GSK-3β
Glycogen synthase kinase-3β (GSK-3β) is a constitutively active serine/threonine kinase that regulates numerous cellular substrates and functions as a central signaling node in metabolism, development, and cell fate control[1]. Mechanistically, GSK-3β participates in multiple signaling pathways, including Wnt/β-catenin, PI3K/Akt, Notch, and NF-κB networks, where its phosphorylation-dependent activity influences transcriptional regulation, cellular differentiation, and stress responses[2][3]. Through these pathway interactions, GSK-3β contributes to the control of glucose metabolism and broader cardiometabolic homeostasis, while dysregulated GSK-3β signaling has been linked to pathological remodeling and disease progression in diverse experimental models[4][1]. In neurological disease models, GSK-3β has been associated with hyperphosphorylated tau pathology and neuronal dysfunction, supporting its relevance as a target for mechanistic studies of neurodegeneration[3]. Compared with the closely related isoform GSK-3α, GSK-3β exhibits both overlapping and isoform-specific biological functions, and genome-wide as well as genetic studies demonstrate distinct downstream targets and physiological roles for the two kinases[4][5][6]. This isoform divergence is particularly important for experimental design because GSK-3α and GSK-3β can exert different or even opposing effects in specific biological contexts[4]. For experimental applications, small-molecule GSK-3 inhibitors remain widely used research tools; however, many available compounds lack isoform selectivity, emphasizing the need for isoform-specific pharmacological and genetic approaches when investigating GSK-3β-dependent mechanisms[6][5].
References:
- [1]. Beurel E, et al. Glycogen synthase kinase-3 (GSK3): regulation, actions, and diseases. Pharmacol Ther. 2015 Apr;148:114-31. [Content Brief]
- [2]. Espinosa L, et al. Phosphorylation by glycogen synthase kinase-3 beta down-regulates Notch activity, a link for Notch and Wnt pathways. J Biol Chem. 2003 Aug 22;278(34):32227-35. [Content Brief]
- [3]. Kaidanovich-Beilin O, et al. GSK-3: Functional Insights from Cell Biology and Animal Models. Front Mol Neurosci. 2011 Nov 16;4:40. doi: 10.3389/fnmol.2011.00040. PMID: 22110425; PMCID: PMC3217193. [Content Brief]
- [4]. Umbarkar P, et al. GSK-3 at the heart of cardiometabolic diseases: Isoform-specific targeting is critical to therapeutic benefit. Biochim Biophys Acta Mol Basis Dis. 2023 Aug;1869(6):166724. doi: 10.1016/j.bbadis.2023.166724. Epub 2023 Apr 23. PMID: 37094727; PMCID: PMC10247467. [Content Brief]
- [5]. Lee HC, et al. Glycogen synthase kinase 3 alpha and 3 beta have distinct functions during cardiogenesis of zebrafish embryo. BMC Dev Biol. 2007 Aug 3;7:93. [Content Brief]
- [6]. Chen X, et al. A Chemical-Genetic Approach Reveals the Distinct Roles of GSK3α and GSK3β in Regulating Embryonic Stem Cell Fate. Dev Cell. 2017 Dec 4;43(5):563-576.e4. doi: 10.1016/j.devcel.2017.11.007. PMID: 29207259; PMCID: PMC5851779. [Content Brief]
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GSK-3β Related Products (187)
Related Products (187)
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Recombinant Proteins (5)
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Antibodies (4)
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AChE/BChE-IN-37
0 ImagesCat. No.: HY-183760AChE/BChE-IN-37 is a blood-brain barrier-permeable AChE/BChE inhibitor, with an IC50 of 73.65 μM against electric eel-derived AChE and an IC50 of 82.93 μM against horse-derived BChE. AChE/BChE-IN-37 exhibits chelating activity towards Cu2+, Ca2+, Mg2+, Fe2+ and Zn2+. AChE/BChE-IN-37 interacts with HSP90AA1 and GSK-3β. AChE/BChE-IN-37 inhibits the self-induced aggregation of Aβ1-42. AChE/BChE-IN-37 suppresses LPS-induced NO production in cells. AChE/BChE-IN-37 can be used in research related to Alzheimer's disease and inflammatory diseases.
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JGK-263
0 ImagesCat. No.: HY-114270CAS No.: 1408054-46-5JGK-263 is an orally active Glycogen synthase kinase-3β (GSK-3β) inhibitor. JGK-263 exhibits neuroprotective effect and can improve motor function. JGK-263 can be used for the research of neurological disease, such as amyotrophic lateral sclerosis (ALS).
