1. Metabolic Enzyme/Protease
    Neuronal Signaling
    Apoptosis
  2. Aldehyde Dehydrogenase (ALDH)
    AChE
    Apoptosis
  3. α-NETA

α-NETA 

Cat. No.: HY-138097
Handling Instructions

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.

For research use only. We do not sell to patients.

α-NETA Chemical Structure

α-NETA Chemical Structure

CAS No. : 115066-04-1

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Description

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].

IC50 & Target

IC50: 9 μM (ChAT); 0.04 µM (ALDH1A1); CMKLR1; 84 µM (ChE); 300 µM (AChE)[1][2]

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
In Vivo

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

369.24

Formula

C₁₆H₂₀INO

CAS No.

115066-04-1

SMILES

O=C(CC[N+](C)(C)C)C1=CC=CC2=C1C=CC=C2.[I-]

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

α-NETAAldehyde Dehydrogenase (ALDH)AChEApoptosisAcetylcholinesteraseHo8910Ho8910PMA2780Iose80cholineacetyltransferaseCMKLR1cholinesteraseALDH1A1G9ahistonelysinemethyltransferasefluorescentβ-ARR2β-arrestin2Inhibitorinhibitorinhibit

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