GSK-3
Glycogen synthase kinase-3; Glycogen synthase kinase 3
Glycogen synthase kinase 3 (GSK-3) is a multifunctional serine/threonine kinase consisting of two isoforms, alpha and beta. It is a highly conserved negative regulator of receptor tyrosine kinase, cytokine, and Wnt signaling pathways. Stimulation of these pathways inhibits GSK-3 to modulate diverse downstream effectors that include transcription factors, nutrient sensors, glycogen synthesis, mitochondrial function, circadian rhythm, and cell fate. GSK-3 also regulates alternative splicing in response to T-cell receptor activation, and recent phosphoproteomic studies have revealed that multiple splicing factors and regulators of RNA biosynthesis are phosphorylated in a GSK-3-dependent manner.
The malfunction or aberrant activity of GSK-3 leads to several of disorders, such as Alzheimer's disease (AD) and other neurodegenerative pathologies, and other type of diseases as diabetes, cardiovascular disorders and cancer. GSK-3 is also related to innate immune response against pathogens, which makes GSK-3 an excellent target for therapeutic intervention.
GSK-3 Isoform Specific Products
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GSK-3 Inhibitors
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GSK-3 Agonist
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GSK-3 Activators
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GSK-3 Modulators
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GSK-3 Chemicals
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GSK-3 Degraders
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GSK-3 Ligand
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Glycogen Synthase Kinase-3 (GSK-3) Proteins
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GSK-3 alpha Proteins
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GSK-3 beta Proteins
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GSK-3 Related Products (373)
Related Products (373)
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Recombinant Proteins (6)
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Antibodies (9)
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GSK-3 Signaling Pathway
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GSK-3 Isoform Comparison
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MeBIO (Standard)
0 ImagesCat. No.: HY-103221RCAS No.: 667463-95-8
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MRT68921 dihydrochloride (Standard)
0 ImagesMRT68921 (dihydrochloride) (Standard) is the analytical standard of MRT68921 (dihydrochloride) (HY-100006A). This product is intended for research and analytical applications. MRT68921 dihydrochloride is a potent NUAK1/ULK1 dual inhibitor. MRT68921 dihydrochloride inhibits ULK1 and ULK2 with IC50 values of 2.9 nM and 1.1 nM, respectively. MRT68921 dihydrochloride can block cells autophagy and kill tumor cells by breaking the balance of oxidative stress signals. MRT68921 dihydrochloride can inhibit cell proliferation and induce ROS production and apoptosis. MRT68921 dihydrochloride can be used for the research of cancer, such as breast cancer.
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Antitrypanosomal agent 31
0 ImagesCat. No.: HY-183529CAS No.: 551919-54-1Antitrypanosomal agent 31 is an antitrypanosoma agent with a pEC50 of 6.4. Antitrypanosomal agent 31 inhibits GSK-3β, CDK-2, and CDK-4 with pIC50s of 5.8, 6.9, and 7.1, respectively. Antitrypanosomal agent 31 can be used for the research of human african trypanosomiasis.
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(E)-Methyl 4-coumarate (Standard)
0 ImagesSynonyms: Methyl trans-p-coumarate (Standard)(E)-Methyl 4-coumarate (Standard) is the analytical standard of (E)-Methyl 4-coumarate (HY-N2492). This product is intended for research and analytical applications. (E)-Methyl 4-coumarate (Methyl 4-hydroxycinnamate) is a phenolic compound and derivative of Cinnamic acid (HY-N0610A). (E)-Methyl 4-coumarate can be found in several plants, such as the leaves of Allium cepa and Morinda citrifolia L. (E)-Methyl 4-coumarate, when combined with Carnosic acid (HY-N0644), induces Apoptosis. (E)-Methyl 4-coumarate inhibits GSK3β activity and modulates inflammatory cytokine levels (increasing IL-10 and decreasing IL-4). (E)-Methyl 4-coumarate combined with Carnosic acid exhibits anticancer effects against acute myeloid leukemia. (E)-Methyl 4-coumarate ameliorates Plasmodium berghei NK65 infection.
