Catalog No.
Product Name
Application
Product Information
Citations
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GSK-3 inhibitor
AR-A 014418 is a selective glycogen synthase kinase 3 (GSK-3) inhibitor (IC50 = 104 nM). Exhibits specificity for GSK-3 over cdk2 and cdk5 (IC50 values are > 100 μM) and over 26 other kinases. Inhibits β-amyloid-mediated neurodegeneration in hippocampal slices.- Chia-Hui Huang, .et al. , Toxicol Appl Pharmacol, 2020, Apr 17;397:115013 PMID: 32305283
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GSK-3 Inhibitor
CHIR99021 is an aminopyrimidine derivative that inhibits GSK3α and GSK3β with IC50 values of 10 and 6.7 nM, respectively.- Peilin Li, .et al. , Ecotoxicol Environ Saf, 2024, Dec:288:117330 PMID: 39571255
- Peilin Li, .et al. , Stem Cell Res Ther, 2024, Aug 26;15(1):269 PMID: 39183353
- Andreea Manole, .et al. , Cell Rep, 2023, Dec 26;42(12):113466 PMID: 38039131
- Claudia Z Han, .et al. , Immunity, 2023, Sep 12;56(9):2152-2171 PMID: 37582369
- Eric Lian, .et al. , STAR Protoc, 2023, May 22;4(2):102314 PMID: 37220001
- Tomoki Murata, .et al. , Int Immunol, 2023, Apr 13 PMID: 37052267
- Shunsuke Murakami, .et al. , Regen Ther, 2022, Nov 25;21:574-583 PMID: 36475025
- Adam Pietrobon, .et al. , Cell Rep, 2022, Jul 5;40(1):111048 PMID: 35793620
- Takayuki Miyoshi, .et al. , J Gastroenterol, 2022, Jun;57(6):441-452 PMID: 35294680
- Tomoki Kamatani, .et al. , Inflamm Regen, 2022, Feb 2;42(1):4 PMID: 35105370
- Dan Zhao, .et al. , Poult Sci, 2022, Mar; 101(3): 101642 PMID: 35016046
- Otsuka R, .et al. , Sci Rep, 2020, Jan 14;10(1):224 PMID: 31937817
- Yu Huang, .et al. , Stem Cells Int, 2019, 2019: 3975689 PMID: 31565060
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GSK3 inhibitor
AZD1080 is a novel GSK3 inhibitor, rescues synaptic plasticity deficits in rodent brain and exhibits peripheral target engagement in humans.- Shengzhong Liu, .et al. , J Cell Biochem, 2019, 2019 PMID: 30887575
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GSK-3 Inhibitor
Tideglusib is a GSK-3 inhibitor currently in phase II clinical trials for the treatment of Alzheimer disease and progressive supranuclear palsy- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
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GSK-3 inhibitor
LY2090314 is a potent inhibitor of glycogen synthase kinase-3 (GSK-3) which plays an important role in many pathways, including initiation of protein synthesis, cell proliferation, cell differentiation, and apoptosis.- Yuki Shimizu, .et al. , NPJ Precis Oncol, 2022, Mar 17;6(1):16 PMID: 35301419
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GSK-3 inhibitor
CHIR-98014 is a very potent, selective, cell-permeable reversible inhibitor of GSK-3. -
CDK Inhibitor
Aloisine A is a potent cyclin-dependent kinase (CDK) inhibitor, exhibiting IC50 values of 0.15 μM for CDK1/cyclin B, 0.12 μM for CDK2/cyclin A, 0.4 μM for CDK2/cyclin E, and 0.16 μM for CDK5/p35. In addition to its CDK inhibitory effects, Aloisine A also inhibits GSK-3α and GSK-3β with IC50 values of 0.5 μM and 1.5 μM, respectively. Notably, it enhances the activity of wild-type and mutant CFTR with submicromolar affinity through a cAMP-independent mechanism, making it a valuable tool for research related to cystic fibrosis and CFTR-related disorders. -
CDK Inhibitor
NSC693868 is a selective inhibitor of cyclin-dependent kinases CDK1 and CDK5, demonstrating IC50 values of 600 nM and 400 nM, respectively. This compound also exhibits weaker inhibition of GSK3β with an IC50 of 1 µM and does not affect CDC25 activity. NSC693868 is employed in research to elucidate the functions of CDK1 and CDK5 within various cellular signaling pathways. -
GSK-3α/β Inhibitor
(E/Z)-BIO-acetoxime is a potent and selective inhibitor of GSK-3α/β, exhibiting an IC50 of 10 nM. This compound demonstrates exceptional selectivity with over 200-fold preference against CDK5/p25, CDK2/cyclin A, and CDK1/cyclin B, with IC50 values of 2.4, 4.3, and 63 μM, respectively. Its strong inhibitory activity makes it a valuable tool for research focused on signaling pathways involved in cell proliferation, differentiation, and apoptosis. -
Anticholinergic agent
Penehyclidine hydrochloride (also known as Penequinine hydrochloride) is a selective anticholinergic agent that acts as an antagonist of muscarinic M1 and M3 receptors. It exerts anti-inflammatory effects by modulating immune signaling in lung tissue, notably through activation of the NF-κB pathway and inhibition of pro-inflammatory cytokine release. In preclinical studies, Penehyclidine hydrochloride has been shown to alleviate pulmonary inflammation in rat models of chronic obstructive pulmonary disease (COPD), particularly under conditions of mechanical ventilation. These properties suggest its potential utility in managing respiratory inflammatory conditions and improving outcomes in mechanically ventilated patients with COPD. -
GSK-3β/G9a Inhibitor
GSK-3β/G9a-IN-1 is a selective inhibitor of GSK-3β and G9a, acting through competitive mechanisms with IC50 values of 0.8 μM and 1.1 μM, respectively. This compound is effective in lowering tau phosphorylation and reducing Aβ aggregation, making it relevant for Alzheimer's disease research. Additionally, GSK-3β/G9a-IN-1 influences chromatin dynamics by inhibiting H3K9me2 and modulating members of the SAGA complex. Its ability to improve memory and restore social behaviors highlights its potential as a therapeutic agent in neurodegenerative conditions. -
CDK/GSK3β/JNK Inhibitor
Indirubin-3′-oxime (IDR3O) is a synthetic derivative of indirubin that functions as a potent inhibitor of cyclin-dependent kinases (CDKs), glycogen synthase kinase 3β (GSK3β), and all three isoforms of c-Jun N-terminal kinases (JNK1, JNK2, JNK3). It demonstrates inhibitory activity with IC50 values of 0.8 μM, 1.4 μM, and 1.0 μM for each JNK isoform, respectively. Indirubin-3′-oxime is also known to promote chondrocyte height growth through the activation of Wnt/β-catenin signaling, making it relevant for studies in cellular growth and differentiation. -
GSK-3β Inhibitor
GSK-3β inhibitor 13 is a potent inhibitor of glycogen synthase kinase 3 beta (GSK-3β) and GSK-3α, demonstrating IC50 values of 0.73 nM and 0.35 nM respectively. This orally active compound exhibits blood-brain barrier permeability and effectively reduces tau phosphorylation, with an IC50 of 58 nM. Its ability to modulate tau phosphorylation makes it valuable for research focused on neurodegenerative disorders, particularly Alzheimer's disease, by potentially mitigating the formation of neurofibrillary tangles. -
CDK2/GSK3β Inhibitor
Tagtociclib hydrate is a potent and selective inhibitor of cyclin-dependent kinase 2 (CDK2) and glycogen synthase kinase 3 beta (GSK3β), displaying inhibition constants of 1.16 nM and 537.81 nM, respectively. This compound demonstrates significant anti-tumor activity, particularly in cancers characterized by cyclin E1 amplification. Tagtociclib hydrate serves as a valuable research tool for studying cell cycle regulation and therapeutic strategies targeting kinase pathways in cancer biology. -
GSK-3β Inhibitor
GSK-3β Inhibitor 2 is a selective and potent inhibitor of glycogen synthase kinase 3 beta (GSK-3β) with an IC50 of 1.1 nM. This compound is orally active and is capable of penetrating the blood-brain barrier, making it a valuable tool for neurological research. GSK-3β Inhibitor 2 holds potential for therapeutic applications in Alzheimer's disease and other neurodegenerative conditions by modulating signaling pathways associated with neuronal survival and function. -
β-catenin/GSK-3β Activator
C-Peptide 1 (rat) is a peptide that functions as an activator of β-catenin and GSK-3β. Its primary mechanism involves the regulation of the Wnt/β-catenin signaling pathway, which plays a crucial role in cellular processes such as proliferation and differentiation. C-Peptide 1 (rat) is utilized in cancer research, contributing to studies aimed at understanding tumorigenesis and potential therapeutic interventions. -
PROTAC GSK-3β Degrader
