2. Neuronal Signaling Immunology/Inflammation NF-κB Metabolic Enzyme/Protease
  3. Cholinesterase (ChE) Amyloid-β Tau Protein NOD-like Receptor (NLR) Reactive Oxygen Species Mitochondrial Metabolism
  4. AChE/BChE-IN-23

AChE/BChE-IN-23 (Compound 6e) is an AChE/BChE inhibitor (IC50: 0.91 μM, 1.19 μM and 1.01 μM for hAChE, eq BChE and hBChE, respectively). AChE/BChE-IN-23 has antioxidant activity and inhibits Aβ1-42 and Tau protein aggregation. AChE/BChE-IN-23 also inhibits microglial activation by reducing ROS release and mitochondrial injury. AChE/BChE-IN-23 suppresses NLRP3 inflammasome and pro-inflammatory cytokines in human microglial cells. AChE/BChE-IN-23 also reverses the Scopolamine (HY-N0296)-induced memory impairment in mice model.

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AChE/BChE-IN-23 Chemical Structure

AChE/BChE-IN-23 Chemical Structure

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AChE/BChE-IN-23 Related Antibodies

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Description

AChE/BChE-IN-23 (Compound 6e) is an AChE/BChE inhibitor (IC50: 0.91 μM, 1.19 μM and 1.01 μM for hAChE, eq BChE and hBChE, respectively). AChE/BChE-IN-23 has antioxidant activity and inhibits Aβ1-42 and Tau protein aggregation. AChE/BChE-IN-23 also inhibits microglial activation by reducing ROS release and mitochondrial injury. AChE/BChE-IN-23 suppresses NLRP3 inflammasome and pro-inflammatory cytokines in human microglial cells. AChE/BChE-IN-23 also reverses the Scopolamine (HY-N0296)-induced memory impairment in mice model[1].

IC50 & Target[1]

hAChE

0.91 μM (IC50)

eqBCHE

1.19 μM (IC50)

NLRP3

 

hBCHE

1.02 μM (IC50)

In Vitro

AChE/BChE-IN-23 (5-50 μM) causes propidium iodide (has a binding affinity for AChE enzyme) displacement from AChE (5 μM, 2.06%; 10 μM, 11.78%; 20 μM, 14.47%; 50 μM, 27.53%)[1].
AChE/BChE-IN-23 has antioxidant properties (20 μM; radical scavenging of DPPH: 47.30%, IC50:15.17 μM)[1].
AChE/BChE-IN-23 (3.125 μM, 72 h) effectively inhibits Aβ1-42 (12.5 μM) aggregation[1].
AChE/BChE-IN-23 (1.125 μM, 72 h) effectively inhibits Tau (5 μM) aggregation[1].
AChE/BChE-IN-23 (1-20 μM, 24 h) has no cytotoxicity effect on PC-12 cells[1]..
AChE/BChE-IN-23 (12.5 μM, 24 h) inhibits the activation of microglia by reducing the release of ROS and restoring the mitochondrial membrane potential[1].
AChE/BChE-IN-23 (12.5 μM, 24 h) has anti-inflammatory effect by inhibiting NLRP3 inflammasome and NF-κB expression levels in microglial cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

AChE/BChE-IN-23 Related Antibodies

Western Blot Analysis[1]

Cell Line: HMC-3 cells
Concentration: 12.5 μM
Incubation Time: 24 h
Result: Suppressed NLRP3, caspase-1, IL-1β and IL-18 expression.

Immunofluorescence[1]

Cell Line: HMC-3 cells
Concentration: 12.5 μM
Incubation Time: 24 h
Result: Reduced mitochondrial ROS and stabilizes the mitochondrial membrane potential.
In Vivo

AChE/BChE-IN-23 (10 mg/kg, i.p., 14 days) reverses the Scopolamine(HY-N0296)-induced amnesia by enhancing spatial and cognitive memory in the AD mice[1].
AChE/BChE-IN-23 (2000 mg/kg, p.o., 14 days) has no toxicological effect on Swiss albino mice including no increase in overweight, abnormal behavior, convulsions, tremors, or diarrhea associated with acute toxicity[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Scopolamine (1 mg/kg) induced Alzheimer’s disease (AD) model; 6-week-old Swiss albino mice[1]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection (i.p.), 14 days
Result: Decreased escape latency, distance traveled in Morris Water Maze (MWM) experiment.
Increased latency period in passive avoidance.
Increased BDNF and Nr4a2 in brain.
Molecular Weight

367.40

Formula

C19H21N5O3
SMILES

N/C(C1=CC=CC(NC(NCCC2=CNC3=C2C=C(OC)C=C3)=O)=C1)=N\O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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AChE/BChE-IN-23 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AChE/BChE-IN-23Cholinesterase (ChE)Amyloid-βTau ProteinNOD-like Receptor (NLR)Reactive Oxygen SpeciesMitochondrial Metabolismβ-amyloid peptideAβAbetaAlzheimer's diseaseAntioxidant activityNeuroprotectionMicroglialNLRP3HMC-3 cellsInhibitorinhibitorinhibit

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