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GSK-3 inhibitor 4

Names

[ CAS No. ]:
2227279-83-4

[ Name ]:
GSK-3 inhibitor 4

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> Stem Cell/Wnt >> GSK-3
Signaling Pathways >> Cell Cycle/DNA Damage >> CDK
Research Areas >> Neurological Disease
Signaling Pathways >> PI3K/Akt/mTOR >> GSK-3

[Target]

GSK-3α:0.45 nM (IC50)

GSK-3β:0.56 nM (IC50)

CDK2:0.47 μM (IC50)

CDK5:0.68 μM (IC50)


[References]

[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.  

Chemical & Physical Properties

[ Molecular Formula ]:
C22H15F2N5O

[ Molecular Weight ]:
403.38

Related Compounds