gsk-3α

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.

GSK-3 inhibitor 3 is a selective, orally active, brain-permeable GSK-3 inhibitor that inhibits GSK-3α and GSK-3β with IC50s of 0.35 nM and 0.25 nM, respectively.GSK-3 inhibitor 3 reduces the phosphorylation level of tau protein S396 with an IC50 of 10 nM in a triple transgenic mouse model of Alzheimer's disease. GSK-3 inhibitor 3 reduced the phosphorylation level of tau protein S396 in a triple transgenic mouse model of Alzheimer's disease, with an IC50 of 10 nM.GSK-3 inhibitor 3 can be used for the study of neurological diseases.

GSK-3 inhibitor 1 is a GSK-3 inhibitor.

GSK-3β inhibitor 8 (GSK3β Inhibitor XVIII) is a potent and selective GSK-3β inhibitor with an IC50 value of 64 nM.GSK-3β inhibitor 8 is a thienopyrimidine derivative that negatively regulates the Wnt signaling pathway and stimulates β-cell proliferation.

GSK-3 Inhibitor XIII, an ATP-competitive GSK-3 inhibitor (Ki: 24 nM), can be used to study diabetes and obesity.

GSK-3 Inhibitor 5 (4-Cyanophenacyl bromide) is a ketone derivative that is used as an intermediate in pharmaceuticals and organic synthesis, and inhibits glycogen synthase kinase 3 (GSK-3).

GSK-3β inhibitor 14 (1,5-Benzothiazepin-4(5H)-one, 2,3-dihydro-2-methyl-5-(phenylmethyl)-) is a weak GSK-3β inhibitor, IC50﹥ 100μM.

(E/Z)-GSK-3β inhibitor 1 is a glycogen synthase kinase 3β (GSK-3β) inhibitor demonstrating high antidiabetic efficacy.

GSK-3β inhibitor 10 has skin-whitening, anti-oxidizing and PPAR activities.

GSK-3β inhibitor23 (Compound 11726169) is an inhibitor of glycogen synthase kinase 3 (GSK-3), effectively inhibiting GSK-3β and GSK-3α with IC50 values of 12.1 nM and 18.8 nM, respectively. It demonstrates antiviral activity against HIV1 and exhibits good metabolic stability in mouse and human liver microsomes and plasma, although it has poor permeability in Caco-2 cells, indicating potentially low oral bioavailability.

GSK-3β inhibitor 1 is an inhibitor of GSK-3β( IC50 of 4.9 nM) and demonstrates high antidiabetic efficacy.

GSK-3β inhibitor 2 (5-Thiazolecarboxamide,2-[2-[(cyclopropylcarbonyl)amino]-4-pyridinyl]-4-methoxy-) is a BBB-crossing and selective inhibitor of GSK-3β (IC50 = 1.1 nM). GSK-3β inhibitor 2 can be used in studies about Alzheimer's disease.

GSK-3β inhibitor20 (compound 3A) is an effective inhibitor of GSK-3β, exhibiting an IC50 value of 74.4 nM.

GSK-3β inhibitor22 (compound 20o) is a GSK-3β inhibitor with an IC50 of 3.1 nM, showing potential for Alzheimer's disease research.

hAChE/hBuChE/GSK-3β-IN-1 (Compound 6c) is a multi-target compound designed for Alzheimer's treatment capable of crossing the blood-brain barrier. It inhibits hAChE with an IC50 of 28.88 nM, hBuChE with an IC50 of 131.90 nM, and GSK-3β with an IC50 of 51.42 nM. Additionally, it acts as an inhibitor of tau protein and Aβ protein aggregation.

GSK-3β inhibitor24 (Compound 41) is a potent GSK-3β inhibitor with an IC50 of 0.22 nM. It increases GSK-3β phosphorylation at the Ser9 site in a dose-dependent manner and inhibits tau protein hyperphosphorylation by reducing the abundance of p-tau-Ser396. The compound upregulates β-catenin and neurogenesis-related markers (GAP43 and MAP-2), demonstrating significant anti-Alzheimer's disease (AD) activity.

GSK-3β inhibitor25 (Compound 6h) exhibits weak inhibitory activity against GSK-3β with an IC50 greater than 100 μM.

GSK-3β inhibitor26 (Compound D14) is a GSK-3β inhibitor with an IC50 of 18.23 μM. This compound is applicable in research related to cancer, inflammation, and neurodegenerative diseases.

GSK-3β inhibitor 28 is a selective, non-competitive inhibitor of glycogen synthase kinase-3β (GSK-3β), with an IC50 value of 14.82 nM. It enhances the expression of phosphorylated GSK-3β while reducing the levels of p-NF-κB, P65, C-myc, and Cyclin D1. This compound induces apoptosis, causes G1 phase arrest, and inhibits cell migration. GSK-3β inhibitor 28 is applicable for cancer research, including studies on colorectal cancer.

ChE/GSK-3β-IN-1 (compound 18o) is a potent dual inhibitor of ChE/GSK-3β. It effectively inhibits acetylcholinesterase (AChE) with an IC50 of 1.7 μM, butyrylcholinesterase (BChE) with an IC50 of 5.3 μM, and GSK-3β with an IC50 of 5.7 μM. Additionally, ChE/GSK-3β-IN-1 prevents the self-aggregation of Aβ1-42 and is applicable in Alzheimer's disease (AD) research.

GSK-3β/G9a-IN-1 (Compound T2) is an orally active, selective inhibitor that penetrates the blood-brain barrier, targeting G9a (substrate-competitive, IC50: 1.1 μM) and GSK-3β (ATP-competitive, IC50: 0.8 μM). It acts as a potent H3K9me2 inhibitor, facilitating chromatin remodeling and reducing tau protein phosphorylation and Aβ aggregation. Additionally, GSK-3β/G9a-IN-1 inhibits the glucocorticoid receptor, androgen receptor, and alpha-2A adrenergic receptor, and upregulates SAGA complex members such as Eny2 and Sgf29. This compound significantly enhances memory, restores social behavior, and increases synaptic complexity in late-onset Alzheimer's disease.

GSK-3β inhibitor 3 is a potent, selective, and irreversible covalent inhibitor of glycogen synthase kinase 3β (GSK-3β) with an IC50 of 6.6 μM, and can be used to study acute promyelocytic leukemia.

GSK-3/CDK5/CDK2-IN-1 is an imidazole derivative compound that inhibits cdk5, cdk2, and GSK-3.it has demonstrated applications in cancer research and the study of neurodegenerative diseases [1].

GSK-3β inhibitor 12 is a selective GSK-3β inhibitor.GSK-3β inhibitor 12 inhibits 49.11% of 25 μM GSK-3β activity and 37.11% of 50 μM GSK-3β activity.GSK-3β inhibitor 12 can be used for the study of Parkinson's in the presence of lipopolysaccharide induction.