2412364-73-7
2412364-73-7 structure
- Name: AChE/GSK-3β-IN-1
- Chemical Name: AChE/GSK-3β-IN-1
- CAS Number: 2412364-73-7
- Molecular Formula: C31H35N7O3S
- Molecular Weight: 585.72
- Catalog: Signaling Pathways Cell Cycle/DNA Damage Microtubule/Tubulin
- Create Date: 2022-09-06 00:17:01
- Modify Date: 2024-04-08 22:35:58
-
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].
| Name | AChE/GSK-3β-IN-1 |
|---|
| Description | 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]. |
|---|---|
| Related Catalog | |
| In Vitro | 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: N2a-tau cells Concentration: 5, 10, and 15 µM Incubation Time: 6 hours Result: Decreased the level of phosphorylated tau protein was reduced to 49% at 5 µM and 17% at 15 µM. |
| 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: ICR male mice[1] Dosage: 15 mg/kg Administration: Oral administration Result: Improved the cognitive impairment of the mice. |
| References |
| Molecular Formula | C31H35N7O3S |
|---|---|
| Molecular Weight | 585.72 |