Ned 19

Ned 19 是一种选择性膜透性非竞争性 NAADP 拮抗剂，抑制 NAADP 介导的 Ca2+ 信号传导，IC50 为 65 nM。 Ned 19 强烈抑制小鼠的肿瘤生长和血管形成以及肺转移。

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Background

Ned 19 is a selective membrane-permeant non competitive NAADP antagonist and inhibits NAADP-mediated Ca2+ signaling, with an IC50 of 65 nM[1]. Ned 19 strongly inhibits tumor growth and vascularization as well as lung metastases in mice[2]. Ca2+

Ned 19 (25-100 μM; 24-72 hours) reduces cell proliferation[2]. Ned 19 (25-100 μM; 24-72 hours) reduces markedly the cell number[2]. Ned 19 (25-100 μM; 24-72 hours) reduces the S phase percentage and increases of the G0/G1 phase percentage evaluated by cell cycle analysis[2]. Ned 19 (25-100 μM; 24-72 hours) induces cell apoptosis a time-dependent manner[2]. Ned 19 (25-100 μM; 24-72 hours) reduces expression of N-cadherin and increases expression of E-cadherin, affecting the cell migratory behavior[2]. Cell Proliferation Assay[2] Cell Line: B16 cells

Ned 19 (i.p.; 5 mg/Kg/every second day; 4 week) impaires severely tumor growth[2]. Animal Model: Adult male C57BL/6 mice[2]

[1]. Rosen D, et al. Analogues of the nicotinic acid adenine dinucleotide phosphate (NAADP) antagonistNed-19 indicate two binding sites on the 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 and Neoangiogenesis. Sci Rep. 2016; 6: 18925.