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 (210)
Recombinant Proteins (4)
Antibodies (9)
GSK-3 Signaling Pathway
GSK-3 Isoform Comparison

By Effects:	Inhibitors (178) Degraders (2) Activators (11) Modulators (2) Chemicals (2)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-137976

Penehyclidine hydrochloride	Activator	99.2%
Penehyclidine (Penequinine) hydrochloride, a anticholinergic agent, is a selective antagonist of M1 and M3 receptors. Penehyclidine hydrochloride activates NF-kβ in lung tissue and inhibits the release of inflammatory factors. Penehyclidine hydrochloride can alleviate the pulmonary inflammatory response in rats with chronic obstructive pulmonary disease (COPD) undergoing mechanical ventilation.

HY-134393B

6-Me-ATP (trisodium) solution (100mM)	Chemical	99.89%
6-Me-ATP (N6-Methyl-ATP) trisodium solution (100mM) is a N⁶-modified ATP derivative. 6-Me-ATP trisodium shows excellent binding affinity to GSK3, serving as the phosphate group donor for GSK3β-catalyzed phosphorylation of its substrate peptide.

HY-112392

GSK-3 Inhibitor XIII	Inhibitor	98.61%
GSK-3 Inhibitor XIII is a potent and ATP-competitive GSK-3 inhibitor with a K_i of 24 nM.

HY-100950

ABC1183	Inhibitor	99.19%
ABC1183 is an orally active selective dual GSK3 and CDK9 inhibitor. ABC1183 inhibits GSK3β, GSK3α and CDK9/cyclin T1 with the IC₅₀ values of 657 nM, 327 nM and 321 nM, respectively. ABC1183 has anti-inflammatory and anti-tumor activities.

HY-N3181

Nodosin	Inhibitor	99.64%
Nodosin is an orally active diterpenoid compound that can be isolated from Isodon serra. Nodosin can inhibit the proliferation and induce cell cycle arrest and apoptosis of tumor cells. Nodosin can also inhibit oxidative stress, inflammatory responses, and ferroptosis. Nodosin has anti-inflammatory and anti-tumor activities.

HY-B0712A

Ceftriaxone sodium hydrate	Inhibitor	99.25%
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-141480

GSK-3β inhibitor 3	Inhibitor	99.22%
GSK-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.

HY-122665

HTH-01-091	Inhibitor	98.64%
HTH-01-091 is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor, with an IC₅₀ of 10.5 nM. HTH-01-091 also inhibits PIM1/2/3, RIPK2, DYRK3, smMLCK and CLK2. HTH-01-091 can be uesd for breast cancer research.

HY-126144

GSK-3β inhibitor 1	Inhibitor	98.04%
GSK-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.

HY-112388

GSK-3b Inhibitor XI	Inhibitor	99.10%
GSK-3b Inhibitor XI (Compound 33) is a potent and selective GSK3β inhibitor, with a K_i value of 25 nM. GSK-3b Inhibitor XI increases glycogen synthase (GS) activity. GSK-3b Inhibitor XI can be used for research on type 2 diabetes and Alzheimer’s disease.

HY-153166

PT-65	Degrader	98.4%
PT-65 is a potent and selective GSK3 PROTAC degrader with the highest degradation capacity of GSK3α (DC₅₀= 28.3 nM) and GSK3β (DC₅₀= 34.2 nM) in SH-SY5Y cells. PT-65 can be used in Alzheimer's disease research.(Pink: GSK3 inhibitor (HY-15761); Black: linker; Blue: CRBN Ligand (HY-10984))

HY-149845

PROTAC GSK-3β Degrader-1	Degrader	98.16%
PROTAC GSK-3β Degrader-1 (compound 1) is a degrader targets GSK-3β degradation with an IC₅₀ value of 833 nM. PROTAC GSK-3β Degrader-1 contains SB-216763 (a GSK-3β inhibitor), a PEG linker and a CRBN (E3 ligase liand). PROTAC GSK-3β Degrader-1 reduces the neurotoxicity induced by Aβ_25-35 peptide and CuSO₄. PROTAC GSK-3β Degrader-1 can be used to research in Alzheimer's disease.

HY-121035

7BIO	Inhibitor	99.20%
7BIO (7-Bromoindirubin-3-Oxime) is the derivate of indirubin. 7BIO (7-Bromoindirubin-3-Oxime) has inhibitory effects against cyclin-dependent kinase-5 (CDK5) and glycogen synthase kinase-3β (GSK3β). 7BIO (7-Bromoindirubin-3-Oxime) inhibits Aβ oligomer-induced neuroinflammation, synaptic impairments, tau hyper-phosphorylation, activation of astrocytes and microglia, and attenuates Aβ oligomer-induced cognitive impairments in mice^[1].

HY-14679

GSK3β inhibitor II	Inhibitor	99.76%
GSK3β inhibitor II is an inhibitor of GSK3β. GSK3β inhibitor II can be used for research of Alzheimer’s disease (AD).

HY-111055

BIP-135	Inhibitor	99.86%
BIP-135 is a potent and selective ATP-competitive GSK-3 inhibitor, with IC₅₀s of 16 nM and 21 nM for GSK-3α and GSK-3β, respectively. BIP 135 exhibits neuroprotective effect.

HY-147134

GSK-3β inhibitor 10	Inhibitor	98.04%
GSK-3β inhibitor 10 (compound 14a) is a highly potent GSK-3β inhibitor with an IC₅₀ value of 80.5 nM. GSK-3β inhibitor 10 can be used for researching Alzheimer’s disease.

HY-N12625

(R)-(+)-O-Demethylbuchenavianine	Inhibitor	98.67%
(R)-(+)-O-Demethylbuchenavianine is an inhibitor for Cyclin-dependent kinases (CDK). (R)-(+)-O-Demethylbuchenavianine inhibits CDK1, CDK5, glycogen synthase kinase-3 (GSK3), cdc2-like kinase (CLK1) and dual specificity tyrosine-phosphorylation-regulated kinase 1A (DYRK1A), with IC₅₀s of 1.1, 0.95, >10, >10 and >10 μM, respectively.

HY-Q48328

GSK3-IN-1	Inhibitor	99.86%
GSK3-IN-1 (compound 11) is a GSK-3 inhibitor with an IC₅₀ value of 12 μM. GSK3-IN-1 can be used in the research of diabetes.

HY-103381

NSC693868	Inhibitor	≥99.0%
NSC693868 is a selective inhibitor of CDK1 and CDK5 with IC₅₀s of 600 nM and 400 nM, respectively. NSC693868 less potently inhibits GSK3β with an IC₅₀ of 1 µM) and does not block CDC25 activity. NSC693868 is used to help define the roles of CDK1 and CDK5 in various signaling pathways.

HY-134622

GSK-3/CDK5/CDK2-IN-1	Inhibitor	98.10%
GSK-3/CDK5/CDK2-IN-1, an imidazole derivative, is an inhibitor of cdk5, cdk2, and GSK-3 extracted from patent WO2002010141A1, example 9a. GSK-3/CDK5/CDK2-IN-1 can be used for the research of cancer, and neurodegenerative diseases.

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 (210)

Recombinant Proteins (4)

Antibodies (9)

GSK-3 Signaling Pathway

GSK-3 Isoform Comparison

GSK-3 Related Products (210):