GSK-3

Glycogen synthase kinase-3; Glycogen synthase kinase 3

GSK-3

GSK-3 Isoform Specific Products:

GSK-3 Isoform Comparison

GSK-3 Related Products (252)
Recombinant Proteins (4)
Antibodies (9)
GSK-3 Signaling Pathway
GSK-3 Isoform Comparison

By Effects:	Inhibitors (208) Degraders (2) Activators (20) Modulators (2) Chemicals (2)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-172599

GSK-3β probe-1
GSK-3β probe-1 (10c) is a GSK-3β probe (Ex = 341 nm, Em= 574nm, ɛ= 3.51 × 10⁴L/mol·cm⁻¹) and can be be used in the study of Alzheimer's disease.

HY-174398

GSK-3β/HDAC-IN-2	Inhibitor
GSK-3β/HDAC-IN-2 is a potent inhibitor of GSK-3β (IC₅₀ = 0.04 μM), HDAC2 (IC₅₀ = 1.05 μM, Ki = 0.070 μM) and HDAC6 (IC₅₀ = 1.52 μM, Ki = 0.017 μM). GSK-3β/HDAC-IN-2 inhibits HDAC2 and HDAC6 activities and blocks tau hyperphosphorylation. GSK-3β/HDAC-IN-2 exerts neuroprotective effects and shows no significant toxicity. GSK-3β/HDAC-IN-2 can be used in the research of Alzheimer's disease.

HY-P10971

Nef-M1	Activator
Nef-M1 (Nef-Motif-1) is an antagonist peptide targeting CXCR4 and an apoptosis inducer derived from a myristoylated protein encoded by the nef gene in HIV. Nef-M1 inhibits tumor angiogenesis and epithelial-mesenchymal transition (EMT). Nef-M1 activates the apoptosis pathway by increasing the level of caspase-3 in cancer cells. Nef-M1 simultaneously inhibits VEGF-A, p-GSK-3β and vimentin, and enhances E-cadherin, thereby inhibiting angiogenesis and EMT processes. Nef-M1 can be used in the study of colorectal cancer and breast cancer.

HY-117194

18BIOder	Inhibitor
18BIOder is a neuroprotective GSK-3β inhibitor, highly selectively inhibiting HIV-1.

HY-168857

GSK-3β inhibitor 24	Inhibitor
GSK-3β inhibitor 24 (Compound 41) is a potent GSK-3β inhibitor with an IC₅₀ of 0.22 nM. GSK-3β inhibitor 24 increases GSK-3β phosphorylation at Ser9 site dose-dependently. GSK-3β inhibitor 24 inhibits the hyperphosphorylation of tau protein by decreasing the p-tau-Ser396 abundance. GSK-3β inhibitor 24 up-regulates β-catenin and neurogenesis-related markers (GAP43 and MAP-2). GSK-3β inhibitor 24 demonstrates remarkable anti-Alzheimer's disease (AD) effects.

HY-111931

Indirubin-3'-monoxime-5-sulphonic acid	Inhibitor
Indirubin-3'-monoxime-5-sulphonic acid is a potent and selective inhibitor of CDK1, CDK5, and GSK-3β with IC₅₀s of 5 nM, 7 nM, and 80 nM, respectively.

HY-162722

GSK-3 inhibitor 6	Inhibitor
GSK-3 inhibitor 6 (2) is a CNS penetrated GSK-3 inhibitor, with IC₅₀ values of 29 nM and 24 nM for GSK-3α and GSK-3β, respectively.

HY-173395

MAO-B-IN-43	Inhibitor
MAO-B-IN-43 (4) is a potent hMAO-B inhibitor and a weak GSK3β kinase inhibitor, with K_i values of 0.044 μM and 0.004 μM for hMAO-A and hMAO-B, respectively. MAO-B-IN-43 (4) can be used for the research of neurodegenerative disorder.

HY-156032

PIMPC	Inhibitor
PIMPC is a compound with antioxidant and metal-chelating properties. PIMPC is a novel inhibitor of glycogen synthase kinase 3 (GSK-3). PIMPC has potential anti-Alzheimer's disease effect.

HY-B0712R

Ceftriaxone (Standard)	Inhibitor
Ceftriaxone (Standard) is the analytical standard of Ceftriaxone. This product is intended for research and analytical applications. Ceftriaxone (Ro 13-9904 free acid) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone is a covalent inhibitor of GSK3β with IC50 value of 0.78 μM. Ceftriaxone is an inhibitor of Aurora B. Ceftriaxone has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone can be used in the study of bacterial infections and meningitis[1][2][3][4][5][6][7].

HY-112336

Aloisine RP106	Inhibitor
Aloisine RP106 (compound 38) is a potent inhibitor of Cdk1/cyclin B, Cdk5/p25, and GSK3 with IC₅₀s of 0.70µM, 1.5µM, 0.92 µM, respectively.

HY-111932

Indirubin-5-sulfonate	Inhibitor
Indirubin-5-sulfonate is a cyclin-dependent kinase (CDK) inhibitor, with IC₅₀ values of 55 nM, 35 nM, 150 nM, 300 nM and 65 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK4/cyclin D1, and CDK5/p35, respectively. Indirubin-5-sulfonate also shows inhibitory activity against GSK-3β.

HY-151575

PfGSK3/PfPK6-IN-2	Inhibitor
PfGSK3/PfPK6-IN-2 is a potent dual PfGSK3/PfPK6 (Plasmodium falciparum GSK3/PK6) inhibitor (IC₅₀: 172 nM and 11 nM respectively). PfGSK3/PfPK6-IN-2 can be used in the research of Malaria.

