α-NETA 是一种有效的，非竞争性的胆碱乙酰转移酶 (ChA) 抑制剂，IC50为 9 μM。α-NETA 是一种有效的 ALDH1A1 (IC50=0.04 μM) 和趋化因子样受体 1 (CMKLR1) 拮抗剂。α-NETA 微弱的抑制胆碱酯酶 (ChE;IC50=84 μM) 和乙酰胆碱酯 (AChE;IC50=300 μM)。α-NETA 具有抗癌活性。

α-NETA is a potent and noncompetitive choline acetyltransferase (ChA) inhibitor with an IC 50 of 9 μM. α-NETA is a potent ALDH1A1 ( IC 50 =0.04 μM) and chemokine-like receptor-1 (CMKLR1) antagonist. α-NETA weakly inhibits cholinesterase (ChE; IC 50 =84 μM) and acetylcholinesterase (AChE; IC 50 =300 μM). α-NETA has anti-cancer activity [1] [2].

α-NETA (50-150 nM; 24 hours) decreases all cell lines viability in a dose-dependent manner [3]. α-NETA (2.5-10.0 μg/mL; 24 hours) leads to epithelial ovarian cancer (EOC) cell death associated with membrane blistering and cytoplasm leakage [3]. α-NETA treatment increases EOC cell expression of pyroptosis-associated proteins [3]. α-NETA is most potent in inhibiting aldehyde dehydrogenase 1 family, member A1 (ALDH1A1; IC 50 =0.04 μM; purified enzymes assay), followed by CMKLR1 (IC 50 =0.375 μM for β-ARR2 recruitment; Cell-based assay) and G9a histone lysine methyltransferase (IC 50 =0.50 μM; purified enzymes assay). α-NETA selectively inhibits chemerin-stimulated CMKLR1 association with β-arrestin2 [2]. α-NETA possesses fluorescent characteristics (excitation spectrum: maxima 255 and 297 nm; emission spectrum: maximum 437 nm) of naphthyl moiety [1]. Cell Viability Assay [3] Cell Line: Ho8910, Ho8910PM, A2780, and Iose80 cells Concentration: 50, 100, 150 nM Incubation Time: 24 hours Result: Decreased all cell lines viability in a dose-dependent manner. Apoptosis Analysis [3] Cell Line: Epithelial ovarian cancer (EOC) cell Concentration: 2.5, 7.5, 10.0 μg/mL Incubation Time: 24 hours Result: Led to EOC cell death associated with membrane blistering and cytoplasm leakage.

α-NETA (i.p.; 0.125 mg/kg; once every other day for 20 days) significantly decreases tumor volume and tumor weight [3]. α-NETA (s.c. injection; 3 mg/kg or 10 mg/kg; daily; for 30 days) significantly delays the onset of EAE with 3 mg/kg, and completely suppresses clinical signs for an average of nine days with 10 mg/kg beyond the first appearance of disease in control female C57BL/6 mice [2]. Animal Model: BALB/c nude mice with skov3 cells [3] Dosage: 0.125 mg/kg Administration: IP; once every other day for 20 days Result: Significantly decreased tumor volume and tumor weight.

115066-04-1

C16H20INO

369.246

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years