GSK-3

GSK-3β inhibitor 1 (compound 3a) is a glycogen synthase kinase 3β (GSK-3β) inhibitor and demonstrates high antidiabetic efficacy, with an IC50 of 4.9 nM.

Indirubin-3'-monoxime-5-sulphonic acid is a potent and selective inhibitor of CDK1, CDK5, and GSK-3β with IC50s of 5 nM, 7 nM, and 80 nM, respectively.

5-Iodo-indirubin-3'-monoxime is a potent GSK-3β, CDK5/P25 and CDK1/cyclin B inhibitor, competing with ATP for binding to the catalytic site of the kinase, with IC50s of 9, 20 and 25 nM, respectively.

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Bikinin is a potent inhibitor of plant GSK-3/Shaggy-like kinase; activates BR signaling downstream of the BR receptor.

BIO-acetoxime (BIA) is a potent and selective GSK-3 inhibitor, with IC50s of both 10 nM for GSK-3α/β. BIO-acetoxime has anticonvulsant and anti-infection activity.

GSK-3β Inhibitor 3 is a potent and selective irreversible covalent inhibitor of Glycogen Synthase Kinase 3β (GSK-3β), exhibiting an IC50 of 6.6 μM. This compound is instrumental in research applications related to acute promyelocytic leukemia, providing insights into GSK-3β's role in cancer signaling pathways and therapeutic strategies. Its specificity allows for detailed studies of GSK-3β inhibition effects on cellular processes and pathways involved in oncogenesis.

Manzamine A is a selective inhibitor of glycogen synthase kinase 3 beta (GSK-3β) and cyclin-dependent kinase 5 (CDK-5), with respective IC50 values of 10.2 μM and 1.5 μM. This compound exhibits significant biological activity, including antimalarial and anticancer effects, and has been shown to inhibit autophagy in pancreatic cancer cells by targeting vacuolar ATPases. Additionally, Manzamine A demonstrates potent antiviral properties against herpes simplex virus type 1 (HSV-1), making it a valuable reagent for diverse research applications in cancer, autophagy, and virology studies.

GSK3β-IN-2 is a potent GSK3β inhibitor with an IC50 of 0.35 nM. This compound activates the Wnt/β-catenin signaling pathway, leading to enhanced neurogenesis and neurite outgrowth. Additionally, GSK3β-IN-2 effectively inhibits Aβ-induced tau hyperphosphorylation at Ser396 and reduces neurofibrillary tangle formation. Its efficacy in ameliorating Alzheimer's disease has been demonstrated in zebrafish models, making it a valuable tool for neurological research.

Laduviglusib dihydrochloride is a selective inhibitor of glycogen synthase kinase-3 (GSK-3), an enzyme involved in numerous cellular processes including glycogen synthesis, cell differentiation, and apoptosis. By inhibiting GSK-3, Laduviglusib dihydrochloride promotes cell survival and has been extensively studied in the context of neurodegenerative diseases, diabetes, and cancer research. This compound serves as a valuable tool for elucidating the role of GSK-3 in various signaling pathways and therapeutic applications.

BRD1172 is a selective inhibitor of glycogen synthase kinase 3 beta (GSK3β), exhibiting an IC50 of 24 nM. This compound effectively inhibits GSK3β-mediated Tau phosphorylation in SH-SY5Y cells and alleviates the negative regulation of GSK3β on β-catenin degradation and TCF/LEF promoter activity. BRD1172 is applicable in research related to Alzheimer’s disease, cardiac hypertrophy, and various cancers.

GSK-3β inhibitor 24 is a highly potent inhibitor of glycogen synthase kinase 3 beta (GSK-3β), exhibiting an IC50 of 0.22 nM. This compound effectively enhances GSK-3β phosphorylation at the Ser9 site in a dose-dependent manner, while reducing hyperphosphorylation of tau protein, specifically lowering p-tau-Ser396 levels. Additionally, GSK-3β inhibitor 24 promotes the upregulation of β-catenin and neurogenesis-related markers such as GAP43 and MAP-2, making it a valuable tool in Alzheimer's disease research and therapeutic studies.