HY-153760

GSK-3β inhibitor 14	Inhibitor	99.92%
GSK-3β inhibitor 14 (Compound 6i), benzothiazepinone derivative, is a weak GSK-3β inhibitor (IC₅₀ >100 μM).

HY-144826

ZDWX-25	Inhibitor
ZDWX-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.

HY-162638

GSK-3β inhibitor 18	Inhibitor
GSK-3β inhibitor 18 (compound 2) is a potent inhibitor of GSK-3β, with the IC₅₀ of 0.0021 μM.

HY-P3713

Presenilin 1 (349-361)
Presenilin 1 (349-361) is an active petide, and synthetic peptides representing amino acids 349–361 can be phosphorylated by glycogen synthase kinase-3β(GSK3β) in vitro. Presenilin 1 (349-361) can be used for the research of various diseases.

HY-168859

JNK3 inhibitor-9	Inhibitor
JNK3 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 Aβ_1-42 toxicity.

HY-P1385

TCS 183	Inhibitor
TCS 183, a peptide, is a GSK-3β inhibitor. TCS 183 blocks GSK-3β autoinhibition and decreases the level of AMPK phosphorylation. TCS 183 can be used for neuropathological diseases, particularly Alzheimer’s disease, research.

HY-174923

AZ12943203	Inhibitor
AZ12943203 (Compound 13e) is a GSK-3 PET radioligand with a K_d of 2.94  nM. AZ12943203 has a significant inhibitory potency toward GSK-3β (IC₅₀: 4.44 nM), and can specifically bind to GSK-3-rich regions of the rodent brain. AZ12943203 can be used for neurodegenerative diseases imaging, particularly Alzheimer’s disease.

β-catenin β-catenin β-catenin β-catenin DKK GSK-3 Axin APC CK1 CK1/CK2 GSK-3 Dvl Wnt Wnt Wnt Proteasome Axin Dvl GSK-3 GSK-3 sFRP, WIF-1, Cerberus eIF2B β-TrCP Cadherin β-catenin LGS PYGO TCF/LEF CBP Tiki Insulin/IGF IGF1R Glycogen
Synthase Glycogen Gene
Transcription
Cyclin D1, c-Myc,
Axin2, Brachyury, etc. c-Jun CREB HSF1 C-EBPβ STAT3 NF-κB IRS PI3K PIP2 PIP3 PTEN PDK1 PI3K SOS Grb2 Gas1 SHC Akt Trk receptor NT D2R β-arrestin2 PP2A Akt MAP Kinases BAD BAX 5-HT receptor 5-HT_1A 5-HT₂ MAP1B Apoptosis

Download GSK-3 Signaling Pathway Map.

Glycogen synthase kinase 3 (GSK-3) is a multifunctional serine/threonine kinase found in all eukaryotes. GSK-3 is one of the few signaling mediators that play central roles in a diverse range of signaling pathways, including those activated by Wnt, PI3K, growth factors, cytokines, and ligands for G protein-coupled receptors. The PI3K pathway is known for regulating metabolism, cell growth, and cell survival. The PI3K activity is stimulated by diverse oncogenes and growth factor receptors. PI3K-mediated production of PIP3 leads to the activation of Akt. The activation of Akt leads to the phosphorylation of GSK-3, which is active in resting cells, but is inactivated by the phosphorylation. The GSK-3 has been linked to the regulation of an assembly of transcription factors, including β-catenin, NF-κB, c-Jun, CREB, and STAT. Thus, the altered activity of GSK-3 causes various effects on cytokine expression.

In the absence of Wnt signaling, β-catenin is phosphorylated by CK1 and GSK-3. This phosphorylation leads to recognition by β-TrCP, leading to the ubiquitylation of β-catenin and degradation by the proteasome. Upon binding of a lipid-modified Wnt protein to the receptor complex, a signaling cascade is initiated. LRP is phosphorylated by CK1/CK2 and GSK-3, and Axin is recruited to the plasma membrane. The kinases in the β-catenin destruction complex are inactivated and β-catenin translocates to the nucleus to form an active transcription factor complex with TCF, leading to transcription of a large set of target genes.

Some endogenous growth factors could bind to and activate the tyrosine kinase receptor. This facilitates the recruitment of other proteins (SHC, SOS), which results in the activation of the ERK-MAPK cascade and the inhibition of GSK-3. GSK-3 exerts many cellular effects: it regulates cytoskeletal proteins, and is important in determining cell survival/cell death. GSK-3 has also been identified as a target for the actions of lithium. GSK-3 can inhibit glycogen synthase, the enzyme that catalyzes the transfer of glucose from UDPG to glycogen^[1][2].

Reference:

[1]. Brenner D, et al. Regulation of tumour necrosis factor signalling: live or let die.Nat Rev Immunol. 2015 Jun;15(6):362-74.
[2]. Conrad M, et al. Regulated necrosis: disease relevance and therapeutic opportunities.Nat Rev Drug Discov. 2016 May;15(5):348-66.

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GSK-3

GSK-3

GSK-3 Isoform Specific Products:

GSK-3 Isoform Specific Products:

GSK-3 Related Products (252)

Recombinant Proteins (4)

Antibodies (9)

GSK-3 Signaling Pathway

GSK-3 Isoform Comparison

GSK-3 Related Products (252):