AChE Inhibitor

eeAChE-IN-2 is a potent eeAChE inhibitor with an IC₅₀ value of 2 nM.

AChE/BChE-IN-16 (compound C7) is a potent cholinesterase (ChE) inhibitor with IC₅₀s of 30 nM and 48 nM for human acetylcholinesterase (hAChE) and human butyrylcholinesterase (hBChE), respectively. AChE/BChE-IN-16 exhibits a remarkable capacity to safeguard PC12 cells against H₂O₂-induced apoptosis and effectively suppresses the production of reactive oxygen species (ROS).

Anti-Candida auris β-1,3-glucans Antibody (2G8) is an antibody targeting Candida auris β-1,3-glucans, and also acts as an inhibitor of AChE and TGF-β receptor 2. Anti-Candida auris β-1,3-glucans Antibody (2G8) also targets fungal cell wall components, effectively inhibits fungal growth and interferes with capsule formation, thereby significantly reducing the fungal load in mouse tissues. Anti-Candida auris β-1,3-glucans Antibody (2G8) not only blocks TGF-β receptor binding to inhibit the Smad signaling pathway, reduces fibroblast activation and collagen deposition, but also induces epithelial differentiation of tumor cells and reduces pancreatic tumor metastasis. Anti-Candida auris β-1,3-glucans Antibody (2G8) specifically binds to the conserved N-linked glycoepitope on AChE to inhibit its activity without interfering with BChE, and can be used in studies of cryptococcosis and related tumor mechanisms.The isotype control is Human IgG1 kappa, Isotype Control (HY-P99001).

AChE-IN-116 is a selective acetylcholinesterase (AChE) inhibitor with an electric eel AChE IC₅₀ of 1.60 μM and K_i of 1.72 μM. AChE-IN-116 exhibits weak ability to scavenge DPPH radical. AChE-IN-116 can be used for the research of Alzheimer's disease.

hAChE/Aβ1-42-IN-1 (Compound 16) is a potent inhibitor of hAChE and Aβ1-42 aggregation. hAChE/Aβ1-42-IN-1 shows acceptable relative safety upon hepG2 cell line and excellent BBB penetration with wide safety margin. hAChE/Aβ1-42-IN-1 has the potential for the research of Alzheimer disease (AD).

Protriptyline is a potent tricyclic antidepressant (TCA). Protriptyline inhibits AChE activity with an IC₅₀ value of 0.06 mM and inhibits Aβ self-assembly. Protriptyline can be used for the study of depression and Alzheimers disease.

AChE/hCA I-IN-1 (Compound L3) is the inhibitor for acetylcholinesterase (AChE) and carbonic anhydrase (CA), that inhibits AChE, hCA I and hCA II with IC₅₀ of 302, 265 and 283 nM, respectively.

MAO-B-IN-7 is a potent and blood-brain barrier permeable MAO-B and AChE inhibitor with IC₅₀s of 41 nM, 87 nM and 0.3 μM for human AChE, electric eel AChE and MAO-B, respectively. MAO-B-IN-7 can effectively alleviate oxidative stress and neuroinflammatory damage.

Zifrosilone is an orally active acetylcholinesterase (AChE) inhibitor with a mean maximum inhibition of 20.9% at 10 mg. Zifrosilone can be used for the research of neurological disease.

AChE/Aβ-IN-3 (compound AM5) is a dual inhibitor of AChE and Amyloid-β aggregation with IC_50<.sub> values of 1.29 and 4.93 μM, respectively. AChE/Aβ-IN-3 has antioxidant properties that scavenge ROS and restore their normal levels. AChE/Aβ-IN-3 can be used in the study of neurological diseases, such as Alzheimer's disease.

