BChE Inhibitor

Ebeiedinone, a steroidal alkaloid from Fritillaria species, inhibits the bioactivity of human whole blood cholinesterase (ChE) at the concentration of 0.1 mM, with the inhibitory effects of 69.0%.

BChE-IN-17 (compound 6n) is a potent and selective BChE inhibitor with IC₅₀s of 10.5 nM and 32.5 nM for eqBChE and hBChE, respectively. BChE-IN-17 shows over 1000-fold selectivity to BChE against AChE. BChE-IN-17 shows low neurotoxicity and moderate neuroprotective effects.

Sophoflavescenol is a prenylated flavonol, which shows great inhibitory activity with IC₅₀ of 0.013 μM against Phosphodiesterase 5 (PDE5), and also inhibits RLAR, HRAR, AGE, BACE1, AChE and BChE with IC₅₀s of 0.30 μM, 0.17 μM, 17.89 μg/mL, 10.98 μM, 8.37 μM and 8.21 μM, respectively.

ASS234 is a potent monoamino oxidase (MAO) inhibitor with IC₅₀s of 5.2 nM and 43 nM for MAO-A and MAO-B, respectively. ASS234 also inhibits AChE and BuChE with IC₅₀s of 350 nM and 460 nM, respectively.

Kuwanon U is a potent cholinesterase inhibitor with IC₅₀s of 19.69, 10.11 µM and K_is of 6.48, 9.59 µM for acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), respectively. Kuwanon U has the potential for the research of Alzheimer’s disease (AD).

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.

Epiberberine is an alkaloid isolated from Coptis chinensis, acts as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor, with IC₅₀s of 1.07, 6.03 and 8.55 μM, respectively. Epiberberine has antioxidant activity, with peroxynitrite ONOO^- scavenging effect (IC₅₀, 16.83 μM), and can be used for the research of Alzheimer disease. Epiberberine inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways. Epiberberinecan be used for the research of diabetic disease.

Benactyzine hydrochloride is a competitive BChE inhibitor with a K_i of 0.01 mM. Benactyzine hydrochloride is an anticholinergic drug. Benactyzine hydrochloride has the potential for organophosphate poisoning research.

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.

SD-6 is an orally active inhibitor of hAChE and hBChE with IC₅₀ values of 0.907 µM and 1.579 µM, respectively. SD-6 has excellent blood-brain barrier (BBB) permeability and no neurotoxicity, which can be used for research on Alzheimer's disease.

BChE-IN-11 (compound 10) is a potent, selective and non-competitive BChE (butyrylcholinesterase) inhibitor, with an IC₅₀ of 2.1 μM. BChE-IN-11 can be used for Alzheimer's disease (AD) research.

AChE/BChE-IN-10 (Compound 7b) is a potent dual AChE and BChE inhibitor with IC₅₀ values of 0.176, and 0.47 μM, respectively. AChE/BChE-IN-10 shows good blood brain barrier permeability. AChE/BChE-IN-10 can inhibit Aβ-aggregation and be used in Alzheimer’s disease (AD) research.

Dibutyl phenyl phosphate is a flame retardant. Dibutyl phenyl phosphate is a BChE inhibitor (IC₅₀: 83.6 μM; K_i: 94.5 μM).

Lucidadiol is a natural compound isolated from Ganoderma lucidum. Lucidadiol exhibits acetylcholinesterase-inhibitory activity, with IC₅₀ values of 31 μM. Lucidadiol shows antiviral activity against influenza virus type A and HSV type 1.

Z32439948 is a butyrylcholinesterase (BChE) inhibitor (IC₅₀: 1.4 μM, hBChE) and is a derivative of m-sulfamoylbenzamide. Z32439948 also exhibited neuroprotective effects against glutamate in SH-SY5Y cells.

ZLMT-12 (compound 35), tacrine derivatives, is a potent, orally active CDK2/9 inhibitor with IC₅₀ values of 0.002 and 0.011 μM for CDK9 and CDK2, respectively. ZLMT-12 has a weak inhibitory effect on AChE (IC₅₀=19.023 μM) and BChE (IC₅₀=2.768 μM). ZLMT-12 has low toxicity and antiproliferative activity. ZLMT-12 induces apoptosis and arrests the cell cycle in the S phase and G2/M phase.

AChE-IN-72 (Compound 13a) is an inhibitor for acetylcholinesterase (AChE) with an IC₅₀ of 0.59 μM. AChE-IN-72 inhibits BChE with an IC₅₀ of 5.02 μM. AChE-IN-72 exhibits radical scavenging with IC₅₀ of 5.88 μM. AChE-IN-72 exhibits iron-chelating property, inhibits Aβ1−42 aggregation, and inhibits NLRP3 inflammasome activation. AChE-IN-72 ameliorates memory impairment in Betaine (HY-B0710)-induced AD mouse model. AChE-IN-72 is blood-brain barrier (BBB) penetrable.

hAChE-IN-6 (compound 51) is a brain penetrant AChE inhibitor with an IC₅₀ of 0.16 μM. hAChE-IN-6 also inhibits hBuChE and GSK3β with IC₅₀ values of 0.69 μM and 0.26 μM, respectively. hAChE-IN-6 inhibits tau protein and Aβ1-42 self-aggregation, and can be used for Alzheimer's disease (AD) research.

SB-1436 is an Cholinesterase (ChE) inhibitor, inhibits acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and recombinant human acetylcholinesterase (rHuAChE) with IC₅₀s of 0.176, 0.37 and 0.08 μM, respectively. SB-1436 inhibits AChE and BChE in a non-competitive manner with K_is of 0.046 and 0.115 μM, respectively. SB-1436 significantly stops the self-aggregation of Aβ, and can be used for neurological disease research.

BChE/hCA II-IN-1 (Compound 20) is a dual-functional inhibitor of Butyrylcholinesterase (BChE) and human carbonic anhydrase II (hCA II) with IC₅₀s of 76.50 and 10.69  μM for BChE and hCA II, respectively. BChE/hCA II-IN-1 can be used for neurodegenerative diseases like Alzheimer's and glaucoma research.