AChE Inhibitor

AChE/BChE-IN-29 is an AChE/BChE inhibitor. AChE/BChE-IN-29 exhibits balanced dual cholinesterase inhibitory activity with IC₅₀ values of 2.1 μM for Electrophorus electricus AChE (eeAChE) and 6.3 μM for equine serum butyrylcholinesterase (eqBChE). AChE/BChE-IN-29 effectively inhibits amyloid-β (Aβ₄₂) aggregation and tau protein aggregation in E. coli cell models. AChE/BChE-IN-29 can be used for the study of Alzheimer’s disease (AD).

AChE/BChE/MAO-B-IN-3, an indan-1-one derivative, is a potent MAO-B inhibitor with an IC₅₀ of 0.0359 μM for human MAO-B. AChE/BChE/MAO-B-IN-3 is a potent AChE and BChE enzyme inhibitor, with IC₅₀s of 0.0473 μM and 0.0782 μM for human AChE and BChE enzyme, respectively. AChE/BChE/MAO-B-IN-3 shows significant antioxidant activity and has the potential for Alzheimer's disease (AD) research.

Y13g is the potent inhibitor of both AChE and IL-6. Interleukin-6 (IL-6) and acetylcholinesterase (AChE) are two important targets implicated in progression of Alzheimer's Disease (AD). Y13g reverses the STZ (HY-13753)-induced memory deficit, and shows histopathology similarly as in normal animals.

AChE-IN-35 (compound 5g) is an AChE inhibitor with the IC₅₀ of 5.88 μM.

AChE/BuChE-IN-7 is a dual-action inhibitor with an IC₅₀ valueof 0.15 μM for AChE and 0.7 μM for BuChE, SI of 4.7. AChE/BuChE-IN-7 shows anti-oxidant activity and can mitigate H₂O₂-induced cytotoxicity. AChE/BuChE-IN-7 has genomic stability and prolonged systemic availability. AChE/BuChE-IN-7 can be used for the research of neurological disease, such as Alzheimer's disease.

AChE-IN-91 (Compound 8u) is a AChE inhibitor with an IC₅₀ of 0.05 μM. AChE-IN-91 has significant anticholinesterase activity, promising for neurological diseases like Alzheimer's disease (AD) research.

Neuroprotective agent 18 is a potent neuroprotective agent. Neuroprotective agent 18 inhibits the activity of NF-κB thereby significantly downregulating the expression of downstream pro-inflammatory mediators (TNF-α, IL-6) and inflammatory enzymes (COX-2) in the hippocampus. Neuroprotective agent 18 binds to AChE thereby partially inhibiting it and modulating cholinergic neurotransmission. Neuroprotective agent 18 can be used in research on Alzheimer's disease.

TFSeB is an orally active neuroprotective agent. TFSeB can reduce Streptozotocin (STZ) (HY-13753) induced MAO-B and AChE activity. TFSeB exerts neuroprotective effects by increasing the expression of BCL-2, BDNF, NRF2, and decreasing the expression of BAX. TFSeB can reduce lipid peroxidation (TBARS) and reactive oxygen species (ROS) levels. TFSeB can reduce neuroinflammation. TFSeB can be used for research on Alzheimer’s disease.

Isocorydine N-oxide ((+)-Isocorydine N-oxide), an alkaloidal, a acetylcholinesterase (AChE) inhibitor. Isocorydine N-oxide can be used for the study of Alzheimer's disease.

AChE-IN-109 is a potent mixed-type cholinesterase inhibitor with significantly stronger inhibitory activity against AChE than BChE. AChE-IN-109 has IC₅₀ values of 0.55 μM and 12.45 μM against AChE and BChE, respectively. AChE-IN-109 inhibits cholinesterases through a mixed-type mechanism, binds to both the catalytic active site (CAS) and peripheral anionic site (PAS) of AChE. AChE-IN-109 can be used for the study of Alzheimer’s disease (AD).

BChE-IN-41 is a highly selective Butyrylcholinesterase (BChE) inhibitor (IC₅₀ =12 nM, K_i = 6.6 nM). BChE-IN-41 has high brain penetration with a brain-to-plasma ratio of 9.0. BChE-IN-41 has pro-cognitive effects on mice with AD-like symptoms induced by Scopolamine (HY-N0296) and Aβ_1-42.

