Pentamidine isethionate

製品コードS4007 バッチS400701

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C19H24N4O2.2C2H6O4S
分子量 592.68 CAS No. 140-64-7
Solubility (25°C)* 体外 DMSO 119 mg/mL (200.78 mM)
Water 119 mg/mL (200.78 mM)
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* 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.

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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.
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]

プロトコル(参考用のみ)

キナーゼアッセイ 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.
細胞アッセイ 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.
動物実験 動物モデル Human melanoma xenografts WM9
投薬量 0.25 mg
投与方法 i.m. at the hip area every 2 days

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Computational pharmacogenomic screen identifies drugs that potentiate the anti-breast cancer activity of statins [ Nat Commun, 2022, 13(1):6323] PubMed: 36280687
Bioanalytical methods for pharmacokinetic studies of antileishmanial drugs [ Biomed Chromatogr, 2022, e5519.] PubMed: 36208186
Pentamidine Inhibits Prostate Cancer Progression via Selectively Inducing Mitochondrial DNA Depletion and Dysfunction [ Cell Prolif, 2020, 53(1):e12718] PubMed: 31721355
Chemoproteomic Profiling Uncovers CDK4-Mediated Phosphorylation of the Translational Suppressor 4E-BP1 [ Cell Chem Biol, 2019, 10.1016/j.chembiol.2019.03.012] PubMed: 31056462
Pentamidine Inhibits Titanium Particle-Induced Osteolysis In Vivo and Receptor Activator of Nuclear Factor-κB Ligand-Mediated Osteoclast Differentiation In Vitro. [ Tissue Eng Regen Med, 2019, 16(3):265-273] PubMed: 31205855
Functional Assessment of 2,177 U.S. and International Drugs Identifies the Quinoline Nitroxoline as a Potent Amoebicidal Agent against the Pathogen Balamuthia mandrillaris. [ mBio, 2018, 9(5)] PubMed: 30377287
Cyclooxygenase-2 Influences Response to Cotargeting of MEK and CDK4/6 in a Subpopulation of Pancreatic Cancers [ Mol Cancer Ther, 2018, 17(12):2495-2506] PubMed: 30254182
Repurposing the quinoline antibiotic nitroxoline to treat infections caused by the brain-eating amoeba Balamuthia mandrillaris [ bioRxiv, 2018, 10.1101/331785] PubMed: N/A

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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