Protriptyline is a potent antidepressant agent. Protriptyline inhibits AChE activity with IC50 value of 0.06 mM and inhibits Aβ Self-Assembly. Protriptyline can be used for depression and Alzheimers disease[1][2][3].
Epiberberine chloride, a natural alkaloid, is a BACE1 inhibitor, which also exhibits inhibition activity on CYP2D6 and aldose reductase, alpha-adrenoceptors, acetylcholinesterase (AChE), butyrylcholinesterase, and b-site amyloid precursor protein cleaving enzyme 1.
Neoeriocitrin, isolated from Drynaria Rhizome, shows activity on proliferation and osteogenic differentiation in MC3T3-E1. Neoeriocitrin is a potent acetylcholinesterase (AChE) inhibitor[1][2].
RX 67668 is a potent cholinesterase inhibitor with an IC50 of 5 μM for both acetylcholinesterase (AChE) and butyrylcholinesterase. RX 67668 can reverse the neuromuscular blockade induced by D-tubocurarine. RX 67668 is a muscle relaxant used to relieve skeletal muscle fatigue[1][2].
Cyclophostin is an acetylcholinesterase (AChE) inhibitor with IC50 values of 45, 0.76 and 1.3 nM for humans and two different insects, respectively[1].
Picfeltarraenin IA, a triterpenoid obtained from Picriafel-terrae Lour (P.fel-terrae), is an acetylcholinesterase (AChE) inhibitor. Picfeltarraenin IA can be used for the treatment of herpes infections, cancer and inflammation[1].
Pralidoxime is a potent reactivator of acetylcholinesterase (AChE). Pralidoxime reactivates nerve agent-inhibited AChE via direct nucleophilic attack by the oxime moiety on the phosphorus center of the bound nerve agent. Pralidoxime is an antidote for organophosphate poisoning[1][2].
Rivastigmine carbamate impurity (3-Nitrophenyl ethyl(methyl)carbamate) is an impurity of Rivastigmine. Rivastigmine is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM, 4.15 μM, respectively[1][2].
Donepezil-d5 (hydrochloride) is deuterium labeled Donepezil (Hydrochloride). Donepezil Hydrochloride (E2020) is a reversible, selective AChE inhibitor with an IC50 of 6.7 nM for AChE activity. Donepezil shows high selectivity for AChE over BuChE[1]. Donepezil exhibits neuroprotective effect on Aβ42 neurotoxicity[2].
Depramine (GP 31406) is a tricyclic antidepressant with pharmacologically activity. Depramine inhibits acetylcholinesterase，Mg2+-ATPase，and Na+/K+ ATPase activity[1][2].
SD-6 is an orally active inhibitor of hAChE and hBChE with IC50 values of 0.907 µM and 1.579 µM, respectively. SD-6 has excellent blood-brain barrier (BBB) permeability and no neurotoxicity, which can be used for research on Alzheimer's disease[1].
Jatrorrhizine hydroxide is an alkaloid isolated from Coptis chinensis with neuroprotective, antimicrobial, antiplasmodial and antioxidant activities[1]. Jatrorrhizine hydroxide is a potent and orally active inhibitor of AChE (IC50=872 nM) over >115-fold selectivity for BuChE[2]. Jatrorrhizine hydroxide reduces uptake of serotonin (5-HT) and norepinephrine (NE) via inhibition of uptake-2 transporters[3].
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].
BuChE-IN-TM-10 (TM-10) is a potent butyrylcholinesterase (BuChE) inhibitor, with an IC50 of 8.9 nM. BuChE inhibitor 1 inhibits and disaggregates self-induced Aβ aggregation, exhibiting potent antioxidant activity and good blood-brain barrier (BBB) penetration. Has potential to treat Alzheimer’s disease[1].
Memoquin is an anti-amyloid and anti-oxidant multi-target-directed ligand. Memoquin is an orally active inhibitor of BACE-1 and AChE with IC50 values of 108 and 1.55 nM, respectively. Memoquin is a cognitive enhancer that prevents the Aβ-induced neurotoxicity mediated by oxidative stress. Memoquin can be used for the research of Alzheimer’s disease (AD)[1][2].
BChE-IN-9 (Azepano-11-deoxo-glycyrrhetol) is a mixed type BChE inhibitor with a Ki of 0.21 µM[1].
SB-1436 is an Cholinesterase (ChE) inhibitor, inhibits acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and recombinant human acetylcholinesterase (rHuAChE) with IC50s of 0.176, 0.37 and 0.08 μM, respectively. SB-1436 inhibits AChE and BChE in a non-competitive manner with Kis of 0.046 and 0.115 μM, respectively. SB-1436 significantly stops the self-aggregation of Aβ, and can be used for neurological disease research[1].
