Pentamidine isethionate

For research use only.

Catalog No.S4007

5 publications

Pentamidine isethionate Chemical Structure

CAS No. 140-64-7

Pentamidine is an inhibitor of PRL Phosphatases and also inhibits synthesis of DNA, RNA and protein.

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10mM (1mL in DMSO) USD 190 In stock
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Biological Activity

Description Pentamidine is an inhibitor of PRL Phosphatases and also inhibits synthesis of DNA, RNA and protein.
Targets
PRL Phosphatases [1]
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A549 MYjDfZRwfG:6aXPpeJkh[XO|YYm= MXvDfZRwfG:6aXPpeJkh[WejaX7zeEBCPTR7IHPlcIwhdGmwZTygTWM2OD1{NDFOwG0> M3fhR|E2OzV5OUi5
rat L6 cell MXPDfZRwfG:6aXPpeJkh[XO|YYm= NYPZRWZyS3m2b4TvfIlkcXS7IHHnZYlve3RicnH0JGw3KGOnbHzzMEBKSzVyPUKuNUDPxE1? NFW4TZoyPjlzM{eyNi=>
J774A1 NFzpO4tEgXSxdH;4bYNqfHliYYPzZZk> MYq3NkBp MUDDfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDKO|c1STFiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhS0N3ME2xJO69VQ>? M1PZclIzPjB6Nke1
HepG2 NF;JOWtEgXSxdH;4bYNqfHliYYPzZZk> NGXRWIM4OiCq M2PpVGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhmeEd{IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEOFNUC9Nk4{KM7:TR?= NGW4cJAzOjZyOE[3OS=>
HeLa MlHnR5l1d3SxeHnjbZR6KGG|c3H5 NV7JWXV5QTZiaB?= MWTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDI[WxiKGOnbHzzJIFnfGW{IEm2JIhzeyCkeTDy[ZNignW{aX6tZoF{\WRic4DlZ5Rzd2[udX;ybY1mfHKrYzDt[ZRpd2RuIFnDOVA:OTVizszN NYPBNGdHOjNzNkS2OlA>
WM115 MnHKR5l1d3SxeHnjbZR6KGG|c3H5 NILLTGhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBYVTFzNTDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDt[YF{fXKnZDDh[pRmeiB5MjDodpMh[nliY4L5d5RidCC4aX;s[ZQh[XO|YYmsJGlEPTB;ND64JO69VQ>? MVuyN|M4PTB7NB?=

... Click to View More Cell Line Experimental Data

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]

Protocol

Kinase Assay:[3]
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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) × 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:[3]
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  • Cell lines: Human colon carcinoma cell line WM480
  • Concentrations: 0.1-10 μg/mL
  • Incubation Time: 6 days
  • Method: 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)
Animal Research:[3]
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  • Animal Models: Human melanoma xenografts WM9
  • Dosages: 0.25 mg
  • Administration: i.m. at the hip area every 2 days
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (168.72 mM)
Water 100 mg/mL (168.72 mM)
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
Saline
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 592.68
Formula

C19H24N4O2.2C2H6O4S

CAS No. 140-64-7
Storage powder
in solvent
Synonyms N/A
Smiles C1=CC(=CC=C1C(=N)N)OCCCCCOC2=CC=C(C=C2)C(=N)N.C(CS(=O)(=O)O)O.C(CS(=O)(=O)O)O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02669706 Completed Drug: Pentamidine Hematologic Malignancy University of Illinois at Chicago March 2015 --
NCT00729807 Terminated Drug: pentamidine Melanoma (Skin) University of Maryland Baltimore|National Cancer Institute (NCI) July 2008 Phase 2
NCT00802594 Completed Drug: DB289 Trypanosomiasis African Immtech Pharmaceuticals Inc|Bill and Melinda Gates Foundation August 2001 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID