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 (186)
Related Products (186)
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Recombinant Proteins (5)
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Antibodies (4)
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GSK-3 inhibitor 3
0 ImagesGSK-3 inhibitor 3 is a selective, orally active and brain-penetrant inhibitor of GSK-3, with IC50s of 0.35 nM and 0.25 nM for GSK-3α and GSK-3β, respectively. GSK-3 inhibitor 3 lowers levels of tau protein phosphorylation at S396 in a triple-transgenic mouse Alzheimer’s disease model, with IC50 of 10 nM. GSK-3 inhibitor 3 can be used for neurological disease research.
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GSK-3β inhibitor 1
0 ImagesGSK-3β inhibitor 1 (compound 3a) inhibits GSK-3β with an IC50 of 4.19 nM. GSK-3β inhibitor 1 demonstrates high antidiabetic efficacy in obese Streptozotocin (HY-13753)-treated rats.
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GSK-3β inhibitor 3
0 ImagesGSK-3β inhibitor 3 is a potent, selective, irreversible and covalent inhibitor of Glycogen Synthase Kinase 3β (GSK-3β), with an IC50 of 6.6 μM. GSK-3β inhibitor 3 can be used for the research of acute promyelocytic leukemia.
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GSK3β inhibitor II
0 ImagesGSK3β inhibitor II is an inhibitor of GSK3β. GSK3β inhibitor II can be used for research of Alzheimer’s disease (AD).
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Physalin B
0 ImagesCat. No.: HY-N7695CAS No.: 23133-56-4Physalin B is an orally active anti-inflammatory and anticancer agent. Physalin B can be isolated from Physalis alkekengi L. var. Franchetii. Physalin B inhibits the activation of the NF-κB, NLRP3 inflammasome, STAT3, PI3K/Akt and Hedgehog signaling pathways, regulates the phosphorylation levels of GSK-3β, p38 MAPK, ERK1/2 and JNK, and promotes the nuclear translocation of NRF2. Physalin B reduces the levels of pro-inflammatory cytokines and factors, induces mitochondrial reactive oxygen species (mito-ROS) production, Apoptosis, G2/M cell cycle arrest and incomplete Autophagy, alters cytoskeleton structure and alleviates oxidative stress. Physalin B reduces cancer cell viability, ameliorates liver and lung tissue damage and alleviates liver fibrosis. Physalin B can be used in research related to ulcerative colitis, breast cancer, acute lung injury, colon cancer, non-alcoholic steatohepatitis, liver fibrosis, lung cancer, pancreatic cancer, lymphoma, ovarian cancer, sarcoma and leukemia.
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GSK3β-IN-2
0 ImagesGSK3β-IN-2 (Compound S01) is the inhibitor for GSK3β with an IC50 of 0.35 nM. GSK3β-IN-2 activates Wnt/β-catenin signaling pathway, promotes neurogenesis and neurite growth. GSK3β-IN-2 inhibits Aβ-induced tau hyperphosphorylation at Ser396, reduces the formation of neurofibrillary tangles. GSK3β-IN-2 ameliorates Alzheimer's Disease in zebrafish model.
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Erlotinib Hydrochloride (Standard)
0 ImagesSynonyms: CP-358774 hydrochloride (Standard); NSC 718781 hydrochloride (Standard); OSI-774 hydrochloride (Standard)Erlotinib Hydrochloride Standard (CP-358774 hydrochloride Standard) is the analytical standard of Erlotinib Hydrochloride (HY-12008). This product is intended for research and analytical applications. Erlotinib (CP-358774) Hydrochloride is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib Hydrochloride 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 Hydrochloride blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib Hydrochloride 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 Hydrochloride is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib Hydrochloride 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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COB-187
0 ImagesCat. No.: HY-162675CAS No.: 1862177-86-3
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GSK2646264
0 ImagesGSK2646264 (Compound 44) is a potent and selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.1. GSK2646264 also inhibits other kinases with pIC50 values of 5.4, 5.4, 5.3, 5, 4.5, <4.6 and <4.3 against LCK, LRRK2, GSK3β, JAK2, VEGFR2, Aurora B and Aurora A, respectively. GSK2646264 is penetrable into the epidermis and dermis of the skin.
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Wnt/β-catenin-IN-6
0 ImagesCat. No.: HY-172920Purity: 98.34%Wnt/β-catenin-IN-6 is an orally active Wnt/β-catenin pathway inhibitor. Wnt/β-catenin-IN-6 blocks the AKT/GSK-3β/β-catenin signaling pathway, leading to reduced expression of Wnt target genes (c-Myc, c-Jun). Wnt/β-catenin-IN-6 reduces COX2 expression and IL-8 levels, highlighting its dual anti-inflammatory and antitumor effects. Wnt/β-catenin-IN-6 can induce apoptosis. Wnt/β-catenin-IN-6 serves as a tool for non-small cell lung cancer (NSCLC) research.
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8012–3246
0 Images8012-3246 is a selective PLK2 inhibitor with an IC50 of 774.5 nM. 8012-3246 suppresses GSK3β phosphorylation. 8012-3246 exhibits potent anticancer activity against colorectal cancer.
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GSK-3β inhibitor 8
0 ImagesGSK-3β inhibitor 8, a thiophenacil derivative, is an effective and selective inhibitor of GSK-3β (IC50=64 nM). GSK-3β inhibitor 8 negatively regulated Wnt signaling pathway and stimulated β cell proliferation.
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(E)-Methyl 4-coumarate
0 ImagesSynonyms: Methyl trans-p-coumarate(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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Erlotinib-d6
0 ImagesSynonyms: CP-358774-d6; NSC 718781-d6; OSI-774-d6Erlotinib-d6 (CP-358774-d6) 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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GSK-3β inhibitor 23
0 ImagesCat. No.: HY-170491Purity: 99.88%GSK-3β inhibitor 23 (Compound 11726169) is the inhibitor for glycogen synthase kinase-3, that inhibits GSK-3β and GSK-3α with IC50 of 12.1 nM and 18.8 nM. GSK-3β inhibitor 23 exhibits antiviral activity against HIV 1. GSK-3β inhibitor 23 exhibits good metabolic stablility in mouse/human liver microsomes and plasma, but poor Caco-2 permeability (which predicts low oral bioavailability).
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(E/Z)-BIO-acetoxime
0 ImagesSynonyms: GSK-3 Inhibitor X(E/Z)-BIO-acetoxime (GSK-3 Inhibitor X) is a potent and selective GSK-3α/β inhibitor, with an IC50 of 10 nM. (E/Z)-BIO-acetoxime shows more than 200-flod selectivity over CDK5/p25, CDK2/cyclin A and CDK1/cyclin B (IC50=2.4, 4.3, 63 μM).
