2. Neuronal Signaling Stem Cell/Wnt PI3K/Akt/mTOR
  3. Beta-secretase Cholinesterase (ChE) GSK-3
  4. AChE/BACE1/GSK3β-IN-1

AChE/BACE1/GSK3β-IN-1 is an orally active triple inhibitor of AChE/BACE1/GSK3β. AChE/BACE1/GSK3β-IN-1 has effective inhibitory activity against AChE, BACE1 and GSK3β with IC50 values of 1.0 μM, 20 μM and 15 μM, respectively. AChE/BACE1/GSK3β-IN-1 has good blood-brain barrier penetrability, suitable bioavailability. AChE/BACE1/GSK3β-IN-1 can be used for the research of Alzheimer's disease (AD).

For research use only. We do not sell to patients.

AChE/BACE1/GSK3β-IN-1 Chemical Structure

AChE/BACE1/GSK3β-IN-1 Chemical Structure

CAS No. : 2866066-81-9

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AChE/BACE1/GSK3β-IN-1 Related Antibodies

Top Publications Citing Use of Products

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BACE1 BACE2

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AChE BChE

View All GSK-3 Isoform Specific Products:

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GSK-3 GSK-3α GSK-3β

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Description

AChE/BACE1/GSK3β-IN-1 is an orally active triple inhibitor of AChE/BACE1/GSK3β. AChE/BACE1/GSK3β-IN-1 has effective inhibitory activity against AChE, BACE1 and GSK3β with IC50 values of 1.0 μM, 20 μM and 15 μM, respectively. AChE/BACE1/GSK3β-IN-1 has good blood-brain barrier penetrability, suitable bioavailability. AChE/BACE1/GSK3β-IN-1 can be used for the research of Alzheimer's disease (AD)[1].

IC50 & Target[1]

BACE1

20 μM (IC50)

AChE

1 μM (IC50)

GSK-3β

15 μM (IC50)

In Vitro

AChE/BACE1/GSK3β-IN-1 shows effective inhibition for AChE, BACE1 and GSK3β with IC50 values of 1.0 μM, 20 μM and 15 μM, respectively[1].
AChE/BACE1/GSK3β-IN-1 can pass through BBB[1].

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

AChE/BACE1/GSK3β-IN-1 Related Antibodies
In Vivo

AChE/BACE1/GSK3β-IN-1 (oral, 200 and 400 mg/kg, single) shows no acute toxicity and good safety profile in C57B6/J Mice[1].
AChE/BACE1/GSK3β-IN-1 (p.o., 100 mg/kg; i.v., 10 mg/kg)has good PK profiles[1].
AChE/BACE1/GSK3β-IN-1 (gavage, 2.5 mg/kg, 5 mg/kg and 10mg/kg, for 7 consecutive days) can ameliorate the impaired learning and memory in Aβ-induced AD mice[1].
AChE/BACE1/GSK3β-IN-1 inhibits the expression of ADAM17 in the cortex and significantly decreases the expressions of ADAM17 and BACE1 in AD mice[1].

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

Animal Model: C57B6/J Mice[1]
Dosage: 200 and 400 mg/kg
Administration: oral, single
Result: Increased slightly serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST), but no significant difference.
Showed no significant change in the content of blood urea nitrogen (BUN).
Did not change significantly the morphology of liver and kidney tissue of mice.
Animal Model: male Sprague-Dawley (SD) rats[1]
Dosage: 10 mg/kg and 100 mg/kg
Administration: oral and intravenous
Result:
parameters 100 mg/kg (p.o.) 10 mg/kg(i.v.)
Cmax(ng/mL) 167 ± 13 2796 ± 259
AUC0−t(ng/mL) 1010 ± 112 1031 ± 86
AUC0−∞(ng/mL*h) 1635 ± 362 1047 ± 88
t1/2 (h) 20 ± 9 0.4 ± 0.04
Cl (L/h/kg) 63 ± 12 10 ± 1
MRT0−∞(h) 26 ± 11 0.3 ± 0
VZ(L/kg) 1730 ± 387 5 ± 1
Tmax(h) 1 0.08
F (%) 9.8
Animal Model: Aβ-induced AD mice[1]
Dosage: 2.5 mg/kg, 5 mg/kg and 10mg/kg
Administration: gavage, for 7 consecutive days
Result: Decreased the escape latency of mice.
Increased the number of crossing platforms in mice in a dose-dependent trend.
Molecular Weight

450.50

Formula

C26H27FN2O4
CAS No.
SMILES

O=C1C=CC2=C(OCCCN3CCC(NCC4=CC(F)=CC=C4)CC3)C5=C(OC=C5)C=C2O1
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/BACE1/GSK3β-IN-1 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/BACE1/GSK3β-IN-12866066-81-9Beta-secretaseCholinesterase (ChE)GSK-3BACEβ-Secretase Glycogen synthase kinase-3Glycogen synthase kinase 3oralAChEBACE1GSK3βblood-brain barrierbioavailabilityAlzheimer's disease (AD)Inhibitorinhibitorinhibit

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