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)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
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
Related products
-
Camptothecin | Topoisomerase I inhibitor
From $40.00CAS:7689-03-4Catalog Number:10-1041Activity:Topoisomerase I inhibitorChemical Name:(S)-4-Ethyl-4-hydroxy-1H-pyrano-[3′,4′:6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dioneMolecular Weight:348.35Molecular Formula:C20H16N2O4Solubility:Soluble in DMSO (up to 5 mg/ml).Physical Properties:Tan solidPurity:98%Storage Temperature:-20°CStability:Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.Shipping Code:RT -
ZM-447439 | Aurora B kinase inhibitor
From $52.00CAS:331771-20-1Catalog Number:10-1037Activity:Aurora B kinase inhibitorChemical Name:N-[4-[[6-Methoxy-7-[3-(4-morpholinyl)propoxy]-4-quinazolinyl]amino]phenyl]benzamideMolecular Weight:513.59Molecular Formula:C29H31N5O4Solubility:Soluble in DMSO (up to 50 mg/ml) or in Ethanol (up to 25 mg/ml).Physical Properties:White solidPurity:98% by TLCStorage Temperature:RTStability:Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.Shipping Code:RT -
Mirin | Mre11-Rad50-Nbs1 inhibitor
From $50.00CAS:299953-00-7Catalog Number:10-1069Activity:Mre11-Rad50-Nbs1 inhibitorChemical Name:5-(4-Hydroxybenzylidene)-2-imino-1,3-thiazolidin-4-oneMolecular Weight:220.25Molecular Formula:C10H8N2O2SSolubility:Soluble in DMSO (up to 20 mg/ml).Physical Properties:Tan solidPurity:98% by TLC
NMR (Conforms)Storage Temperature:-20°CStability:Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.Shipping Code:RT
Calculate the molar concentration, mass or volume in a solution.
Concentration × Volume × Molecular Weight = Mass