AChE-IN-21 (Compound I-8) is a potent, selective and orally active AChE inhibitor with an IC50 of 2.66 nM. AChE-IN-21 displays excellent BBB permeability in vitro[1].
Bleformin A is a potent BChE inhibitor with an IC50 value of 5.2 μM. Bleformin A is a nature product that could be isolated from Bletilla striata. Bleformin A can be used for research of Alzheimer's disease (AD)[1].
Methylene Violet 3RAX is a phenazine dye to stain the mitochondria of cells. Methylene Violet 3RAX can change the molecular structure of DNA, undermine the module of DNA, and induce the generation of the reactive singlet oxygen. Methylene Violet 3RAX shows inhibition for human erythrocyte AChE and human plasma BChE with an Kis of 1.58, 0.51 μM, respectively. Methylene Violet 3RAX has the potential for the research of potential photosensitizers for mitochondrial targeting action in PDT (photodynamic therapy)[1][2].
BChE-IN-6 (compound 12) is a potent BChE inhibitor, with a Ki of 0.182 μM. BChE-IN-6 shows chelating capacity on Zn2+. BChE-IN-6 can be used for Alzheimer’s disease (AD) research[1].
Fenitrothion-d6 is the deuterium labeled Fenitrothion[1]. Fenitrothion, one of the most widely used organophosphorus pesticides, is a cholinesterase inhibiting insecticide/acaricid. Fenitrothion is widely used, as a broad-spectrum insecticide, on cotton crops, vegetables crops, fruit crops, and field crops especially paddy. Fenitrothion leads to accumulation of nitrophenols[2][3].
Dehydrodiscretamine chloride is a dual inhibitor of AChE and BChE with IC50s of 17.8 and 118.8 μM, respectively. Dehydrodiscretamine chloride has antioxidant activity. Dehydrodiscretamine chloride can be used in study Alzheimer’s disease[1].
AChE/GSK-3β-IN-1 (compound GT15) is a potent, dual AChE/GSK-3β inhibitor with IC50 values of 1.2, 149.8 and 22.4 nM for hAChE , hBChE and hGSK-3β, respectively. AChE/GSK-3β-IN-1 penetrates the blood-brain barrier (BBB). AChE/GSK-3β-IN-1 has high kinase selectivity profiles for the CMGC kinase family. AChE/GSK-3β-IN-1 occupies the ATP binding site of DYRK1A. AChE/GSK-3β-IN-1 inhibits ROS expression and reduces oxidative stress. AChE/GSK-3β-IN-1 can be used for Alzheimer’s disease research[1].
Corynoline, isolated from Corydalis incise (Papaveraceae), is a reversible and noncompetitive acetylcholinesterase (AChE) inhibitor with an IC50 of 30.6 μM[1]. Corynoline exhibits anti-inflammatory activity by activating Nrf2[2].
AChE-IN-44 (Compound Tap4) is an AChE inhibitor. AChE-IN-44 can be converted into the thiazole salt AChE inhibitor Tat2[1].
Itopride (HSR803 free base) is a potent and orally active dopamine-2 antagonist and an acetylcholine esterase (AChE) inhibitor. Itopride enhances gastric motility through both antidopaminergic and anti-acetylcholinesterasic actions, can be used as a gastrointestinal prokinetic agent. Itopride can be used for researching gastro-esophageal reflux disease (GERD)[1].
Galanthamine N-Oxide-d3 is the deuterium labeled Galanthamine N-Oxide. Galanthamine N-Oxide is an alkaloid obtained from the bulbs of Zephyranthes concolor. Galanthamine N-Oxide inhibits electric eel acetylcholinesterase (AChE) with an EC50 of 26.2 μM. Galanthamine N-Oxide is a prominent inhibitor of substrate accommodation in the active site of the Torpedo californica AChE (TcAChE), hAChE and hBChE enzymes[1][2][3].
Huperzine B is a Lycopodium alkaloid isolated from Huperzia serrata and a highly selective acetylcholinesterase (AChE) inhibitor. Huperzine B can be uesd to can be used to improve Alzheimer's disease[1][2].
Obidoxime dichloride is a non-full spectrum oxime agent and can be used as an antidote for organophosphate nerve agent poisoning. Obidoxime dichloride reactivates sarin-inhibited acetylcholinesterase (AChE) and reduces acute toxicity of sarin-evaluated[1].