Pentamidine isethionate
For research use only.
Catalog No.S4007
5 publications
CAS No. 140-64-7
Pentamidine is an inhibitor of PRL Phosphatases and also inhibits synthesis of DNA, RNA and protein.
Selleck's Pentamidine isethionate has been cited by 5 publications
Purity & Quality Control
Choose Selective phosphatase Inhibitors
Biological Activity
| Description | Pentamidine is an inhibitor of PRL Phosphatases and also inhibits synthesis of DNA, RNA and protein. | |||||||||||||||||||||||||||||||||||||||||||||||||||
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| 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] |
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| Cell Data |
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| 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. |
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| Cell Research:[3] |
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| Animal Research:[3] |
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Solubility (25°C)
| In vitro | DMSO | 100 mg/mL (168.72 mM) |
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| 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 |
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| 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 |
In vivo Formulation Calculator (Clear solution)
| Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment) | ||||||||||
| Dosage | mg/kg |  |
Average weight of animals | g | |
Dosing volume per animal | ul | |
Number of animals | |
| Step 2: Enter the in vivo formulation () | ||||||||||
| % DMSO % % Tween 80 % ddH2O | ||||||||||
| CalculateReset | ||||||||||
Calculation results:
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
Bio Calculators
Molarity Calculator
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Dilution Calculator
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Molarity Calculator
Clinical Trial Information
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
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| 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 |
Tech Support
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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