AChE Inhibitor

Magnotriol B is a cholinesterase inhibitor with IC₅₀ values of 12.63 nM and 14.5 nM against AChE and BChE, respectively. Magnotriol B also exhibits significant NO inhibitory activity with an IC₅₀ of 2.02 μM. Magnotriol B can be used in the research of neurodegenerative and inflammatory diseases.

hAChE-IN-2 is a potent hAChE inhibitor, with an IC₅₀ of 0.71 μM. hAChE-IN-2 can also inhibits tau-oligomerization, with an EC₅₀ of 2.21 μM. hAChE-IN-2 exhibits neuroprotective activity.

AChE-IN-75 (N-(2′-methyl)allylnorgalanthamine) is an AChE inhibitor. AChE-IN-75 can be used in Alzheimer's disease research.

AChE/MAO-B-IN-3 (Compound D30) is a dual AChE and MAO-B inhibitor with IC₅₀s of 0.0257 μM and 0.0456 μM against human AChE and MAO-B, respectively. AChE/MAO-B-IN-3 can be used for the research of Alzheimer’s disease.

Picfeltarraenin X, a triterpenoid isolated, is an AChE inhibitor.

MR33317 is an inhibitor of acetylcholinesterase with an IC₅₀ value of 41nM. MR33317 is also an agonist at brain 5-HT₄ receptors.

CAI/II-IN-5 (compound MZ8) is a potent hCA I and hCA II (human carbonic anhydrase isoenzymes I and II) inhibitor, with IC₅₀ values of 37.88 and 45.23 nM, respectively. CAI/II-IN-5 also shows inhibition profile against α-Glycosidase and AChE, with IC₅₀ values of 48.98 and 420.14 nM, respectively. CAI/II-IN-5 can be used for the research of many diseases such as diabetes, Alzheimer’s disease, heart failure, ulcer, and epilepsy.

H3R antagonist 4 (compound 11L) was a dual inhibitor of cholinesterase and histamine receptor (H3R), with corresponding IC₅₀ of 7.04 μM (eeAChE), 9.73 μM (hAChE)(reversible) and 1.09 nM (H3R) , respectively. H3R antagonist 4 inhibited the aggregation of Aβ_1-42 induced by itself and Cu²⁺ (95.48% and 88.63%) , and degraded the Aβ_1-42 fibrils induced by itself and Cu²⁺ (80.16% and 89.30%) . H3R antagonist 4 chelate biometals such as Cu²⁺, Zn²⁺, Al³⁺, and Fe²⁺. H3R antagonist 4 significantly reduced tau protein hyperphosphorylation induced by Aβ_1-42 and inhibited RSL-3-induced apoptosis and ferroptosis in PC12 cells. H3R antagonist 4 had the best blood-brain barrier permeability and intestinal absorption in hCMEC/D3 and hPepT1-MDCK cells.H3R antagonist 4 ameliorates learning and memory impairment in a mouse model of Alzheimer's disease induced by scopolamine (HY-N0296) .

Multitarget AD inhibitor-2 (Compound VN-19) is a multitargeting inhibitor acetylcholinesterase (AChE, IC₅₀=0.14 μM), butyrylcholinesterase (BChE, IC₅₀=11.6 μM), monoamine oxidase B (MAO B, IC₅₀=0.45 μM). Multitarget AD inhibitor-2 inhibits self-induced aggregation of amyloid beta protein Aβ1-42 (inhibition rate is 47.3% at 20 μM), and downregulates the level of ROS in SH-SY5Y (80 inhibition rate at 25 μM). Multitarget AD inhibitor-2 ameliorates the cognitive decline in Scopolamine (HY-N0296)-induced Alzheimer’s Disease zebrafish models.

hAChE/hBACE-1-IN-1 (compounds 5d) is an orally active inhibitor of hAChE with blood-brain permeability. hAChE/hBACE-1-IN-1 inhibits hAChE and hBACE-1 with IC₅₀ values of 0.076 and 0.23 μM, respectively. hAChE/hBACE-1-IN-1 inhibits Aβ_1-42 aggregation and improves mouse learning and memory ability. hAChE/hBACE-1-IN-1 can be used to research in Alzheimer's disease.