SBN-284 (compound 3x) is a dual inhibitor of blood-brain permeable Cholinesterases and the NLRP3 inflammasome and is effective against EeAChE, hAChE and eqBChE, the IC₅₀ values of are 0.37, 0.31, 0.29 μM respectively, and the EC₅₀ of NLRP3 inflamm is 1 μM. SBN-284 can be used in Alzheimer's disease research.

MAO-IN-6 (Compound 3f) is a BBB permeable and reversible MAO-B inhibitor with an IC₅₀ of 0.09 μM. MAO-IN-6 also exhibits certain inhibitory activities against AChE and BChE, with IC₅₀ values of 4.48 μM and 17.03 μM, respectively. MAO-IN-6 has low cytotoxicity and can be used in the research of Alzheimer's disease.

AChE/BACE1/GSK3β-IN-1 is an orally active triple inhibitor of AChE/BACE1/GSK3β. AChE/BACE1/GSK3β-IN-1 has effective inhibitory activity against AChE, BACE1 and GSK3β with IC₅₀ values of 1.0 μM, 20 μM and 15 μM, respectively. AChE/BACE1/GSK3β-IN-1 has good blood-brain barrier penetrability, suitable bioavailability. AChE/BACE1/GSK3β-IN-1 can be used for the research of Alzheimer's disease (AD).

AChE/MAO-IN-1 (Compound D28) is a potent AChE, MAO-A and MAO-B inhibitor with IC₅₀s of 0.0248, 0.0409 and 0.1108 μM against human AChE, MAO-B and MAO-A, respectively.

Dyclonine (Dyclocaine) is an orally active, blood-brain barrier-permeable piperidine phenylacetone small molecule commonly used as a local anesthetic. Dyclonine acts as a highly selective allosteric antagonist of TRPV3; it also reversibly inhibits G9a, ALDH2 and ALDH3A1, non-competitively blocks AChE. Dyclonine activates the Nrf2/ARE pathway, relieves the epigenetic silencing of FXN, blocks Aβ42 aggregation, and promotes remyelination and reparative polarization of microglia. Dyclonine alleviates pruritus via TRPV3 inhibition; it is used in studies of neurodegenerative disease models based on its AChE inhibitory, antioxidant and remyelinating effects; it sensitizes drug-resistant tumors through ALDH inhibition, and combined use with protease inhibitors induces more tumor cell apoptosis; it inhibits Candida albicans in vitro. Dyclonine can be used for research on multiple diseases including neurodegenerative diseases, cancer and pruritic dermatitis.

(+)-(R)-Ribalinine (Folifine) is an inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), with an IC₅₀ value of 153.31 μM against electric eel acetylcholinesterase and an IC₅₀ value of 12.99 μM against equine butyrylcholinesterase.

AChE-IN-94 is an orally active and blood-brain barrier penetrable AChE inhibitor with an IC₅₀ of 0.40 μM and K_i of 0.28 μM. AChE-IN-94 prevents self-induced and AChE-mediated Aβ_1-42 aggregation. AChE-IN-94 alleviates cognitive/memory deficits in Scopolamine (HY-N0296)-induced amnesic model. AChE-IN-94 can be used for the study of Alzheimer's disease (AD).

AChE-IN-22 (compound 10q) is a selective acetylcholinesterase (AChE) inhibitor against AChE and BuChE with the IC₅₀ values of 0.88 μM and 10 μM, respectively. AChE-IN-22 can bind to both the CAS (catalytic active site) and PAS (peripheral anionic site) of AChE and has the potential for the research of Alzheimer's disease.

BChE/MAO-B-IN-2 is a dual inhibitor of BChE (IC₅₀ = 0.05 μM, K_i = 0.01 μM) and MAO-B (IC₅₀ = 0.45 μM, K_i = 0.08 μM) with good blood-brain barrier permeability. BChE/MAO-B-IN-2 exhibits antioxidant activity, including DPPH radical scavenging, CUPRAC copper ion reduction, and superoxide anion scavenging. BChE/MAO-B-IN-2 can be used for the study of Alzheimer's disease (AD).