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5-Iodo-indirubin-3'-monoxime (Standard)
0 ImagesCat. No.: HY-111930RCAS No.: 331467-03-95-Iodo-indirubin-3'-monoxime (Standard) is the analytical standard of 5-Iodo-indirubin-3'-monoxime (HY-111930). This product is intended for research and analytical applications. 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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Cefetecol hydrate
0 ImagesCat. No.: HY-159796CAS No.: 127182-67-6Synonyms: GR69153 hydrateCefetecol hydrate (GR69153 hydrate) is a semisynthetic β-lactam antibacterial agent and α-glucosidase inhibitor (yeast IC50 = 2.1 μM; Ki = 5.78 μM) that crosses the blood-brain barrier. Cefetecol hydrate reduces blood glucose levels in Streptozotocin-induced diabetic mice. Cefetecol hydrate decreases the mRNA expression of GSK-3, PPAR-γ, and UCP-3. Cefetecol hydrate induces bacterial cell filamentation and exhibits bactericidal activity against Gram-positive and Gram-negative bacteria. Cefetecol hydrate is used in the study of diabetes and bacterial infections.
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Laduviglusib trihydrochloride (Standard)
0 ImagesSynonyms: CHIR-99021 trihydrochloride (Standard); CT99021 trihydrochloride (Standard)Laduviglusib (trihydrochloride) (Standard) is the analytical standard of Laduviglusib (trihydrochloride). This product is intended for research and analytical applications. Laduviglusib (CHIR-99021) trihydrochloride is a potent and selective GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. Laduviglusib trihydrochloride shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. Laduviglusib trihydrochloride is also a potent Wnt/β-catenin signaling pathway activator. Laduviglusib trihydrochloride enhances mouse and human embryonic stem cells self-renewal. Laduviglusib trihydrochloride induces autophagy.
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Erlotinib mesylate
0 ImagesCat. No.: HY-12008ACAS No.: 248594-19-6Synonyms: CP-358774 mesylate; NSC 718781 mesylate; OSI-774 mesylateErlotinib (CP-358774) mesylate is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib mesylate also acts as a substrate and inhibitor of OATP2B1, with an IC50 of approximately 0.079 μM for inhibiting OATP2B1-mediated uptake of estrone 3-sulfate. Erlotinib mesylate blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib mesylate inhibits MMP-10-mediated renal injury, fibrotic lesions, the ERK1/2, GSK-3β and β-catenin signaling pathways, as well as the deposition of fibronectin, α-SMA, collagen and renal injury markers. Erlotinib mesylate is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib mesylate can be used in research related to non-small cell lung cancer, gastric cancer, papillary renal cell carcinoma, EGFR inhibitor resistance and renal fibrosis.
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Cazpaullone
0 ImagesCat. No.: HY-12074CAS No.: 914088-64-5Cazpaullone is a glycogen synthase kinase-3 (GSK-3) inhibitor. Cazpaullone can activate pancreatic beta cell protection and replication. Cazpaullone can be used for the research of diabetes.
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DC-120
0 ImagesCat. No.: HY-119884CAS No.: 1261080-40-3DC-120 is an ATP-competitive AKT inhibitor, with particular activity against AKT1 (an IC50 of 0.153 μM). DC-120 functionally blocks AKT kinase activity and reduces the phosphorylation levels of FOXO3a and GSK-3β. DC-120 induces cancer cell apoptosis (apoptosis) and inhibits cancer cell proliferation. DC-120 activates the mTORC1 pathway via the Ca2+/calmodulin (calmodulin)/hVps34 signaling pathway. DC-120 abrogates AKT-mediated inhibition of CRAF, thereby activating the MEK/ERK MAPK pathway. DC-120 exerts anti-tumor activity in a nude mouse hepatocellular carcinoma xenograft model. DC-120 can be used for hepatocellular carcinoma-related research.
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LY2090314 (Standard)
0 ImagesCat. No.: HY-16294RCAS No.: 603288-22-8
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Schisantherin B (Standard)
0 ImagesCat. No.: HY-N0695RCAS No.: 58546-55-7Synonyms: Gomisin-B (Standard); Wuweizi ester-B (Standard); Schisantherin-B (Standard)Schisantherin B (Gomisin-B) (Standard) is the analytical standard of Schisantherin B. This product is intended for research and analytical applications. Schisantherin B is a lignan compound and one of the active components of Schisandra chinensis. Schisantherin B activates the PI3K/AKT signaling pathway, restores the activity of GSK3β, and reduces the hyperphosphorylation of tau protein in hippocampal and cerebral cortical tissues. Schisantherin B upregulates the level of GLT-1, decreases the expression of pro-inflammatory cytokines TNF-α/IL-1β/IL-6, upregulates the expression of IL-10, and inhibits cell apoptosis. Schisantherin B is applicable to the research of spinal cord injury, Alzheimer's disease and depression.
