BChE Inhibitor

p38α-IN-13 is p38α MAPK, BChE and AChE inhibitor with IC₅₀ values of 5.79, 16.24, 51.8 µM for p38α MAP, hBChE, hAChE, respectively. p38α-IN-13 has the potential for the research of Alzheimer’s disease.

AChE-IN-59 (compounds 3b) is an AChE inhibitor, with an IC₅₀ value of 0.05 μM. AChE-IN-59 can inhibit the aggregation of Aβ1-42, protect nerve cells and penetrate the blood-brain barrier well. AChE-IN-59 can be used for the research of Alzheimer's disease (AD).

Desoxypeganine (Deoxypeganine) hydrochloride, 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 hydrochloride can be used for alcohol abuse research.

AChE/BChE-IN-3 (BMC-1) hydrochloride is a dual AChE and BChE inhibitor with IC₅₀ values of 6.08 μM and 0.383 μM against electric eel AChE (elAChE) and equine serum BChE (eqBChE), respectively.

MR2938 is a potent AChE inhibitor, with an IC₅₀ of 5.04 μM. MR2938 also suppresses NO production obviously (IC₅₀ = 3.29 μM). MR2938 suppresses the neuroinflammation through blocking MAPK/JNK and NF-κB signaling pathways. MR2938 can be used for Alzheimer’s disease (AD) research.

Icopezil (CP-118954) is an orally active, selective AchE inhibitor with an IC₅₀ of 0.33 nM. Icopezil increases acetylcholine levels in the brain and striatum of mammals, induces centrally mediated tremors and peripherally mediated salivation, and improves working memory performance in aged dogs. Icopezil serves as a parent compound for radioiodine-labeled acetylcholinesterase imaging agents. Icopezil is applicable to research related to Alzheimer's disease.

Multi-target kinase-IN-11 (compound 2a) is a potent multi-target inhibitor of Cholinesterase and Carbonic Anhydrase. Multi-target kinase-IN-11 inhibits AChE, BChE, hCA I, and hCA II with IC₅₀ values of 2.78, 4.88, 0.94, and 4.15 μM, respectively. Multi-target kinase-IN-11 inhibits these enzymes through hydrogen bonding and electrostatic interactions with active site residues. Multi-target kinase-IN-11 can be used for research on Alzheimer's disease.

BChE/AChE-IN-1 (Compound 4m) is a potent dual inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) with IC₅₀ values of 0.7 μM and 0.2 μM, respectively. BChE/AChE-IN-1 is promising for research of neurodegenerative diseases such as Alzheimer’s disease (AD).

AP2238 is a dual-function acetylcholinesterase (AChE) inhibitor with K_i values for human AChE (HuAChE) and butyrylcholinesterase (BuChE) of 21.7 and 48.9 μM respectively. AP2238 blocks the pro-fibrotic interaction between the peripheral site of AChE and Aβ, and can inhibit Aβ aggregation. AP2238 can be used for the research of Alzheimer's disease.

BChE-IN-10 (compound 6) is a potent butyrylcholinesterase (BChE) mixed-type inhibitor with an IC₅₀ value of 6.4 μM. BChE-IN-10 can be isolated from Bletilla striata. BChE-IN-10 can be used for the research of Alzheimer's disease (AD).

AChE-IN-122 is an acetylcholinesterase (AChE) and monoamine oxidase B (MAO-B) inhibitor with IC₅₀ values of 0.084 μM and 0.65 μM, respectively, and an IC₅₀ of 0.667 μM against butyrylcholinesterase (BuChE). AChE-IN-122 can be used for research on Alzheimer's disease.

CAI/II-IN-8 (Compound 8) is a hydrazide derivative based on 4-hydroxybenzaldehyde. CAI/II-IN-8 primarily targets human carbonic anhydrase isomerase I (hCA I) and II (hCA II) for inhibition (IC₅₀ = 21.35 ± 0.39 nM (CA I); 7.12 ± 0.12 nM (CA II)). CAI/II-IN-8 inhibits AChE and BChE as well(IC₅₀ = 46.27 ±0.75 nM (AChE); 43.38 ± 0.83 nM (BChE)). ..