GSK-3α/β-IN-1 is a selective inhibitor of glycogen synthase kinase-3 alpha and beta (GSK-3α/β), demonstrating IC50 values of 0.265 μM for GSK-3α and 0.255 μM for GSK-3β. Additionally, GSK-3α/β-IN-1 exhibits PKA inhibition with an IC50 of 0.188 μM. This compound effectively reduces cell viability in several glioblastoma (GBM) cell lines, with IC50 values ranging from 3 to 6 μM over 72 hours, while displaying minimal toxicity to human astrocytes. GSK-3α/β-IN-1 also shows promising central nervous system activity in human blood-brain barrier models of GBM, supporting its potential as a therapeutic agent in cancer research.

Manzamine A hydrochloride is an orally active beta-carboline alkaloid that specifically inhibits GSK-3β and CDK-5, with IC50 values of 10.2 μM and 1.5 μM, respectively. This compound demonstrates significant antimalarial and anticancer properties, with additional effects such as inhibiting vacuolar ATPases and autophagy processes in pancreatic cancer cells. Furthermore, Manzamine A hydrochloride exhibits potent activity against HSV-1, making it valuable for various research applications in cancer biology and virology.

Fyn-IN-1 is a selective inhibitor of Fyn and GSK-3β, demonstrating IC50 values of 0.044 μM and 0.61 μM, respectively. This compound effectively downregulates the expression of the pro-inflammatory enzyme iNOS, making it a valuable tool in studying neuroinflammatory processes. Fyn-IN-1 is particularly relevant for research focused on neurodegenerative diseases, providing insights into potential therapeutic interventions.

GNF4877 is a potent dual inhibitor of DYRK1A and GSK3β, demonstrating IC50 values of 6 nM and 16 nM, respectively. This inhibition results in the blockade of nuclear export of nuclear factor of activated T-cells (NFATc) and promotes β-cell proliferation, with an EC50 of 0.66 μM in mouse β (R7T1) cells. GNF4877 serves as a valuable tool in research related to diabetes and T-cell signaling pathways.

ARN25068 is a sub-micromolar inhibitor targeting the protein kinases GSK-3β, FYN, and DYRK1A. It plays a significant role in modulating tau hyperphosphorylation, which is implicated in neurodegenerative diseases. This compound is valuable for research applications focused on neurobiology and pathology related to tau protein and related neurodegenerative processes.

GSK3-IN-10 is a potent inhibitor of glycogen synthase kinase 3 (GSK3) isoforms α and β, demonstrating IC50 values of 1.0 nM and 2.0 nM, respectively. This compound effectively inhibits the activation of β-catenin, thereby promoting neuronal survival and providing a protective effect against endoplasmic reticulum stress. GSK3-IN-10 is valuable for research applications focused on neuroprotection and cellular stress response mechanisms.

AChE/GSK-3β-IN-1 is a dual inhibitor targeting acetylcholinesterase (AChE) and glycogen synthase kinase 3 beta (GSK-3β), demonstrating potent inhibition with IC50 values of 1.2 nM for hAChE, 149.8 nM for hBChE, and 22.4 nM for hGSK-3β. This compound effectively penetrates the blood-brain barrier and displays high selectivity for the CMGC kinase family, particularly binding to the ATP site of DYRK1A. Additionally, AChE/GSK-3β-IN-1 has been shown to inhibit reactive oxygen species (ROS) expression, thereby reducing oxidative stress. It is a valuable tool for research into Alzheimer's disease and related neurodegenerative conditions.

SGK1-IN-8 is a potent inhibitor of SGK1 and GSK3β, exhibiting an IC50 of 0.11 μM against human SGK1 and 3.39 μM against human GSK3β. This compound effectively inhibits the catalytic activities of both SGK1 and GSK3β, leading to a reduction in the phosphorylation of the TAU protein at the Ser214 site. SGK1-IN-8 is utilized in research focused on Alzheimer's disease and related neurodegenerative disorders.