Shopping Cart
- Remove All
![TargetMol](https://www.targetmol.com/storage/error/oops.webp)
Your shopping cart is currently empty
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $350 | In Stock | |
5 mg | $970 | In Stock | |
10 mg | $1,200 | In Stock | |
25 mg | $1,590 | In Stock | |
50 mg | $1,980 | In Stock | |
100 mg | $2,500 | In Stock | |
500 mg | $3,930 | In Stock |
Description | GSK-3 inhibitor 4 is an orally active and brain-permeable compound that acts as a triple inhibitor of GSK-3, CDK2, and CDK5, with IC50 values of 0.56 nM (GSK-3β), 0.45 nM (GSK-3α), 0.47 μM (CDK2), and 0.68 μM (CDK5). It effectively reduces Tau protein levels and can be used in the study of Alzheimer's disease. |
Targets&IC50 | CDK2:0.47 μM, CDK5:0.68 μM, GSK-3α:0.45 nM, GSK-3β:0.56 nM |
In vitro | GSK-3 inhibitor 4 (compound 40) demonstrates excellent selectivity and efficacy against CDK2 (840-fold, IC50 = 0.47 μM), CDK5 (1200-fold, IC50 = 0.68 μM), GSK-3β (IC50 = 0.56 nM), and GSK-3α (IC50 = 0.45 nM). It also exhibits good permeability and a high capacity for binding to plasma proteins and brain tissue due to its lipophilicity.[1] |
In vivo | GSK-3 inhibitor 4 (10 mg/kg; p.o.) reduced pTau396 by 37% when administered orally as a nanosuspension. GSK-3 inhibitor 4 (2 mg/kg, i.v.; 10 mg/kg, p.o.) exhibits low to moderate clearance (15.8 to 23.3 mL/min/kg) and is well absorbed orally in solution.[1] |
Molecular Weight | 403.38 |
Formula | C22H15F2N5O |
Cas No. | 2227279-83-4 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 50 mg/mL (123.95 mM) ![]() | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
|
Copyright © 2015-2024 TargetMol Chemicals Inc. All Rights Reserved.