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α-NETA

CAS No. : 115066-04-1

MCE 站：α-NETA

产品活性：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 ?M) 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 ?M) 和乙酰胆碱酯 (AChE; IC₅₀=300 ?M)。α-NETA 具有抗癌活性。

研究领域：Metabolic Enzyme/Protease  |  Neuronal Signaling  |  Apoptosis

作用靶点：Aldehyde Dehydrogenase (ALDH)  |  AChE  |  Apoptosis

In Vitro: α-NETA (50-150 nM; 24 hours) decreases all cell lines viability in a dose-dependent manner.
α-NETA (2.5-10.0 ?g/mL; 24 hours) leads to epithelial ovarian cancer (EOC) cell death associated with membrane blistering and cytoplasm leakage.
α-NETA treatment increases EOC cell expression of pyroptosis-associated proteins.
α-NETA is most potent in inhibiting aldehyde dehydrogenase 1 family, member A1 (ALDH1A1; IC₅₀=0.04 ?M; purified enzymes assay), followed by CMKLR1 (IC₅₀=0.375 ?M for β-ARR2 recruitment; Cell-based assay) and G9a histone lysine methyltransferase (IC₅₀=0.50 ?M; purified enzymes assay). α-NETA selectively inhibits chemerin-stimulated CMKLR1 association with β-arrestin2.
α-NETA possesses fluorescent characteristics (excitation spectrum: maxima 255 and 297 nm; emission spectrum: maximum 437 nm) of naphthyl moiety.

In Vivo: α-NETA (i.p.; 0.125 mg/kg; once every other day for 20 days) significantly decreases tumor volume and tumor weight.
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.

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