AChE/GSK-3β-IN-1_product_DataBase

Bioactivity	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].
Invitro	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]. Western Blot Analysis[1] Cell Line:
In Vivo	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]. Animal Model:
Name	AChE/GSK-3β-IN-1
CAS	2412364-73-7
Formula	C31H35N7O3S
Molar Mass	585.72
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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.

PeptideDB

AChE/GSK-3β-IN-1

CAS: 2412364-73-7 F: C31H35N7O3S W: 585.72