Ned 19

Names

[ CAS No. ]:
874374-25-1

[ Name ]:
Ned 19

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> Calcium Channel
Research Areas >> Cancer

[Target]

Ca2+


[In Vitro]

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 Concentration: 25, 50, 100 μM Incubation Time: 24, 48, 72 hours Result: Reduced cell proliferation. Cell Viability Assay[2] Cell Line: B16 cells Concentration: 25, 50, 100 μM Incubation Time: 24, 48, 72 hours Result: Reduced markedly the cell number. Cell Cycle Analysis[2] Cell Line: B16 cells Concentration: 25, 50, 100 μM Incubation Time: 24, 48, 72 hours Result: Reduced the S phase percentage and increased of the G0/G1 phase percentage. Apoptosis Analysis[2] Cell Line: B16 cells Concentration: 25, 50, 100 μM Incubation Time: 24, 48, 72 hours Result: Induced cell apoptosis a time-dependent manner. Western Blot Analysis[2] Cell Line: B16 cells Concentration: 25, 50, 100 μM Incubation Time: 24, 48, 72 hours Result: Reduced expression of N-cadherin and increased expression of E-cadherin.

[In Vivo]

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] Dosage: 5 mg/Kg Administration: I.p.; every second day; 4 week Result: Impaired severely tumor growth.

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C30H31FN4O3

[ Molecular Weight ]:
514.59100

[ Exact Mass ]:
514.23800

[ PSA ]:
80.83000

[ LogP ]:
4.65780


Related Compounds