alpha-NETA

115066-04-1

369.24

10 mM in DMSO

Metabolic Enzyme/Protease; Apoptosis; Neuronal Signaling

alpha-NETA is a potent and noncompetitive choline acetyltransferase (ChA) inhibitor with an IC50 of 9 uM. alpha-NETA is a potent ALDH1A1 (IC50=0.04 uM) and chemokine-like receptor-1 (CMKLR1) antagonist. alpha-NETA weakly inhibits cholinesterase (ChE; IC50=84 uM) and acetylcholinesterase (AChE; IC50=300 uM). alpha-NETA has anti-cancer activity.
IC50 & Target: IC50: 9 uM (ChAT); 0.04 uM (ALDH1A1); CMKLR1; 84 uM (ChE); 300 uM (AChE)
In Vitro: alpha-NETA (50-150 nM; 24 hours) decreases all cell lines viability in a dose-dependent manner.

alpha-NETA (2.5-10.0 ug/mL; 24 hours) leads to epithelial ovarian cancer (EOC) cell death associated with membrane blistering and cytoplasm leakage.

alpha-NETA treatment increases EOC cell expression of pyroptosis-associated proteins.

alpha-NETA is most potent in inhibiting aldehyde dehydrogenase 1 family, member A1 (ALDH1A1; IC50=0.04 uM; purified enzymes assay), followed by CMKLR1 (IC50=0.375 uM for beta-ARR2 recruitment; Cell-based assay) and G9a histone lysine methyltransferase (IC50=0.50 uM; purified enzymes assay). alpha-NETA selectively inhibits chemerin-stimulated CMKLR1 association with beta-arrestin2.

alpha-NETA possesses fluorescent characteristics (excitation spectrum: maxima 255 and 297 nm; emission spectrum: maximum 437 nm) of naphthyl moiety.

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

alpha-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.