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DA5-CH
0 ImagesCat. No.: HY-P12141CAS No.: 2227651-65-0Synonyms: KP405DA5-CH (KP405) is a blood-brain barrier-permeable GLP-1/GIP receptor agonist. DA5-CH activates GLP-1 and GIP receptors, inhibits the NF-κB inflammatory pathway, reduces α-synuclein (α-synuclein) levels, restores the expression of tyrosine hydroxylase and neurotrophic factors, improves motor function, decreases amyloid plaques and phosphorylated tau protein levels in the hippocampus, restores synaptic plasticity, regulates the PI3K/AKT/GSK3β and CREB signaling pathways, and alleviates mitochondrial stress. DA5-CH can be used for research on Parkinson's disease and Alzheimer's disease.
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BI-5521
0 ImagesCat. No.: HY-171881CAS No.: 864686-48-6BI-5521 is an orally active GSK-3 inhibitor with an IC50 of 1.1 nM against GSK-3β. BI-5521 targets the two GSK-3 isoforms with similar potency and exhibits potent inhibitory activity against DYRK1A. By modulating GSK-3 activity, BI-5521 inhibits tumor proliferation and cancer cell growth, exerts cytotoxic effects, and reduces cancer cell viability. It shows consistent chemosensitivity across all subtypes of rhabdomyosarcoma, produces synergistic growth inhibitory effects when combined with SOS1 inhibitors, reduces oral glucose levels, regulates the myofibroblast differentiation pathway, decreases the nuclear localization of YAP/SMAD2/3, and lowers the positive rate of α-SMA in fibroblasts without affecting the apoptosis of CD4+ T cells. BI-5521 can be used in the research of non-small cell lung cancer, pleomorphic rhabdomyosarcoma, type 2 diabetes, pancreatic ductal adenocarcinoma, Alzheimer's disease, bipolar disorder, and metabolic dysfunction-associated steatotic liver disease.
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GSK-3β-IN-31
0 ImagesCat. No.: HY-187681CAS No.: 889768-87-0GSK-3β-IN-31 is a glycogen synthase kinase-3β (GSK-3β) inhibitor. GSK-3β-IN-31 binds to the ATP-binding pocket of GSK-3β, forms hydrogen bonds with Lys183 and Ser203, and also engages in π-anion interactions with Asp181 and Asp200 to stabilize the binding conformation. GSK-3β-IN-31 can be used for the research of Alzheimer's disease.
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ZDWX-25
0 ImagesCat. No.: HY-144826CAS No.: 2668297-70-7ZDWX-25 is a highly potent GSK-3β and DYRK1A dual inhibitor with an IC50 value of 71 nM for GSK-3β. ZDWX-25 possesses significant cytotoxic activities against SH-SY5Y and HL-7702 cells. ZDWX-25 can be used for researching alzheimer's disease.
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GSK-3β/VEGFR2-IN-1
0 ImagesCat. No.: HY-184741GSK-3β/VEGFR2-IN-1 is an orally active dual inhibitor of GSK-3β (IC50 = 325 nM) and VEGFR2 (IC50 = 78 nM). GSK-3β/VEGFR2-IN-1 suppresses the phosphorylation of VEGFR2, AKT, MEK and ERK, inhibits human tongue squamous cell carcinoma cells migration and suppresses formation of HUVECs, exhibits low toxicity towards other cancer cells and normal cells, demonstrates significant antitumor efficacy in a CAL27 xenograft mouse model. GSK-3β/VEGFR2-IN-1 can be used for the study of tongue squamous cell carcinoma.
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GSK-3β inhibitor 18
0 ImagesCat. No.: HY-162638GSK-3β inhibitor 18 (compound 2) is a potent inhibitor of GSK-3β, with the IC50 of 0.0021 μM.
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JNK3 inhibitor-9
0 ImagesCat. No.: HY-168859JNK3 inhibitor-9 (Compound 24a) is a potent, selective and BBB-permeable JNK3 inhibitor with an IC50 value of 12 nM. JNK3 inhibitor-9 also potently inhibits GSK3α/β (IC50s: 14 and 35 nM, respectively) involved in Tau phosphorylation. JNK3 inhibitor-9 reduces c-Jun and APP phosphorylation. JNK3 inhibitor-9 protects neurons from Aβ1-42 toxicity.
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Erlotinib-13C6
0 ImagesCat. No.: HY-50896S1CAS No.: 1211107-68-4Synonyms: CP-358774-13C6; NSC 718781-13C6; OSI-774-13C6Erlotinib-13C6 (CP-358774-13C6) is the 13C-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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Dihydronarwedine
0 ImagesCat. No.: HY-133102CAS No.: 21041-10-1Synonyms: LycoraminoneDihydronarwedine (Lycoraminone) is the alkaloid. Dihydronarwedine inhibits 39% activity of glycogen synthase kinase-3β (GSK-3β) at a concentration of 10 μM.
