Ned-19 _Calcium Channel 抑制劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENed 19Cat. No.: HY-103316ACAS No.: 874374-25-1分式: CHFNO分量: 514.59作靶點: Calcium Channel作通路: Membrane Transporter/Ion Channel; Neuronal Signaling儲存式: Please store the product under the recommended conditions inthe COA.BIOLOGICAL AC

2、TIVITY物活性 Ned 19種選擇性膜透性競爭性 NAADP 拮抗劑，抑制 NAADP 介導的 Ca2+ 信號傳導，IC50 為 65 nM。Ned 19 強烈抑制的腫瘤長和管形成以及肺轉移。IC50 & Target Ca2+體外研究Ned 19 (25-100 M; 24-72hours) reduces cell proliferation 2.Ned 19 (25-100 M; 24-72hours) reduces markedly the cell number 2.Ned 19 (25-100 M; 24-72hours) reduces the S phase percen

3、tage and increases of the G0/G1 phasepercentage evaluated by cell cycle analysis 2.Ned 19 (25-100 M; 24-72hours) induces cell apoptosis a time-dependent manner 2.Ned 19 (25-100 M; 24-72hours) reduces expression of N-cadherin and increases expression of E-cadherin,affecting the cell migratory behavio

4、r 2.Cell Proliferation Assay 2Cell Line: B16 cellsConcentration: 25, 50, 100 MIncubation Time: 24, 48, 72hoursResult: Reduced cell proliferation.Cell Viability Assay 21/3 Master of Small Molecules 您邊的抑制劑師www.MedChemECell Line: B16 cellsConcentration: 25, 50, 100 MIncubation Time: 24, 48, 72hoursResu

5、lt: Reduced markedly the cell number.Cell Cycle Analysis 2Cell Line: B16 cellsConcentration: 25, 50, 100 MIncubation Time: 24, 48, 72hoursResult: Reduced the S phase percentage and increased of the G0/G1 phase percentage.Apoptosis Analysis 2Cell Line: B16 cellsConcentration: 25, 50, 100 MIncubation

6、Time: 24, 48, 72hoursResult: Induced cell apoptosis a time-dependent manner.Western Blot Analysis 2Cell Line: B16 cellsConcentration: 25, 50, 100 MIncubation Time: 24, 48, 72hoursResult: Reduced expression of N-cadherin and increased expression of E-cadherin.體內(nèi)研究 Ned 19 (i.p.; 5mg/Kg/every second da

7、y; 4 week) impaires severely tumor growth 2.Animal Model: Adult male C57BL/6 mice 2Dosage: 5mg/KgAdministration: I.p.; every second day; 4 weekResult: Impaired severely tumor growth.REFERENCES2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE1. Rosen D, et al. Analogues of the nicotinic acid adenine

8、dinucleotide phosphate (NAADP) antagonistNed-19 indicate two binding sites onthe NAADP receptor. J Biol Chem. 2009 Dec 11;284(50):34930-4.2. Annarita Favia, et al. NAADP-Dependent Ca2+ Signaling Controls Melanoma Progression, Metastatic Dissemination andNeoangiogenesis. Sci Rep. 2016; 6: 18925.McePdfHeightCaution: Product has not been fully validated for medical applications