AChE-IN-14 is a potent cholinesterase inhibitor with IC50s of 0.46 , 0.48, and 0.44 μM for electric eel acetylcholinesterase (eeAChE), human recombinant acetylcholinesterase (hAChE), and equine serum butyrylcholinesterase (eqBuChE), respectively. AChE-IN-14 exhibits high affinity toward human H3 receptor (H3R; Ki= 159.8 nM). AChE-IN-14 can be used for the research of Alzheimer’s disease[1].
(S)-Donepezil is a S-enantiomer of Donepezil (HY-14566). Donepezil is a specific and potent AChE inhibitor[1][2].
Corydaline is an acetylcholinesterase inhibitor isolated from Corydalis yanhusuo.
Polygalacic acid, is a triterpene, isolated from the root of Polygala tenuifolia Willd. Polygalacic acid inhibits MMP expression. Polygalacic acid may have a therapeutic effect in Osteoarthritis (OA) treatment [1]. Polygalacic acid exerts a significant neuroprotective effect on cognitive impairment, PA improves cholinergic system reactivity by inhibiting acetylcholinesterase (AChE) activity, increasing choline acetyltransferase (ChAT) activity, and elevating levels of acetylcholine (Ach) in the hippocampus and frontal cortex[2].
AChE/BuChE-IN-3 (compound C4) is a potent and blood-brain barrier (BBB) penetrant AChE and BuChE dual inhibitor with IC50s of 0.65 μM and 5.77 μM for AChE and BuChE. AChE/BuChE-IN-3 also inhibits Aβ1-42 aggregation. AChE/BuChE-IN-3 has effectively neuroprotective activities and nearly no toxicity on SH-SY5Y cells. AChE/BuChE-IN-3 can be used for researching Alzheimer's disease[1].
Pteryxin, a coumarin in Peucedanum japonicum Thunb leaves, exerts antiobesity activity[1]. Pteryxin is a potent butyrylcholinesterase (BChE) inhibitor, with an IC50 of 12.96 μg/ml[2].
Swertianolin, a xanthone isolated from Gentianella Acuta, inhibits acetylcholinesterase (AChE). Swertianolin also exhibits anti-HBV and anti-bacterial activity[1][2].
Pirimicarb is a fast-acting selective carbamate insecticide on a wide range of crops including cereals, sugar beet, potatoes, fruits and vegetables. Pirimicarb is an AChE inhibitor and an acaricide[1].
HY-101653 is a drug with multiple CNS targets, and inhibits acetylcholinesterase (AChE) with Ki of 69 μM; also active against muscarinic M1 and M2 receptors, serotonin 5HT4 receptors, and imidazole I2 receptors.
Galanthamine-d6 (Galantamine-d6) is the deuterium labeled Galanthamine. Galanthamine is a potent acetylcholinesterase (AChE) inhibitor with an IC50 of 500 nM[1][2].
AChE/BChE-IN-5 (BMC-16) is a dual AChE and BChE inhibitor with IC50 values of 266 nM and 10.6 nM against human AChE (hAChE) and human BChE (hBChE), respectively. AChE/BChE-IN-5 can cross the BBB[1].
Pirimiphos-methyl is a rapid-acting organophosphorus insecticide and acaricide, causing inhibition of AChE in target organisms. Pirimiphos-methyl is often used for prevention and control of beetles, snout beetles, moths and Ephestia cautella during storage of agricultural grains[1][2][3].
(-)-Carvone is an insect neurotoxin and a irreversible acetylcholinesterase (AChE) inhibitor. (-)-Carvone can be used as a bird repellent, inhibits larval growth, decreases pupatation rate, and increases mortality of larvae[1][2].
Manghaslin is a flavonoid glycoside with anti-inflammatory activities. Manghaslin shows inhibitory activity against AChE with an IC50 of 94.92 µM[1][2].
Demecarium Bromide (BC-48) is a potent cholinesterase inhibitor, with an apparent affinity (Kiapp) of 0.15 μM[1]. Demecarium Bromide (BC-48) is used as a glaucoma agent[2].