S16–1029 is a selective and orally active butyrylcholinesterase (BChE) inhibitor with IC₅₀s of 11.35 nM and 48.1 nM for eqBChE and hBChE, respectively. S16–1029 could cross the blood-brain barrier (BBB) and reach the central nervous system (CNS). S16–1029 can be used for Alzheimer's disease (AD) research.

Multi-kinase-IN-10 (Compound IIIk) is a multi-kinase inhibitor. Multi-kinase-IN-10 exhibits significant calcium channel blocking activity, with its IC₅₀ being 26.67 μM. Multi-kinase-IN-10 is a potent dual cholinesterase inhibitor, with its IC₅₀ values for hAChE and hBuChE being 0.304 μM and 1.033 μM respectively. Multi-kinase-IN-10 has antioxidant and neuroprotective activities, and shows significant anti-amnesia activity. Multi-kinase-IN-10 can be used for research on Alzheimer's disease.

AChE/BChE-IN-37 is a blood-brain barrier-permeable AChE/BChE inhibitor, with an IC₅₀ of 73.65 μM against electric eel-derived AChE and an IC₅₀ of 82.93 μM against horse-derived BChE. AChE/BChE-IN-37 exhibits chelating activity towards Cu²⁺, Ca²⁺, Mg²⁺, Fe²⁺ and Zn²⁺. AChE/BChE-IN-37 interacts with HSP90AA1 and GSK-3β. AChE/BChE-IN-37 inhibits the self-induced aggregation of Aβ_1-42. AChE/BChE-IN-37 suppresses LPS-induced NO production in cells. AChE/BChE-IN-37 can be used in research related to Alzheimer's disease and inflammatory diseases.

Drofenine (Cycloadiphene; Hexahydroadiphenine) is an brain-penetrant antispasmodic agent. Drofenine is a Kv2.1 channel inhibitor with human IC₅₀ of 9.53 μM. Drofenine is a butyrylcholinesterase (BChE) inhibitor with K_i of 0.003 mM, and is a TRPV3 activator. Drofenine blocks Kv2.1-dependent potassium efflux, inhibits Kv2.1/JNK/NF-κB and IkBa/NF-kB signaling, suppresses Kv2.1 mRNA/protein expression. Drofenine suppresses oligomeric Aβ-induced microglial NLRP3 inflammasome activation and neuronal Tau hyperphosphorylation, improves cognitive impairment, promotes neurite outgrowth. Drofenine induces calcium influx in keratinocytes and exert cytotoxicity against keratinocytes. Drofenine ameliorates diabetic peripheral neuropathy -like pathology. Drofenine can be used for the researches of Alzheimer's disease, diabetic peripheral neuropathy and smooth muscle spasm.

BuChE-IN-4 (Compound C6) is a potent inhibitor of BuChE with an IC₅₀ of 7.7 nM. BuChE-IN-4 exhibits mild antioxidant capacity, nontoxicity, lipophilicity and neuroprotective activity.

hBChE-IN-3 (compound 30) is a combination of carbonic anhydrase (CA) activator and cholinesterase (ChE) inhibitor with IC50 values of 7.4 and 1.9 nM for AchE and BchE, respectively. hBChE-IN-3 can be used in the study of neurodegeneration and psychiatric disorders.

Brassicasteryl linoleate is a cholinesterase inhibitor. Brassicasteryl linoleate inhibits acetylcholinesterase, butyrylcholinesterase and urease. Brassicasteryl linoleate inhibits lipid peroxidation. Brassicasteryl linoleate is applicable to research related to breast cancer, lung cancer and colon adenocarcinoma.

hAChE-IN-3 (compounds 5c) is a potent and blood-brain barrier permeable AChE, BuChE， MAO-B-IN-1 and BACE-1 inhibitor, with IC₅₀ values of 0.44, 0.08, 5.15 and 0.38 μM, respectively. hAChE-IN-3 has antioxidant activity and metal chelating ability. In addition, hAChE-IN-3 can bind to peripheral anion sites, and affect β amyloid and reduce Alzheimer's-associated neurodegeneration. hAChE-IN-3 has the potential for the research of Alzheimer's disease.