Bioactivity | α-NETA is a potent and noncompetitive choline acetyltransferase (ChA) inhibitor with an IC50 of 9 μM. α-NETA is a potent ALDH1A1 (IC50=0.04 µM) and chemokine-like receptor-1 (CMKLR1) antagonist. α-NETA weakly inhibits cholinesterase (ChE; IC50=84 µM) and acetylcholinesterase (AChE; IC50=300 µM). α-NETA has anti-cancer activity[1][2]. |
Invitro | 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; IC50=0.04 µM; purified enzymes assay), followed by CMKLR1 (IC50=0.375 µM for β-ARR2 recruitment; Cell-based assay) and G9a histone lysine methyltransferase (IC50=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: |
Name | α-NETA |
CAS | 115066-04-1 |
Formula | C16H20INO |
Molar Mass | 369.24 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | 4°C, protect from light, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen) |