BChE Inhibitor

AChE/BuChE-IN-9 is a dual Cholinesterase inhibitor that acts on electric eel acetylcholinesterase (AChE) (IC₅₀ = 14.82 μM) and horse serum butyrylcholinesterase (IC₅₀ = 27.91 μM) through non-competitive and mixed-mode inhibition, respectively. AChE/BuChE-IN-9 can be used for research on Alzheimer's disease.

α-Amylase/α-Glucosidase-IN-7 (Compound 3f) is a competitive α-glucosidase and α-amylase enzyme inhibitor with IC₅₀ values of 18.52 and 20.25 µM, respectively. α-Amylase/α-Glucosidase-IN-7 can also effectively inhibit AChE and BChE, with IC₅₀ values of 9.25 and 10.06 µM respectively. α-Amylase/α-Glucosidase-IN-7 can be used in diabetes and Alzheimer’s research.

AChE-IN-63 (Compound 5AD) is a selective inhibitor of hAChE (IC₅₀=0.103 μM). AChE-IN-63 also inhibits hBChE and hBACE-1 (IC₅₀= 10 μM (hBChE); 1.342 μM (hBACE-1)). AChE-IN-63 inhibits Aβ aggregation, preventing the formation and deposition of Aβ1-42. AChE-IN-63 can effectively penetrate the blood-brain barrier and is orally effective. It is primarily used in Alzheimer's disease research.

BChE-IN-34 is a potent and selective butyrylcholinesterase (BChE) inhibitor with an IIC₅₀ of 25 nM. BChE-IN-34 shows excellent selectivity against BChE over acetylcholinesterase. BChE-IN-34 has neuroprotective and antioxidant effects.

Methyl isoplatydesmine is a cholinesterase inhibitor with spasmolytic activity, with a K_i value of 30.0 μM against electric eel acetylcholinesterase and a K_i value of 19.0 μM against horse serum butyrylcholinesterase. Methyl isoplatydesmine mediates spasmolytic activity by blocking voltage-dependent calcium channels. Methyl isoplatydesmine can be used in the research of Alzheimer's disease and related dementias.

BChE-IN-22 (compound 5A) is a selective eqBChE inhibitor (IC₅₀: 0.53 μM), has anti-inflammatory and neuroprotective activities. BChE-IN-22 can inhibit cell damage caused by Aβ_25-35 (HY-P0128) and improve cognitive dysfunction caused by Scopolamine (HY-N0296).

AChE/BChE/MAO-A-IN-2 is an AChE, BChE, and MAO-A inhibitor with IC₅₀ values of 104.28 nM, 23.04 nM, and 215.50 nM, respectively. AChE/BChE/MAO-A-IN-2 exhibits selective antiproliferative activity against cancer cells and low toxicity toward normal cells. AChE/BChE/MAO-A-IN-2 can be used for the research of alzheimer's disease, neuroblastoma.

BuChE-IN-11 (Compound 3b-1) is an selective BuChE inhibitor with an IC₅₀ of 0.44 μM for hBuChE. BuChE-IN-11 has high blood-brain barrier permeability and exhibits strong antioxidant activity due to its free radical scavenging properties. BuChE-IN-11 interacts with the choline binding site, acetyl binding site, and peripheral anionic site, exhibiting submicromolar BuChE inhibitory activity and preventing β-amyloid (Aβ) self-aggregation. BuChE-IN-11 holds promise for research in the field of Alzheimer's disease.

AChE-IN-104 (compound 3e) is a potent acetylcholinesterase (AChE) inhibitor with an IC₅₀ of 8.01 µM. AChE-IN-104 also inhibits BChE and MAO-A with IC₅₀s of 65.41 µM and 1.51 µM, respectively. AChE-IN-104 can be used for Alzheimer’s disease (AD) research.

BChE-IN-28 (compound 6J) is a selective butyrylcholinesterase (BChE) inhibitor with an IC₅₀ of 8 nM and a K_i of 12.16 nM. BChE-IN-28 shows the lower inhibition against AChE, MAO-A and MAO-B.

