gsk3-in-1

GSK3-IN-1 is a GSK3B-glycogen synthase kinase-3 beta inhibitor.

CDKL5 GSK3-IN-1 (Compound 2) acts as a potent and selective chemical probe for CDKL5 and GSK3. It effectively inhibits CDKL5 and GSK3α β with IC50 values of 4.6 nM for CDKL5, 24 nM for GSK3β, and 9.5 nM for GSK3α in NanoBRET assays. This compound is useful in the study of central nervous system disorders.

GSK3-IN-4 is a GSK-3 inhibitor with IC50 of 0.101-1 μM of GSK-3α and GSK-3β in Calipe Assay.

GSK3-IN-2 is a potent GSK3 inhibitor for the treatment of diabetes and neurodegenerative diseases.

API-1 (NSC-177223) is a potent inhibitor of Akt. It induces GSK3-dependent, β-TrCP- and FBXW7-mediated Mcl-1 degradation, resulting in induction of apoptosis .

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].

SAR502250 is a potent, selective, ATP-competitive, orally active, and brain-penetrant GSK3 inhibitor with a human GSK-3β IC50 value of 12 nM, exhibiting antidepressant-like activity and being researched for potential application in Alzheimer's disease (AD) treatment.

Potent and selective CLK inhibitor (IC50 values are 28, 88 and 510 nM for CLK4, 1 and 2, respectively). Exhibits no significant activity at CLK3, DYRK, CDK or GSK3 at a concentration of 10 μM. Inhibits growth of a range of cancer cell lines in vitro at subnanomolar concentrations. Walter et al (2018) Molecular structures of cdc2-like kinases in complex with a new inhibitor chemotype. PLoS One 13 e0196761 PMID:29723265

6-Me-ATP (N6-Methyl-ATP), a N6-modified adenosine triphosphate (ATP) derivative, exhibits strong binding affinity for glycogen synthase kinase 3 (GSK3) and serves as the phosphate donor in GSK3β-catalyzed phosphorylation of its substrate peptide [1].

6-Me-ATP (N6-Methyl-ATP) trisodium, an N6-modified ATP derivative, exhibits high binding affinity for GSK3 and effectively serves as the phosphate group donor in GSK3β-catalyzed phosphorylation of its substrate peptide [1].

Antitrypanosomal agent 14 (Compound 1), a potent T. brucei inhibitor with an effective concentration (EC50) of 0.47 μM, also inhibits Tb GSK3 with an inhibitory concentration (IC50) of 12 μM, and is utilized in the research of Human African Trypanosomiasis [1].

PT-65, a potent and selective GSK3 degrader, demonstrates the highest degradation capacity for GSK3α (DC50 = 28.3 nM) and GSK3β (DC50 = 34.2 nM) in SH-SY5Y cells, making it applicable for Alzheimer's disease research [1].