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GNF7156
0 ImagesCat. No.: HY-183955CAS No.: 2041071-54-7GNF7156 is a DYRK1A/GSK3B inhibitor, IC50 values of 100 nM for DYRK1A and 40 nM for GSK3B. GNF7156 inhibits DYRK1A and GSK3B kinase activity and induces NFAT nuclear retention. GNF7156 stimulates beta-cell cycle entry and division and maintains insulin secretory capacity. GNF7156 can be used for the research of type 1 diabetes, and type 2 diabetes.
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Multi-kinase-IN-14
0 ImagesCat. No.: HY-181046CAS No.: 2201083-51-2Multi-kinase-IN-14 is an orally active and blood-brain barrier-permeable multi-kinase inhibitor. Multi-kinase-IN-14 reduces the excessive phosphorylation of α-synuclein by inhibiting four kinases (ABL1, DYRK1A, GSK3β, and LRRK2) and stabilizing microtubules. Multi-kinase-IN-14 is applicable for research on neurodegenerative diseases such as Parkinson’s disease and Alzheimer’s disease.
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PHA-793887 hydrochloride
0 ImagesCat. No.: HY-11001ACAS No.: 718630-60-5PHA-793887 hydrochloride is a CDK inhibitor (with IC50 values of 8 nM for Cdk2, 60 nM for Cdk1, 62 nM for Cdk4, 138 nM for Cdk9). PHA-793887 hydrochloride inhibits purified GSK3β (IC50 79 nM). PHA-793887 hydrochloride reduces the phosphorylation level of nucleophosmin/cdc6, induces G1/G2/M phase arrest, and triggers Apoptosis by activating Caspase-3. PHA-793887 hydrochloride exhibits anticancer activity against leukemia. PHA-793887 hydrochloride can be used in research related to acute leukemia, chronic myeloid leukemia, and advanced/metastatic solid tumors.
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Amsacrine isethionate
0 ImagesCat. No.: HY-13551CCAS No.: 80277-14-1Synonyms: m-AMSA isethionate; Acridinyl anisidide isethionateAmsacrine isethionate (m-AMSA isethionate) is a Topoisomerase II inhibitor. Amsacrine isethionate intercalates into DNA. Amsacrine isethionate induces Ca2+-mediated inactivation of ERK, and also downregulates AKT, promoting MCL1 downregulation mediated by GSK3β via reducing the phosphorylation level of GSK3β. Amsacrine isethionate induces Apoptosis by activating Caspase-9 and Caspase-3. Amsacrine isethionate blocks HERG potassium channels in the open/inactivated state. Amsacrine isethionate induces chromosomal aberrations and sister chromatid exchanges, and inhibits the synthesis of RNA and DNA. Amsacrine isethionate exhibits anti-leukemic activity. Amsacrine isethionate causes cardiac repolarization disorders, QT interval prolongation, ventricular arrhythmias, and increases the risk of sudden cardiac death. Amsacrine isethionate can be used in research related to acute myeloid leukemia, lymphoma and progressive malignancies.
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Bisphenol F-13C12
0 ImagesCat. No.: HY-W014901S1CAS No.: 1410794-08-9Synonyms: BPF-13C12; 4,4'-Dihydroxydiphenylmethane-13C12Bisphenol F-13C12 is the 13C labeled Bisphenol F (HY-W014901). Bisphenol F is an orally active endocrine disruptor. Bisphenol F promotes ROS generation, upregulates p-AKT/p-GSK3β, and induces Apoptosis. Bisphenol F interferes with glucose metabolism, affects neurodevelopment and reproductive function. Bisphenol F reduces social novelty preference in mouse offspring. Bisphenol F can be used in bone, blood, and fat-related studies. Bisphenol F is used as a substitute for Bisphenol A (HY-18260).
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2-Cyanoethylalsterpaullone
0 ImagesCat. No.: HY-112394CAS No.: 852527-97-02-Cyanoethylalsterpaullone (compound 7) is an Alsterpaullone (HY-108359) derivative, which exhibits potent and selective inhibitory activities against CDK1/Cyclin B and GSK-3β (GSK-3β: IC50=0.8 nM; CDK1/Cyclin B: IC50=0.23 nM).
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Bisphenol F (Standard)
0 ImagesSynonyms: BPF (Standard); 4,4'-Dihydroxydiphenylmethane (Standard)Bisphenol F (Standard) is the analytical standard of Bisphenol F (HY-W014901). This product is intended for research and analytical applications. Bisphenol F is an orally active endocrine disruptor. Bisphenol F promotes ROS generation, upregulates p-AKT/p-GSK3β, and induces Apoptosis. Bisphenol F interferes with glucose metabolism, affects neurodevelopment and reproductive function. Bisphenol F reduces social novelty preference in mouse offspring. Bisphenol F can be used in bone, blood, and fat-related studies. Bisphenol F is used as a substitute for Bisphenol A (HY-18260).
