|Aliases: Arecoline hydrobromide, 1,2,5,6-tetrahydro-1-methyl-3-pyridinecarboxylic acid, methyl ester, hydrobromide|
|Catalog No: 14132||Format: 1 g||$85||Buy|
|Catalog No: 14133||Format: 250 mg||$35||Buy|
MW = 236.1
C8H13NO2 • HBr
>98% (TLC); NMR (Conforms)
Tyrosine 407 phosphorylation activates mitochondrial acetyl-CoA acetyltransferase 1 (ACAT1) by stabilizing its tetramer. This is believed to be the mechanisms by which ACAT1 is "hijacked" and contributes to the Warburg effect in cancer. Arecoline is a covalent inhibitor of ACAT1 which binds to and disrupts only ACAT1 tetramers (IC50 = 11.1 µM). ACAT2 and DLAT are not inhibited. Treatment of xenograft nude mice with Arecoline resulted in a dose-dependent reduction in tumor mass (ref 1). Agonist at muscarinic acetylcholine receptors M1-M5 (EC50 in the range of 7-410 nM) (ref 2). May be effective in dementia (ref 3).
White crystalline powder. May be dissolved in water (50 mg/ml).
Store desiccated as supplied at room temperature for up to 2 years. Do not store solutions for longer than one day.
1. J Fan et al. Mol. Cell 2016, 64:859
2. JN Heinrich et al. Eur. J. Pharmacol. 2009, 605:53
3. JE Christie et al. Br. J. Psychiatry 1981, 138:46