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 (260)
Recombinant Proteins (4)
Antibodies (9)
GSK-3 Signaling Pathway
GSK-3 Isoform Comparison

By Effects:	Inhibitors (215) Degraders (2) Activators (21) Modulators (2) Chemicals (2)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

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.

HY-117739

BRD1652	Inhibitor
BRD1652 is a highly selective GSK3 inhibitor. BRD1652 can be used in the study of emotion-related diseases.

HY-W267446

6-Methoxy-4-methylcoumarin	Activator	99.00%
6-Methoxy-4-methylcoumarin is a 4-methylcoumarin derivative with an antitumor activity. 6-Methoxy-4-methylcoumarin activates melanin synthesis in B16F10 melanoma cells. 6-Methoxy-4-methylcoumarin is a pigmentation stimulator, and can be used for the study of skin conditions such as vitiligo.

HY-40294R

Indazole (Standard)	Inhibitor
Indazole (Standard) is the analytical standard of Indazole. This product is intended for research and analytical applications. Indazole, also called isoindazole, a heterocyclic aromatic organic compound. Its derivatives display a broad variety of biological activities including anti-inflammatory, antibacterial, anti-HIV, antiarrhythmic, antifungal and antitumour properties. Indazole and its derivatives can be used for research of cancer, neurological disorders, cardiovascular diseases, gastrointestinal diseases.

HY-133102

Dihydronarwedine	Inhibitor
Dihydronarwedine (Lycoraminone) is the alkaloid. Dihydronarwedine inhibits 39% activity of glycogen synthase kinase-3β (GSK-3β) at a concentration of 10 μM.

HY-171031

TFGF-18	Inhibitor
TFGF-18 is a GSK-3β inhibitor (IC₅₀: 0.59 μM). TFGF-18 inhibits LPS-induced microglia activation and proinflammatory mediators release via inhibiting GSK-3β and downstream p65/NF-κB signaling. TFGF-18 inhibits neuronal apoptosis and oxidative stress, inhibits expressions of Bax, caspase3 and cleaved-caspase3 and increases the expression of Bcl-2. TFGF-18 has neuroprotection effect, inhibit neuroinflammation and attenuates cognitive impairment.

HY-B0712AR

Ceftriaxone sodium hydrate (Standard)	Inhibitor
Ceftriaxone (sodium hydrate) (Standard) is the analytical standard of Ceftriaxone (sodium hydrate). This product is intended for research and analytical applications. Ceftriaxone sodium hydrate (Ro 13-9904 sodium hydrate) 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 sodium hydrate is a covalent inhibitor of GSK3β with IC₅₀ value of 0.78 μM. Ceftriaxone sodium hydrate is an inhibitor of Aurora B. Ceftriaxone sodium hydrate has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone sodium hydrate can be used in the study of bacterial infections and meningitis.

HY-126201

GSK-3 inhibitor 7	Inhibitor
GSK-3 inhibitor 7 (compound 22) is a glycogen synthase kinase-3 (GSK-3) inhibitor. GSK-3 inhibitor 7 can be used in nervous system research.

HY-B1014R

Acenocoumarol (Standard)	Activator
Acenocoumarol (Standard) is the analytical standard of Acenocoumarol. This product is intended for research and analytical applications. 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.

HY-W014901S1

Bisphenol F-¹³C₁₂	Activator
Bisphenol 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).

HY-112394

2-Cyanoethylalsterpaullone	Inhibitor
2-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).

HY-12292R

IM-12 (Standard)	Inhibitor
IM-12 (Standard) is the analytical standard of IM-12. This product is intended for research and analytical applications. IM-12 is an inhibitor of GSK-3β, with an IC50 of 53 nM, and also enhances Wnt signalling.

HY-13867AR

Bisindolylmaleimide I hydrochloride (Standard)
Bisindolylmaleimide I (hydrochloride) (Standard) is the analytical standard of Bisindolylmaleimide I (hydrochloride). This product is intended for research and analytical applications. Bisindolylmaleimide I (GF109203X) hydrochloride is a cell-permeable and reversible PKC inhibitor (IC50 of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ. Bisindolylmaleimide I hydrochloride is also a GSK-3 inhibitor.

HY-W014901R

Bisphenol F (Standard)	Activator
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).

HY-N0721R

Neoandrographolide (Standard)	Inhibitor
Neoandrographolide (Standard) is the analytical standard of Neoandrographolide. This product is intended for research and analytical applications. Neoandrographolide is a diterpenoid compound isolated from Andrographis paniculata. Neoandrographolide inhibits osteoclasts differentiation and bone resorption through inhibition of MAPK/NF-κB/PI3K/AKT/GSK3β/PPAR/CAMK signaling pathway. Neoandrographolide inhibits apoptosis in rat embryonic ventricular cardiomyocytes. Neoandrographolide inhibits iNOS and the generation of ROS, activates eNOS, exhibiting anti-inflammatory and hypolipidemic activity.

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 (260)

Recombinant Proteins (4)

Antibodies (9)

GSK-3 Signaling Pathway

GSK-3 Isoform Comparison

GSK-3 Related Products (260):