AChE/BChE-IN-28 (Compound 5q) is a BChE inhibitor with an IC₅₀ of 13.49 μM. AChE/BChE-IN-28 also exerts moderate inhibitory effect on AChE, with an IC₅₀ of 35.23 μM. AChE/BChE-IN-28 can be used in the research of Alzheimer's disease.

NSC 620023 TFA is a highly selective butyrylcholinesterase (BChE) inhibitor with an IC₅₀ of 32 nM. NSC 620023 TFA acts via π-stacking interactions with dual benzimidazole moieties and hydrophobic interactions within the BChE binding site. NSC 620023 TFA can be used for the research of alzheimer’s disease.

AChE/BChE-IN-32 (Compound 4a) is an AChE and BChE inhibitor, with K_i values of 2.48 and 0.696 μM respectively. AChE/BChE-IN-32 inhibits Aβ aggregation and exhibits a strong ABTS•+ scavenging ability (TEAC = 2.40). AChE/BChE-IN-32 shows significant neuroprotective activity in glutamate and hydrogen peroxide-induced oxidative stress models. AChE/BChE-IN-32 can be used for the study of Alzheimer's disease.

AChE/BChE-IN-35, Tacrine (HY-111338) derivative, is a brain-penetrant dual AChE/BChE inhibitor with an Electric Eel AChE IC₅₀ of 123.66 nM, human AChE IC₅₀ of 122.34 nM, and equine BChE IC₅₀ of 488.00 nM. AChE/BChE-IN-35 undergoes LAT1-mediated active transport across cell membranes. AChE/BChE-IN-35 exhibits enhanced brain exposure with slower brain tissue elimination. AChE/BChE-IN-35 can be used for the research of alzheimer's disease.

BChE/MAO-B-IN-1 (compound 7) is a dual BChE/MAO-B inhibitor with IC₅₀ values ​​of 375 nM and 20 nM, respectively. BChE/MAO-B-IN-1 protects against oxidative damage induced by H₂O₂ and 6-OHDA in SH-SY5Y cells. BChE/MAO-B-IN-1 can penetrate the central nervous system in a cell model that mimics the blood-brain barrier. BChE/MAO-B-IN-1 can be used in the study of neurological diseases such as Alzheimer's disease (AD).

AChE-IN-82 (compound 49) is an acetylcholinesterase (AChE) inhibitor. AChE-IN-82 inhibits eeAChE, eqBChE, hMAO-A, hMAO-B, and BACE-1 with IC₅₀s of 0.072, 9.81, 14.52, 0.024, 2.42 μM, respectively. AChE-IN-82 inhibits COX-1, COX-2 and 5-LOX with IC₅₀s of 60.41, 0.187, 0.18 μM, respectively. AChE-IN-82 shows an excellent neuroprotective effect by significantly reducing oxidative stress induced by H₂ O₂.

AChE-IN-68 (compound 2l) is a potent and selective AChE inhibitor, with an IC₅₀ value of 0.040 μM. AChE-IN-68 has high blood-brain barrier permeability. AChE-IN-68 can be used for the research of neurodegenerative disorders, particularly Alzheimer’s disease.

Cymserine is a blood-brain barrier-permeable butyrylcholinesterase (BuChE) inhibitor with an IC₅₀ value of 56.43 nM and a K_i of 38 nM. Cymserine binds to the catalytic domain of BuChE in a concentration-dependent manner to form a stable carbamylated enzyme complex, and exhibits BuChE selectivity over acetylcholinesterase due to its structural compatibility with the larger acyl-binding pocket of BuChE. Cymserine can be used in the research of Alzheimer's disease.

AChE/BChE-IN-19 (Compound 12) is a nicotinic hydrazide derivative. AChE/BChE-IN-19 is a inhibitor of AChE (IC₅₀ = 21.45 nM) and BChE (IC₅₀ =18.42 nM). AChE/BChE-IN-19 can be used in Alzheimer's disease research.

Isograndifoliol is a selective inhibitor of butyrylcholinesterase (BChE) with an IC₅₀ value of 0.9 μM. And Isograndifoliol moderately inhibits acetylcholinesterase (AChE) with an IC₅₀ value of 342.9 μM. Isograndifoliol also has vasorelaxant effect and anti-tumor effect. Isograndifoliol can be used for research against dementia caused by neurodegenerative diseases.