GSK-3 inhibitor 4 

GSK-3 inhibitor 4 is an orally active and brain-penetrant inhibitor of GSK-3, CDK2, and CDK5, with IC₅₀ values of 0.56 nM (GSK-3β), 0.45 nM (GSK-3α), 0.47 μM, and 0.68 μM, respectively. GSK-3 inhibitor 4 effectively reduces the phosphorylation level of Tau protein. GSK-3 inhibitor 4 can be used in Alzheimer's disease (AD) studies^[1].

GSK-3 inhibitor 4 (compound 40) exhibits excellent selectivity 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)^[1].
GSK-3 inhibitor 4 has good permeability and exhibits a high ability to bind to plasma proteins and brain tissue due to its lipophilic nature^[1].

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

GSK-3 inhibitor 4 (10 mg/kg, p.o.) produce a 37% reduction in pTau396, when administered orally as a nanosuspension at a dose of 10 mg/kg^[1].
GSK-3 inhibitor 4 (2 mg/kg, i.v.; 10 mg/kg, p.o.) exhibite low-moderate clearance ranging from 15.8 to 23.3 mL/min/kg and are well-absorbed when administered orally as a solution^[1].
Pharmacokinetic Parameters of GSK-3 Inhibitor 4 (compound 40) in Mice. ^[1]

小鼠体内 GSK-3 Inhibitor 4 (compound 40) 的药代动力学参数^[1]

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

403.38

C₂₂H₁₅F₂N₅O

2227279-83-4

O=C(C1=NC(NC2=CC=C(C=C2)F)=NC=C1)NC3=C(C4=CC=C(F)C=C4)C=CN=C3

Room temperature in continental US; may vary elsewhere.

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

• [1]. Hartz RA, et al. Discovery of 2-(Anilino)pyrimidine-4-carboxamides as Highly Potent, Selective, and Orally Active Glycogen Synthase Kinase-3 (GSK-3) Inhibitors. J Med Chem. 2023 Jun 8;66(11):7534-7552.  [Content Brief]