AChE/BuChE-IN-2 (Compound 5f) is an orally active AChE and BuChE inhibitor with IC50 values of 0.72 μM and 0.16 μM, respectively. AChE/BuChE-IN-2 shows a non-competitive inhibition with AChE and shows potent self-induced β-amyloid (Aβ) aggregation inhibition with an IC50 of 62.52 μM. AChE/BuChE-IN-2 can cross the BBB[1].
Dehydrogeijerin is an inhibitor of acetylcholinesterase with an IC50 of 9.7 μM. Dehydrogeijerin can be used in study Alzheimer’s disease[1].
Cyanidin-3-O-galactoside chloride (Ideain chloride) is a component from extract peel of hawthorn fruit (EPHF) with the value of 179.4 mg/g. EPHF exhibits strong AChE inhibitory activity[1].
AChE-IN-27 (compound 8c) is an AChE inhibitor (IC50=0.19 µM). AChE-IN-27 can be used in studies of neurological diseases such as alzheimer's disease, dementia, ataxia and myasthenia gravis[1].
AChE/BChE-IN-9 (Compound 7a) is a potent, orally active AChE and BChE inhibitor with IC50 values of 5.74 μM and 14.05 μM against hAChE and eqBChE, respectively. AChE/BChE-IN-9 is also an efficacious antioxidant with an IC50 of 57.35 μM. AChE/BChE-IN-9 is able to chelate iron and modulates aggregation of amyloid β1-42. AChE-IN-16 can cross the BBB[1].
(+)-Phenserine is a novel selective cholinesterase noncompetitive inhibitor with an IC50 of 45.3 μM.
Pirimiphos-methyl-d6 is the deuterium labeled Pirimiphos-methyl. 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].
AChE/BChE-IN-4 (BMC-3) is a dual AChE and BChE inhibitor with IC50 values of 792 nM and 2.2 nM against human AChE (hAChE) and human BChE (hBChE), respectively. AChE/BChE-IN-4 can cross the BBB[1].
Broussonin A is a potent BChE inhibitor, with an IC50 of 4.16 µM. Broussonin A is a diarylpropane natural product that can be isolated from the bark of Broussonetia papyrifera after solid fermentation[1][2][3].
Lanuginosine (Compound 12) is an AChE inhibitor (IC50: 10.9 μM). Lanuginosine inhibits Aβ aggregation. Lanuginosine can be used for research of Alzheimer’s disease[1].
(Rac)-Sclerone is a natural product, that can be isolated from the green husk of Carya illinoinensis. (Rac)-Sclerone shows appreciable inhibition of AChE, with an IC50 of 192.65 ± 10.12 μg/mL[1].
Axillaridine A can be isolated from Sarcococca hookeriana var. digyna. Axillaridine A inhibits the catalytic activity of AChE[1].
Acetylcholinesterase (ACHE; EC 3.1.1.7) is a cholinergic enzyme mainly found in neuromuscular junctions and cholinergic type chemical synapses, and is often used in biochemical research. Acetylcholinesterase catalyzes the breakdown or hydrolysis of acetylcholine and some other choline esters that act as neurotransmitters into acetate and choline. Acetylcholinesterase's main role is to terminate neuronal transmission and signaling between synapses to prevent ACh spread and activation of nearby receptors[1].
RPR121056 (APC) is a metabolite of Irinotecan (CPT-11), which is generated by CYP3A4. Irinotecan (CPT-11) is an antineoplastic agent that inhibits topoisomerase type I, causing cell death, and is widely used in the treatment of colorectal cancer. Irinotecan also directly inhibits AChE[1].
Drofenine hydrochloride is a potent competitive inhibitor of BChE, and the ki values of Drofenine is calculated to be 3 uM.IC50 value: 3 uM (ki)Target: BChEBenactyzine is widely used anticholinergic drugs, acts on smooth muscle to stop muscle spasms.
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].
Lycoramine hydrobromide, a dihydro-derivative of galanthamine, is isolated from Lycoris radiate. Lycoramine hydrobromide is a potent acetylcholinesterase (AChE) inhibitor[1][2].
Physostigmine hemisulfate (Eserine hemisulfate) is a potent cholinesterase inhibitor. Physostigmine hemisulfate crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine hemisulfate induces reanimation from isoflurane anesthesia in adult rats[1].
Ambenonium (WIN 8077) chloride is an orally active and reversible inhibitor of Acetyicholinesterase (AChE) with high affinity. Ambenonium chloride inhibits human AChE with an IC50 value of 0.7 nM (hAChE)[1][2].
BuChE-IN-5 (compound 25b) is a potent BuChE inhibitor with an IC50 value of 1.94 μM. BuChE-IN-5 efficiently inhibits aggregation Aβ and tau protein in Escherichia coli. BuChE-IN-5 also has free radical scavenging capacity and antioxidant activity. BuChE-IN-5 can be used for researching Alzheimer’s disease[1].
AChE-IN-23 (compound 3h) is an acetylcholinesterase (AChE) inhibitor with an IC50 value of 48.3 μM[1].
BChE-IN-13 (Compound 17c) is an orally active, potent and selective Butyrylcholinesterase (BChE) inhibitor with IC50s of 0.22 and 0.016 μM for eqBChE and hBChE, respectively. BChE-IN-13 can improve memory and cognitive impairments, and be used in Alzheimer’s disease (AD) research[1].
Azamethiphos is an organophosphate insecticide and a neurotoxic agent, causing acetylcholinesterase (AChE) inhibition[1].
Isoprocarb-d3 is deuterium labeled Isoprocarb. Isoprocarb is carbamate insecticide that widely used to control rice paddy lice and leafhopper. Isoprocarb is also an AChE inhibitor[1].
Monarsen (EN101) is a synthetic 20-base antisense oligodeoxynucleotide directed against the human AChE gene. Monarsen is used in the study of Autoimmune myasthenia gravis (MG), a neuromuscular disorder caused by autoantibodies directed against the acetylcholine receptor (AChR).
BuChE-IN-6 (compound 1b) is a potent and selective BuChE (butyrylcholinesterase) inhibitor, with IC50 values of 0.46 and 0.51 μM for eqBuChE and hBuChE, respectively. BuChE-IN-6 also inhibits Aβ42 self-aggregation[1].
Huperzine C is an alkaloid isolated from Huperzia serrate. Huperzine C is an acetylcholinesterase (AChE) inhibotor, with an IC50 of 0.6 μM. Huperzine C can be used for the research of Alzheimer’s Disease[1][2].
Picfeltarraenin IB, a triterpenoid obtained from Picriafel-terrae Lour (P.fel-terrae), is an acetylcholinesterase (AChE) inhibitor. Picfeltarraenin IB can be used for the treatment of herpes infections, cancer and inflammation[1].
AChE/BChE/MAO-B-IN-1 (Compound 10) is a reversible and non-time-dependent AChE, BChE and MAO-B inhibitor with IC50 values of 7.31, 0.56 and 26.1 μM for hAChE, hBChE and hMAO-B, respectively. AChE/BChE/MAO-B-IN-1 can cross the BBB and shows neuroprotective effects without cytotoxicity[1].
Fasciculin-II (Fas-2) is a potential inhibitor of acetylcholinesterase (AChE)[1].