AChE/GSK-3β-IN-1 

AChE/GSK-3β-IN-1 (compound GT15) is a potent, dual AChE/GSK-3β inhibitor with IC₅₀ values of 1.2, 149.8 and 22.4 nM for hAChE , hBChE and hGSK-3β, respectively. AChE/GSK-3β-IN-1 penetrates the blood-brain barrier (BBB). AChE/GSK-3β-IN-1 has high kinase selectivity profiles for the CMGC kinase family. AChE/GSK-3β-IN-1 occupies the ATP binding site of DYRK1A. AChE/GSK-3β-IN-1 inhibits ROS expression and reduces oxidative stress. AChE/GSK-3β-IN-1 can be used for Alzheimer’s disease research^[1].

AChE/GSK-3β-IN-1 (compound GT15) (300 nM) has strong binding affinities with GSK3 family and exhibits a potent inhibitory activity against dual tyrosine phospho-regulated kinase 1 (DYRK1) (DYRK1α and DYRK1β with IC₅₀ of 28.3 nM and 119.7 nM, respectively)^[1].
AChE/GSK-3β-IN-1 (compound GT15) (5-15 µM; 1 hours; N2a-tau cells) exhibits good permeability across the blood-brain-barrier and ability to inhibit the phosphorylation of tau protein^[1].
AChE/GSK-3β-IN-1 (compound GT15) (5 µM; BV2 cells) prevents the increase of ROS caused by LPS and reduces oxidative stress^[1].

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

AChE/GSK-3β-IN-1 (compound GT15) (15 mg/kg,; p.o.; ICR male mice) has a function of improving memory and cognition in mice^[1].

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

585.72

C₃₁H₃₅N₇O₃S

2412364-73-7

CNC(C(S1)=C(N=C1C2=CC(NC(CNCCNC3=C4CCCCC4=NC5=CC=CC=C35)=O)=NC=C2)OCC6CC6)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Jiang X, et, al. Rational design and biological evaluation of a new class of thiazolopyridyl tetrahydroacridines as cholinesterase and GSK-3 dual inhibitors for Alzheimer's disease. Eur J Med Chem. 2020 Dec 1;207:112751.  [Content Brief]