GSK-3α
GSK-3α is a serine/threonine kinase within the GSK-3 family, whose activity is negatively regulated by serine phosphorylation and positively controlled by tyrosine phosphorylation[1]. Mechanistically, GSK-3 regulates glycogen synthase, glucose metabolism, energy homeostasis, gene expression, cellular architecture, apoptosis, epithelial barrier proteins, and dendritic-cell inflammatory activation[2][3][4]. In disease models, Gsk3a−/− mice developed progressive cardiomyocyte hypertrophy and contractile dysfunction, and the heart failed to respond effectively to hemodynamic stress[5]. Compared with GSK-3β, GSK-3α showed distinct regulation of CRE- and NF-κB-dependent transactivation, neuronal survival responses, and sperm fertilization, supporting non-redundant isoform biology[1][6][7]. For experimental applications, small-molecule GSK-3 inhibitors and GSK-3α siRNA help test barrier integrity, neuroprotection, β-adrenergic responsiveness, and isoform-specific transcriptional control[1][3][5][6].
References:
- [1]. Liang MH, et al. Differential roles of glycogen synthase kinase-3 isoforms in the regulation of transcriptional activation. J Biol Chem. 2006 Oct 13;281(41):30479-84. [Content Brief]
- [2]. Wang L, et al. Glycogen synthesis and beyond, a comprehensive review of GSK3 as a key regulator of metabolic pathways and a therapeutic target for treating metabolic diseases. Med Res Rev. 2022 Mar;42(2):946-982. [Content Brief]
- [3]. Severson EA, et al. Glycogen Synthase Kinase 3 (GSK-3) influences epithelial barrier function by regulating occludin, claudin-1 and E-cadherin expression. Biochem Biophys Res Commun. 2010 Jul 2;397(3):592-7. [Content Brief]
- [4]. Rodionova E, et al. GSK-3 mediates differentiation and activation of proinflammatory dendritic cells. Blood. 2007 Feb 15;109(4):1584-92. [Content Brief]
- [5]. Zhou J, et al. GSK-3alpha directly regulates beta-adrenergic signaling and the response of the heart to hemodynamic stress in mice. J Clin Invest. 2010 Jul;120(7):2280-91. [Content Brief]
- [6]. Liang MH, et al. Regulation and function of glycogen synthase kinase-3 isoforms in neuronal survival. J Biol Chem. 2007 Feb 9;282(6):3904-17. [Content Brief]
- [7]. Dey S, et al. Roles of glycogen synthase kinase 3 alpha and calcineurin in regulating the ability of sperm to fertilize eggs. FASEB J. 2020 Jan;34(1):1247-1269. [Content Brief]
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GSK-3α Related Products (47)
Related Products (47)
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Recombinant Proteins (1)
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Laduviglusib
0 ImagesSynonyms: CHIR-99021; CT99021Laduviglusib (CHIR-99021) is a potent, selective and orally active GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. Laduviglusib shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. Laduviglusib is also a potent Wnt/β-catenin signaling pathway activator. Laduviglusib enhances mouse and human embryonic stem cells self-renewal. Laduviglusib induces autophagy.
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LY2090314
0 ImagesLY2090314 is a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50 values of 1.5 nM and 0.9 nM for GSK-3α and GSK-3β, respectively.
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Laduviglusib monohydrochloride
0 ImagesSynonyms: CHIR-99021 monohydrochloride; CT99021 monohydrochlorideLaduviglusib (CHIR-99021) monohydrochloride is a potent and selective GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. Laduviglusib monohydrochloride shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. Laduviglusib monohydrochloride is also a potent Wnt/β-catenin signaling pathway activator. Laduviglusib monohydrochloride enhances mouse and human embryonic stem cells self-renewal. Laduviglusib monohydrochloride induces autophagy.
