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Pentamidine isethionate

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

Pentamidine isethionate化学構造

CAS No. 140-64-7

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Pentamidine isethionate関連製品

phosphatase阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
J774A1 Cytotoxicity assay 72 h Cytotoxicity against mouse J774A1 cells after 72 hrs by MTT assay, CC50=1 μM 22608675
HepG2 Cytotoxicity assay 72 h Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay, CC50=2.3 μM 22608675
HeLa Cytotoxicity assay 96 h Cytotoxicity against human HeLa cells after 96 hrs by resazurin-based spectrofluorimetric method, IC50=15 μM 23164660
A549 Cytotoxicity assay Cytotoxicity against A549 cell line, IC50=24 μM 15357989
rat L6 cell Cytotoxicity assay Cytotoxicity against rat L6 cells, IC50=2.1 μM 16913722
WM115 Cytotoxicity assay Cytotoxicity against human WM115 cells assessed as growth inhibition measured after 72 hrs by crystal violet assay, IC50=4.8 μM 23375094
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生物活性

製品説明 Pentamidine is an inhibitor of PRL Phosphatases and also inhibits synthesis of DNA, RNA and protein.
Targets
PRL Phosphatases [1]
In Vitro
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]
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) × 100%]. Reactions performed under comparable conditions in the absence of recombinant PTPases only are used as controls and shows no detectable PTPase activity.
細胞実験 細胞株 Human colon carcinoma cell line WM480
濃度 0.1-10 μg/mL
反応時間 6 days
実験の流れ 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.
In Vivo
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]
動物実験 動物モデル Human melanoma xenografts WM9
投与量 0.25 mg
投与経路 i.m. at the hip area every 2 days
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05458752 Completed
Pneumocystis Jirovecii Infection
Central Hospital Nancy France
 April 1 2020 --
NCT02669706 Completed
Hematologic Malignancy
University of Illinois at Chicago
 March 2015 --
NCT00729807 Terminated
Melanoma (Skin)
University of Maryland Baltimore|National Cancer Institute (NCI)
 July 2008 Phase 2
NCT00802594 Completed
Trypanosomiasis African
Immtech Pharmaceuticals Inc|Bill and Melinda Gates Foundation
 August 2001 Phase 2

化学情報

分子量 592.68 化学式

C19H24N4O2.2C2H6O4S
CAS No. 140-64-7 SDF Download Pentamidine isethionate SDFをダウンロードする
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
保管

In vitro
Batch:

DMSO : 100 mg/mL ( (168.72 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : 100 mg/mL

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

mg/kg g μL 匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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