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Hispidin (Standard)
0 ImagesHispidin (Standard) is the analytical standard of Hispidin. This product is intended for research and analytical applications. Hispidin, a PKC inhibitor and a phenolic compound can be found in Phellinus linteus, has been shown to possess strong anti-oxidant, anti-cancer, anti-diabetic, and anti-dementia properties[1][2][3][4][5][6][7].
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K00546 (Standard)
0 ImagesCat. No.: HY-103647RCAS No.: 443798-47-8K00546 (Standard) is the analytical standard of K00546 (HY-103647). This product is intended for research and analytical applications. K00546 is a potent CDK1 and CDK2 inhibitor with IC50s of 0.6 nM and 0.5 nM for CDK1/cyclin B and CDK2/cyclin A, respectively. K00546 is also a potent CDC2-like kinase 1 (CLK1) and CLK3 inhibitor with IC50s of 8.9 nM and 29.2 nM, respectively.
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Acenocoumarol-d5
0 ImagesCat. No.: HY-B1014SCAS No.: 1185071-64-0Acenocoumarol-d5 is the deuterium labeled Acenocoumarol (HY-B1014). Acenocoumarol is an anticoagulant that functions as a Vitamin K antagonist. Acenocoumarol inhibits MAPK/ERK/JNK signaling pathway, reduces the nuclear translocation of NF-κB p65, activates Akt/GSK3β signaling pathway. Acenocoumarol induces apoptosis in cell A549, arrests cell cycle at S phase.
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Flurochloridone (Standard)
0 ImagesCat. No.: HY-121337RCAS No.: 61213-25-0Synonyms: R-40244 (Standard)Flurochloridone (Standard) (R-40244 (Standard)) is the analytical standard of Flurochloridone (HY-121337). This product is intended for research and analytical applications. Flurochloridone (R-40244) is an orally active herbicide and an inducer of ER stress, apoptosis, and cytotoxicity. Flurochloridone upregulates GRP78 and activates the PERK-eIF2α-ATF4 UPR axis, ATF6, CHOP, Bax, and Bim. Flurochloridone decreases Akt, p-Akt, GSK3β, and p-GSK3β levels, and induces ROS, oxidative stress, γ-glutamyl cycle activation, and GSH accumulation. Flurochloridone inhibits mitochondrial respiration and ATP production while enhancing glycolysis and cell viability inhibition. Flurochloridone inhibits spermatogonial proliferation, spermatocyte meiosis, and sperm mitochondrial membrane potential, and induces Sertoli cell apoptosis and mitochondrial damage. Flurochloridone non-competitively binds phytoene desaturase, blocking phytoene desaturation and carotenoid synthesis, leading to leaf bleaching and phytotoxicity. Flurochloridone can be used for research on male reproductive toxicity, hepatotoxicity, and as a herbicide.
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Erlotinib-d4
0 ImagesCat. No.: HY-50896S2CAS No.: 1130852-41-3Synonyms: CP-358774-d4; NSC 718781-d4; OSI-774-d4Erlotinib-d4 (CP-358774-d4) is the deuterated-labeled Erlotinib (HY-50896). Erlotinib (CP-358774) is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib also acts as a substrate and inhibitor of OATP2B1, with an IC50 of approximately 0.079 μM for inhibiting OATP2B1-mediated uptake of estrone 3-sulfate. Erlotinib blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib inhibits MMP-10-mediated renal injury, fibrotic lesions, the ERK1/2, GSK-3β and β-catenin signaling pathways, fibronectin, α-SMA, collagen deposition, and renal injury markers. Erlotinib is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib can be used in research related to non-small cell lung cancer, gastric cancer, papillary renal cell carcinoma, pancreatic cancer, renal fibrosis, and other conditions.
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GCN2/GSK3α-IN-1
0 ImagesCat. No.: HY-208758CAS No.: 1627180-54-4GCN2/GSK3α-IN-1 is a GCN2 and GSK3α inhibitor with an IC50 of less than 1 μM for both targets. GCN2/GSK3α-IN-1 can be used in cancer research.