AChE-IN-98 (Compound 26) is an AChE inhitibor, with an IC₅₀ value of 7.3 μM for ee AChE. AChE-IN-98 is also a Coumarin (HY-N0709) derivative. AChE-IN-98 can be used in the research of Alzheimer's disease.

K1833 is a hrAChE inhibitor/reactivator, with an IC₅₀ of 58 μM. K1833 also shows high inhibition (IC₅₀=0.57μM) and low reactivation for hrBChE.

AChE/CA I-IN-1 (Compound 2g) is the inhibitor for AChE and hCA I with K_i of 1.85 and 0.53 µM. AChE/CA I-IN-1 exhibits potential application in researches about Alzheimer's disease, glaucoma, and epilepsy.

Desoxypeganine (Deoxypeganine), an alkaloid, is a potent and orally active cholinesterase (BChE and AChE) and selective MAO-A inhibitor, with IC₅₀ values of 2, 17, and 2 μM, respectively. Desoxypeganine can be used for alcohol abuse research.

Multitarget AD-IN-5 (Compound 20), 9-Aminoacridine (HY-B1422) derivative, is a neuroprotective agent. Multitarget AD-IN-5 shows IC₅₀ values of 0.614, 0.448, 3.73 and 1.55 μM for hAChE, hBChE, hMAO-A and hMAO-B. Multitarget AD-IN-5 can reduce length and diameter of Aβ₄₂ fibers, and decrease the number of fibers per unit area. Multitarget AD-IN-5 can be used for research of Alzheimer's disease.

BChE-IN-48 (Compound 12a) is a BChE inhibitor that can cross the blood-brain barrier with IC₅₀ values for eqBChE and huBChE of 1.3 and 0.95 μM respectively. BChE-IN-48 exhibits an IC₅₀ value for eeAChE of 8.6 μM. BChE-IN-48 exhibits significant neuroprotective activity in cell damage and significantly improves cognitive impairment in mouse models. BChE-IN-48 can be used for research on Alzheimer's disease.

AJ-4 is an orally active, blood-brain barrier-permeable GSK-3β/AChE inhibitor, with an IC₅₀ of 4.7 nM against GSK-3β and 2.97 μM against AChE. AJ-4 increases the level of phosphorylated GSK-3β and reduces the expression of Amyloid-β and phosphorylated Tau. AJ-4 improves scopolamine-induced learning and memory impairment and alleviates hippocampal neuron damage in AD mice. AJ-4 can be used for the research of Alzheimer's disease.

AChE/BChE-IN-12 (compound 10b), a 3,5-dimethoxy analogue, is a potent AChE, BChE, and β-secretase-1 (BACE-1) inhibitor, with IC₅₀ values of 2.57, 3.26, and 10.65 μM, respectively. AChE/BChE-IN-12 crosses the blood-brain barrier via passive diffusion and inhibits the self-aggregation of amyloid-β monomers. AChE/BChE-IN-12 can be used for Alzheimer’s disease (AD) research.

ω-Hydroxydigitoemodin is an anthraquinone derivative with anti-acetylcholinesterase activity, found in the marine fungus Trichoderma harzianum XS-20090075.

AChE-IN-105 (Compound C5) is a potent, mixed AChE inhibitor with an IC₅₀ of 5.02 μM. AChE-IN-105 scavenges ROS, decreases Hydrogen peroxide-induced Caspase-3 activation, reduces activity of the Nrf2-ARE pathway. AChE-IN-105 prevents memory impairments in the Scopolamine (HY-N0296)-induced cognitive dysfunction zebrafish model. AChE-IN-105 has potent antioxidant activity. AChE-IN-105 can be used in the research of Alzheimer's disease.