Arecoline HBr | ACAT1 inhibitor
NMR (Conforms)
Available Options
| Size : | Price | Quantity | |
|---|---|---|---|
| 250 mg | $30.00 | ||
| 1 gram | $60.00 |
Arecoline (CAS 300-8-3) is a covalent inhibitor of ACAT1 which binds to and disrupts only ACAT1 tetramers (IC50=11.1 μM). ACAT2 and DLAT are not inhibited. Tyrosine407 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. Treatment of xenograft nude mice with Arecoline resulted in a dose-dependent reduction in tumor mass.1 Agonist at muscarinic acetylcholine receptors M1 – M5 (EC50 in the range of 7-410 nM).2 May be effective in dementia.3
References/Citations:
1) Fan et al. (2016), Tetrameric Acetyl-CoA Acetyltransferase 1 is Important for Tumor Growth; Mol. Cell, 64 859
2) Heinrich et al. (2009), Pharmacological comparison of muscarinic ligands: historical versus more recent muscarinic M1-preferring receptor agonists; Eur. J. Pharmacol., 605 53
3) Christie et al. (1981), Physostigmine and arecoline: effects of intravenous infusions in Alzheimer presenile dementia; Br. J. Psychiatry, 138 46
NMR (Conforms)
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Product Data Sheet:
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Arecoline (CAS 300-8-3) is a covalent inhibitor of ACAT1 which binds to and disrupts only ACAT1 tetramers (IC50=11.1 μM). ACAT2 and DLAT are not inhibited. Tyrosine407 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. Treatment of xenograft nude mice with Arecoline resulted in a dose-dependent reduction in tumor mass.1 Agonist at muscarinic acetylcholine receptors M1 – M5 (EC50 in the range of 7-410 nM).2 May be effective in dementia.3
References/Citations:
1) Fan et al. (2016), Tetrameric Acetyl-CoA Acetyltransferase 1 is Important for Tumor Growth; Mol. Cell, 64 859
2) Heinrich et al. (2009), Pharmacological comparison of muscarinic ligands: historical versus more recent muscarinic M1-preferring receptor agonists; Eur. J. Pharmacol., 605 53
3) Christie et al. (1981), Physostigmine and arecoline: effects of intravenous infusions in Alzheimer presenile dementia; Br. J. Psychiatry, 138 46
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