AChE-IN-12 is a potent and blood-brain barrier (BBB) penetrant acetylcholinesterase (AChE) with IC50s of 0.41 μM and 1.88 μM for rat AChE and electric eel AChE. AChE-IN-12 is also a good antioxidant (ORAC = 3.3 eq), selective metal chelator and huMAO-B inhibitor (IC50 = 8.8 µM). AChE-IN-12 has remarkable inhibition of self- and Cu2+-induced Aβ1-42 aggregation, as well as exhibits a good neuroprotective effect. AChE-IN-12 can be used for researching Alzheimer’s disease[1].
Galanthamine is a potent acetylcholinesterase (AChE) inhibitor with an IC50 of 500 nM.
BChE-IN-20 (compound 7c) is a highly potent BChE-selective inhibitor and exhibits IC50s of 105 and 2.3 nM for eqBChE and hBChE, respectively. BChE-IN-20 inhibits P glycoprotein with IC50 of 0.27 μM. BChE-IN-20 is a promising template to improve design and development of BChE-selective ligands of pharmaceutical interest, including inhibitors and fluorogenic probes.
BChE-IN-17 (compound 6n) is a potent and selective BChE inhibitor with IC50s of 10.5 nM and 32.5 nM for eqBChE and hBChE, respectively. BChE-IN-17 shows over 1000-fold selectivity to BChE against AChE. BChE-IN-17 shows low neurotoxicity and moderate neuroprotective effects[1].
Resorufin butyrate is a fluorogenic substrate for triglyceride lipases and cholinesterase (Ex=570 nm, Em=580 nm)[1][2][3].
Pralidoxime chloride is a useful agent in the treatment of organophosphate poisoning. Pralidoxime binds to organophosphate-inactivated acetylcholinesterase, used to combat poisoning by organophosphates or acetylcholinesterase inhibitors (nerve agents) in conjunction with atropine and diazepam.
Benactyzine hydrochloride is a butyrylcholinesterase (BChE) inhibitor with a Ki of 0.010 mM.
Edrophonium chloride is a readily reversible acetylcholinesterase inhibitor; prevents breakdown of the neurotransmitter acetylcholine and acts by competitively inhibiting the enzyme acetylcholinesterase, mainly at the neuromuscular junction.
Galanthamine hydrobromide is a long-acting, centrally active acetylcholinesterase(AChE) inhibitor (IC50 = 410 nM) and allosteric potentiator at neuronal nicotinic ACh receptors. IC50 Value: 410 nM Target: AChEGalanthamine hydrobromide prevents β-amyloid-induced apoptosis in SH-SY5Y and bovine chromaffin cells. Long-term administration reduces amyloid precursor protein deposition and neurodegeneration in a mouse model of Alzheimer's disease.
Aloveroside A is a triglucosylnaphthalene derivative isolated from ethanolic extract of aloe vera. Aloveroside A has weak bACE inhibitory activity (inhibition rate at a dose of 100 μg/mL is approximately 18.68%)[1].
(-)-Corynoxidine is an acetylcholinesterase inhibitor with an IC50 value of 89.0 μM, isolated from the aerial parts of Corydalis speciosa[1].(-)-Corynoxidine exhibits antibacterial activities against Staphylococcus aureus and methicillin-resistant S. aureus strains in different degrees[2].
hBChE-IN-2 (compound 15d) is a butyrylcholinesterase (BChE) inhibitor (IC50 of 0.62 μM) and a cannabinoid receptor 2 (CB2R) agonist. hBChE-IN-2 has neuroprotection activities[1].
PE154 (Compound 13) is a potent fluorescent inhibitor of human acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) (IC50s=280 pM and 16 nM, respectively)[1]. PE154 can label β-amyloid plaques in histochemical analysis[2].
BChE/HDAC6-IN-1 is a potent and selective dual BChE/HDAC6 inhibitor with IC50 values of 4 and 8.9 nM, respectively. BChE/HDAC6-IN-1 ameliorates the cognitive impairment in an Aβ1–42-induced mouse model and has the potental for AD research[1].
Protopine hydrochloride, an isoquinoline alkaloid, is a specific reversible and competitive inhibitor of acetylcholinesterase. Protopine hydrochloride exhibits anti-inflammation, anti-microbial, anti-angiogenic and anti-tumour activity[1][2].