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100 mg	In stock	$ 33.00
200 mg	In stock	$ 39.00
1 mL * 10 mM (in DMSO)	In stock	$ 30.00

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Purity: 99.83%

Purity: 99.5%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Pentamidine isethionate (Pentamidine diisethionate) is a synthetic amidine derivative, Pentamidine Isethionate is an antiprotozoal and antifungal agent.
Targets&IC50	Leishmania infantum:2.5 μM (IC50)
In vitro	Pentamidine is known experimentally to interfere with numerous cellular processes. Specifically, Pentamidine has been shown to bind to DNA in a nonintercalative manner and appears to preferentially bind to kinetoplast DNA in trypanosomes. Additionally, Pentamidine may inhibit RNA polymerase and ribosomal function, as well as nucleic acid, protein, phospholipid, and polyamine synthesis. Pentamidine also inhibits certain proteases, including trypsin, and impairs cellular oxygen consumption. [1] Pentamidine has a potent in vitro antiprotozoal activity. Pentamidine displays cytotoxic activity against L. infantum promastigotes with IC50 of 2.5 μM. 2.5 μM Pentamidine induces early programmed cell death in 49.6% of L. infantum promastigotes. 2.5 μM Pentamidine induces a notorious decrease in promastigotes in both G1 and S phases relative to the control-untreated samples (G1:77.0 vs 15.0%; S:11.0 vs 2.4% for control- and pentamidine-treated promastigotes, resp). Pentamidine is able to bind with calf-thymus DNA (CT-DNA) and induces conformational changes in the DNA double helix. Pentamidine also binds with ubiquitin to modifiy the β-cluster of ubiquitin. [2] Pentamidine is an inhibitor of phosphatase of regenerating liver (PRLs). 1 μg/mL of Pentamidine complete inhibits the activity of recombinant PTP1B in dephosphorylating a phos-photyrosine peptide. 10 μg/mL of Pentamidine completely inhibits the activities of recombinant PRL-1, PRL-2 and PRL-3 in dephosphorylating a phosphotyrosine peptide substrate. Incubation with Pentamidine (1 μg/mL) for 48 h reduces the activity of intracellular PRL phosphatases in transfected NIH3T3 cells by more than 85%. 10 μg/mL Pentamidine completely inhibits the growth of melanoma cell line (WM9), prostate carcinoma cell line (DU145 and C4–2), ovarian carcinoma cell line (Hey), colon carcinoma cell line (WM480), and lung carcinoma cell line (A549) which all express endogenous PRLs. [3]
In vivo	Pentamidine has a potent antiprotozoal activity in animal models. Pentamidine (0.3-9 mg/L) decreased the viability of P. carinii in experimental models in chick embryo lung epithelial cells and lung cells of rats with pneumonia. 5 mg/kg Pentamidine treatment for 2 weeks eradicates Pneumocystis carinii pneumonia in 75% of the animals. [4] Pentamidine inhibits the growth of WM9 human melanoma tumors in nude mice. During the 16-week study period, the tumors in 250 μg pentamidine-treated mice stays at sizes similar to those at the treatment initiation point, whereas the tumors in the control mice grow so rapidly that humane sacrifice of the animals is required at the 4th week. Pentamidine induces significant necrosis that accounts for more than 50% of the tumor mass. [3]
Kinase Assay	In vitro PTPase assays: Individual PTPases (0.01 μg/reaction) in 50 μL of PTPase buffer [50 mM Tris (pH 7.4)] are incubated at 22 ℃ for 10 min or as indicated in the absence or presence of inhibitory compounds. Substrates (0.2 mM phosphotyrosine peptide) are then added and allows to react at 22 ℃ for 18 hr. PTPase activity of individual reactions is measured by adding 100 μL of malachite green solution (UBI) and then quantifying the amounts of free phosphate cleaved by the PTPase from the peptide substrate by spectrometry (A660 nm). Relative PTPase activities are calculated based on the formula [(PTPase activity in the presence of an inhibitory compound)/(PTPase activity in the absence of the compound) &times 100%]. Reactions performed under comparable conditions in the absence of recombinant PTPases only are used as controls and shows no detectable PTPase activity.
Cell Research	Cells are washed in 10% FCS contained RPMI 1640 medium twice, resuspended in 10% FCS medium, incubated at 37 ℃ for 16 hr, and then cultured at 37 ℃ in 10% FCS medium containing various amounts of Pentamidine for 6 days. The cell numbers in proliferation assays are determined by an MTT assay.(Only for Reference)

Synonyms	Pentamidine isethionate salt, Pentamidine diisethionate
Molecular Weight	592.68
Formula	C23H36N4O10S2
CAS No.	140-64-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 168.7 mM

H2O: 168.7 mM

References and Literature

1. Sands M, et al. Rev Infect Dis, 1985, 7(5), 625-634. 2. Nguewa PA, et al. Chem Biodivers, 2005, 2(10), 1387-1400. 3. Pathak MK, et al. Mol Cancer Ther, 2002, 1(14), 1255-1264. 4. Monk JP, et al. Drugs, 1990, 39(5), 741-756.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Parasitic Compound Library Anti-Cancer Active Compound Library Drug Repurposing Compound Library Anti-Cancer Approved Drug Library Inhibitor Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library NO PAINS Compound Library Target-Focused Phenotypic Screening Library Anti-Lung Cancer Compound Library

Related Products

Related compounds with same targets

h-NTPDase-IN-1 TPI-1 PROTAC PTPN2 degrader-2 PTP1B/AKR1B1-IN-2 PTP1B/AKR1B1-IN-1 7-BIA TCS 401 Cyclosporin A

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

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Keywords

Pentamidine isethionate 140-64-7 Metabolism Microbiology/Virology Phosphatase Antibacterial Antibiotic Parasite Antifungal DNA cell-cycle Pentamidine isethionate salt Bacterial pneumonia Pneumocystis PTP1B carinii biosynthetics Kidney MP601205 MP 601205 Pentamidine diisethionate arrest Pentamidine antitumor Fungal Inhibitor MP-601205 inhibit inhibitor

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