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Laduviglusib trihydrochloride
0 ImagesSynonyms: CHIR-99021 trihydrochloride; CT99021 trihydrochlorideLaduviglusib (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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Multitarget AD-IN-7
0 ImagesCat. No.: HY-182788CAS No.: 3113741-59-3Multitarget AD-IN-7 is an orally active multi-target anti-AD compound. Multitarget AD-IN-7 exhibits inhibitory activity against GSK-3β and GSK-3α (IC50 = 0.66, 0.83 nM). Multitarget AD-IN-7 upregulates the expression of p-GSK-3β-Ser9, inhibits the phosphorylation of tau-Ser396, targets Aβ1-42, chelates pathogenic metal ions, scavenges ABTS•+, upregulates the expression of β-catenin and neurogenesis biomarkers, and promotes neurite outgrowth. Multitarget AD-IN-7 improves motor ability in Alzheimer's disease zebrafish. Multitarget AD-IN-7 is applicable to research related to Alzheimer's disease.
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PROTAC GSK3 degrader-1
0 ImagesCat. No.: HY-185634PROTAC GSK3 degrader-1 is a potent, blood-brain barrier-permeable GSK3 PROTAC degrader, with a DC50 of 1.4 nM against GSK3β. PROTAC GSK3 degrader-1 exerts equally potent degradation activity against both GSK3α and GSK3β. It inhibits the phosphorylation of CRMP2, PRKAA1 and Tau, and stabilizes β-catenin. PROTAC GSK3 degrader-1 can be used in the research of Alzheimer's disease and Parkinson's disease.
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GSK 3 Inhibitor IX
0 ImagesSynonyms: 6-Bromoindirubin-3'-oxime; BIO; MLS 2052GSK 3 Inhibitor IX (6-Bromoindirubin-3'-oxime; BIO) is a potent, selective, reversible and ATP-competitive inhibitor of GSK-3α/β and CDK1-cyclinB complex with IC50s of 5 nM/320 nM/80 nM for (GSK-3α/β)/CDK1/CDK5, respectively.
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Laduviglusib (GMP)
0 ImagesCat. No.: HY-10182GCAS No.: 252917-06-9Synonyms: CHIR-99021 (GMP); CT99021 (GMP)Laduviglusib (CHIR-99021) (GMP) is Laduviglusib (HY-10182) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Laduviglusib is a potent, orally active and selective GSK-3α/β inhibitor.
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AZD1080
0 ImagesAZD1080 is a potent and selective GSK3 inhibitor. AZD1080 inhibits recombinant human GSK3α and GSK3β with pKi (IC50) of 8.2 (6.9 nM) and 7.5 (31 nM), respectively.
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BRD0705
0 ImagesBRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50 of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML) research.
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Alsterpaullone
0 ImagesSynonyms: 9-Nitropaullone; NSC 705701Alsterpaullone (9-Nitropaullone) is a potent CDK inhibitor, with IC50s of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also competes with ATP for binding to GSK-3alpha/GSK-3beta with IC50s of both 4 nM. Alsterpaullone has antitumor activity, and possesses potential for the study in neurodegenerative and proliferative disorders. Alsterpaullone induces apoptosis in leukemia cell line.
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PT-65
0 ImagesPT-65 is a GSK3α and GSK3β PROTAC degrader with DC50 values of 28.3 nM and 34.2 nM, respectively. PT-65 inhibits excessive tau phosphorylation mediated by GSK3β, Aβ and Okadaic acid (HY-N6785). PT-65 is applicable for the research of Alzheimer's disease.
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BIO-acetoxime
0 ImagesSynonyms: BIABIO-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.
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PF-04802367
0 ImagesSynonyms: PF-367PF-04802367 (PF-367) is a highly selective GSK-3 inhibitor with an IC50 of 2.1 nM based on a recombinant human GSK-3β enzyme assay and 1.1 nM based on ADP-Glo assay. PF-04802367 shows desirable central nervous system (CNS) properties and potency. PF-04802367 is equally effective at inhibition of the two known GSK-3 isoforms (GSK-3α and GSK-3β) with IC50 values of 10.0 and 9.0 nM in mobility shift assays, respectively.
