Two isoforms, alpha and beta, make up the multifunctional serine/threonine kinase known as glycogen synthase kinase-3 (GSK-3). It controls the receptor tyrosine kinase, cytokine, and Wnt signaling pathways negatively and is highly conserved. Inhibiting GSK-3 through the stimulation of these pathways affects a variety of downstream effectors, such as transcription factors, nutrient sensors, glycogen synthesis, mitochondrial function, circadian rhythm, and cell fate. In response to T-cell receptor activation, GSK-3 also controls alternative splicing, and current phosphoproteomic studies have shown that numerous splicing regulators and splicing factors are phosphorylated in a GSK-3-dependent manner.
Alzheimer's disease (AD) and other neurodegenerative pathologies, as well as other types of diseases like diabetes, cardiovascular problems, and cancer, are caused by the dysfunction or abnormal activity of GSK-3. GSK-3 is a prime candidate for therapeutic intervention because it is also connected to innate immune defense against pathogens.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V69855 | Cu(II)GTSM | 68341-14-0 | Cu(II)GTSM is a cell-permeable (penetrable) copper complex that significantly inhibits GSK3β. |
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V67513 | FRATtide | 251087-38-4 | FRATtide is a bioactive peptide extracted from GSK-3 binding protein that can inhibit the phosphorylation of Axin and β-catenin. |
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V69706 | GNF4877 | 2041073-22-5 | GNF4877 is a potent inhibitor of DYRK1A and GSK3β with IC50s of 6 nM and 16 nM respectively, leading to blockage of NFATc nuclear export and increased β-cell proliferation/growth (EC50 for mouse β (R7T1) cells is 0.66 μM). |
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V3531 | GSK-3 inhibitor 1 | 603272-51-1 | GSK-3 inhibitor 1 is a novel and potent inhibitor ofGSK-3 (Glycogen synthase kinase-3). |
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V69841 | GSK-3 Inhibitor XIII | 404828-14-4 | GSK-3 Inhibitor XIII is a potent ATP-competitive GSK-3 inhibitor (antagonist) with Ki of 24 nM. |
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V69858 | GSK-3β inhibitor 11 | 536731-65-4 | GSK-3β inhibitor 11 (compound 21) is a glycogen synthase-3β (GSK-3β) inhibitor (IC50=10.02 μM). |
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V69843 | GSK-3β inhibitor 12 | 784170-07-6 | GSK-3β inhibitor 12 (compound 15) is an inhibitor (blocker/antagonist) of GSK-3β. |
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V69844 | GSK-3β inhibitor 14 | 863004-48-2 | GSK-3β inhibitor 14 (Compound 6i), a benzothiazazone analogue, is a weak GSK-3β inhibitor (IC50 >100 μM). |
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V69856 | GSK-3β inhibitor 3 | 1448990-73-5 | GSK-3β inhibitor 3 is a specific, irreversible and covalent inhibitor of glycogen synthase kinase 3β (GSK-3β) with IC50 of 6.6 μM. |
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V69857 | GSK-3β inhibitor 8 | 1139875-74-3 | GSK-3β inhibitor 8 is a thienopyrimidine analogue that is a potent and specific GSK-3β inhibitor (IC50=64 nM). |
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V76954 | GSK3 Substrate, α, β subunit | GSK3 Substrate, α, β subunit is a bioactive peptide substrate for glycogen synthase kinase-3 (GSK-3) and may be utilized to measure GSK-3 activity. | |
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V69849 | GSK3-IN-2 | 380450-97-5 | GSK3-IN-2 (compound 8) is a potent GSK3 inhibitor. |
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V69842 | GSK3-IN-4 | 748145-19-9 | GSK3-IN-4 (compound 0715) is a potent GSK3 inhibitor. |
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V0226 | IM-12 | 1129669-05-1 | IM-12, anindolylmaleimide analog, is a novel, potent, cell-permeable and selective inhibitor of GSK-3β (glycogen synthase kinase-3β) withpotential neuroprotective effects. |
|
V0225 | Indirubin (NSC 105327; Couroupitine B) | 479-41-4 | Indirubin(also known as NSC-105327; Couroupitine B)is a potent and selective inhibitor of CDK (cyclin-dependent kinases) and GSK-3β(glycogen synthase kinase-3)with potential antitumor activity. |
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V3648 | Indirubin-3′-monoxime | 160807-49-8 | Indirubin-3'-monoxime is a novel, potent and selective inhibitor ofGSK-3β(glycogen synthase kinase 3β) which also weakly inhibits5-LipoxygenasewithIC50s of 22 nM and 7.8-10 µM, respectively; Indirubin-3'-monoxime also shows inhibitory activities against CDK5/p25 and CDK1/cyclin B, withIC50s of 100 and 180 nM. |
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V2448 | KY19382 | 2226664-93-1 | KY-19382 is a novel, potent and orally active dual inhibitor of CXXC5-DVL( IC50s =19)and GSK3β( IC50s = 10 nM). |
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V69847 | L803-mts (Myristoylated L 803; GSK-3β Inhibitor XIII) | 1043881-55-5 | L803-mts (Myristoylated L 803) is a selective substrate-competitive GSK-3 peptide inhibitor (IC50= 40 μM). |
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V2805 | Laduviglusib (CHIR-99021; CT99021) HCl | 1797989-42-4 | Laduviglusib (CHIR-99021; CT99021 or CHIR-911) HCl is the hydrochloride salt of CHIR-99021, which is a potent and orally available GSK-3α/β (glycogen synthase kinase 3α/β) inhibitor with IC50 of 10 nM/6.7 nM in cell-free assays; CHIR-99021 was proved to promote self-renewal and maintain pluripotency of both B6 and BALB/c ES cells via stabilizing the downstream effectors like c-Myc and β -catenin. |
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V0211 | Laduviglusib (CHIR99021) | 252917-06-9 | Laduviglusib (CHIR-99021; CT99021; CT 99021) is a novel, potent and orally bioavailable inhibitor of GSK-3α/β (glycogen synthase kinase 3α/β) with the potential to treattype 2 diabetes. |
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