K027 is a potent reactivator of Organophosphates (OP)-inhibited acetylcholinesterase (AChE). K027 can be used for the research of Alzheimer's disease.

hAChE/hBuChE/GSK-3β-IN-1 (Compound 6c) is a BBB-penetrable and multi-target anti-Alzheimer's disease compound. hAChE/hBuChE/GSK-3β-IN-1 is the inhibitors of hAChE (IC₅₀: 28.88 nM), hBuChE (IC₅₀: 131.90 nM) and GSK-3β (IC₅₀: 51.42 nM). hAChE/hBuChE/GSK-3β-IN-1 is the tau and Aβ protein aggregation inhibitors.

Dyclonine-d₉ hydrochloride (Dyclocaine-d₉ hydrochloride) is the deuterated-labeled Dyclonine hydrochloride (HY-B0364A). Dyclonine hydrochloride (Dyclocaine hydrochloride) is an orally active, blood-brain barrier-permeable piperidine phenylacetone small molecule commonly used as a local anesthetic. Dyclonine hydrochloride acts as a highly selective allosteric antagonist of TRPV3; it also reversibly inhibits G9a, ALDH2 and ALDH3A1, non-competitively blocks AChE. Dyclonine hydrochloride activates the Nrf2/ARE pathway, relieves the epigenetic silencing of FXN, blocks Aβ42 aggregation, and promotes remyelination and reparative polarization of microglia. Dyclonine hydrochloride 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 hydrochloride can be used for research on multiple diseases including neurodegenerative diseases, cancer and pruritic dermatitis.

AChE/BChE/MAO-B-IN-2 is a potent AChE, BChE, and MAO-B enzymes inhibitor with IC₅₀ values of 48.2 nM, 83.9 nM, and 31.2 nM, respectively. AChE/BChE/MAO-B-IN-2 has significant antioxidant activity, and can be used for Parkinson’s disease research.

Bis-(-)-8-demethylmaritidine, a natural alkaloid, is a potent acetylcholinesterase (AChE) inhibitor. Bis-(-)-8-demethylmaritidine can be used for Alzheimer's disease research.

Carbonic anhydrase/AChE-IN-1 (compound 16) is a carbonic anhydrase and AChE inhibitor with K_is of 24.42 nM, 19.95 nM, and 5.07 nM for hCA I, hCA II, and AChE, respectively.

5α-Epoxyalantolactone is an orally active, blood-brain barrier-permeable ANXA2 inhibitor. 5α-Epoxyalantolactone binds to ANXA2, blocks the formation of ANXA2-S100A10 heterotetramers, inhibits the membrane trafficking of E-cadherin, and prevents metastasis of breast cancer cells as well as proliferation of breast cancer stem cells. 5α-Epoxyalantolactone improves cognitive and memory impairments by inhibiting the iNOS/COX-2/NF-κB pathway and reducing the activity of cerebral AChE. 5α-Epoxyalantolactone can be used in studies related to Alzheimer's disease and triple-negative breast cancer.

Toddacoumaquinone is a coumarin-naphthoquinone dimer found in the roots of Toddalia asiatica. Toddacoumaquinone inhibits acetylcholinesterase (AChE) and β-amyloid (Aβ_1-42) aggregation, with an IC₅₀ of 46 μM against electric eel acetylcholinesterase. Toddacoumaquinone exerts antiviral effects against herpes simplex virus type 1 and herpes simplex virus type 2 (HSV). Toddacoumaquinone is used in research related to Alzheimer's disease and herpesvirus infections.

PJ17 is a potent dual-target inhibitor of AChE and GSK-3β, with IC₅₀ values of 8.84 μM and 4.19 μM, respectively. PJ17 shows no significant neurotoxic effect in primary cerebellar granule neuron cultures. PJ17 serves as a template for the design of multitarget drugs. PJ17 can be used for the research of Alzheimer's disease.

AChE-IN-106 is an AChE inhibitor. AChE-IN-106 shows no obvious cytotoxicity at low concentrations. AChE-IN-106 can be used for the research of Alzheimer's disease.