PROTAC GSK-3β Degrader-1 is a targeted GSK-3β degrader that induces the proteasomal degradation of GSK-3β with an IC50 value of 833 nM. This compound integrates SB-216763, a known GSK-3β inhibitor, a PEG linker, and a CRBN ligand to facilitate E3 ligase-mediated degradation. It has demonstrated efficacy in reducing neurotoxicity induced by Aβ25-35 peptide and CuSO4, making it a valuable tool for researching Alzheimer's disease mechanisms and potential therapeutic interventions. -
GSK-3 Inhibitor
PF-04802367 is a highly selective glycogen synthase kinase 3 (GSK-3) inhibitor, demonstrating an IC50 of 2.1 nM in recombinant human GSK-3β assays and 1.1 nM in ADP-Glo assays. This compound effectively inhibits both GSK-3 isoforms, GSK-3α and GSK-3β, with IC50 values of 10.0 nM and 9.0 nM, respectively, as measured by mobility shift assays. PF-04802367 is distinguished by its favorable central nervous system (CNS) properties, making it a valuable tool in neurobiological research and related therapeutic investigations. -
GSK3α/GSK3β PROTAC Degrader
PT-65 is a PROTAC degrader targeting GSK3α and GSK3β, exhibiting DC50 values of 28.3 nM and 34.2 nM, respectively. This compound effectively inhibits excessive tau phosphorylation induced by GSK3β, amyloid-beta, and okadaic acid. PT-65 is a valuable tool for research into the pathophysiology of Alzheimer's disease, allowing for further investigation into tau-related mechanisms and potential therapeutic interventions. -
GSK3β/AβOs Inhibitor
Cu(II)GTSM is a cell-permeable copper complex that acts as a potent inhibitor of glycogen synthase kinase 3 beta (GSK3β). This compound significantly reduces the formation of amyloid-beta oligomers (AβOs) and lowers tau phosphorylation levels, thereby influencing key pathways related to neurodegenerative diseases. Additionally, Cu(II)GTSM diminishes the abundance of amyloid-beta trimers and exhibits potential as an anticancer and antimicrobial agent, making it valuable for various research applications in disease modeling and therapeutic development. -
GSK3β Inhibitor
BRD3731 is a selective inhibitor of glycogen synthase kinase 3 beta (GSK3β), demonstrating an IC50 of 15 nM for GSK3β and 215 nM for GSK3α. This compound exhibits significant potential in research related to post-traumatic stress disorder (PTSD), various psychiatric disorders, diabetes, and neurodegenerative diseases. Its specificity and potency make it a valuable tool for studying GSK3β-related signaling pathways and therapeutic interventions. -
CDKL5/GSK3 Inhibitor
SGC-CDKL5/GSK3 is a selective inhibitor targeting CDKL5 and GSK3α/β. This compound demonstrates potent inhibition, with IC50 values of 4.6 nM for CDKL5, 24 nM for GSK3β, and 9.5 nM for GSK3α, as assessed by the NanoBRET assay. Its specificity and efficacy make it a valuable tool for investigating central nervous system diseases and related biological pathways. -
GSK-3β Inhibitor
GSK-3β inhibitor 22 is a potent inhibitor of glycogen synthase kinase 3 beta (GSK-3β) with an IC50 of 3.1 nM. This compound is suitable for research applications focused on neurodegenerative diseases, particularly Alzheimer's disease. It provides a valuable tool for investigating the role of GSK-3β in cellular pathways and potential therapeutic interventions in related pathologies. -
GSK3α/β Inhibitor
BRD0209 is a potent and selective dual inhibitor of glycogen synthase kinase 3 alpha and beta (GSK3α/β), exhibiting IC50 values of 19 nM and 5 nM, respectively. This reversible ATP-competitive inhibitor demonstrates fast-off kinetics with a Ki of 4.2 nM. As a tricyclic pyrazolotetrahydroquinolinone compound, BRD0209 is primarily utilized in the investigation of mood disorders and related neurobiological research. -
GSK-3 Inhibitor
GSK-3 Inhibitor 3 is a selective inhibitor targeting glycogen synthase kinase 3 (GSK-3) with notable brain penetration. It exhibits low nanomolar potency, with IC50 values of 0.35 nM for GSK-3α and 0.25 nM for GSK-3β. This compound effectively reduces tau protein phosphorylation at the S396 site in a triple-transgenic mouse model of Alzheimer's disease, demonstrating an IC50 of 10 nM. GSK-3 Inhibitor 3 is valuable for research into neurological diseases and related signaling pathways. -
GSK3 Inhibitor
CHIR 98024 is a potent glycogen synthase kinase 3 (GSK3) inhibitor with an EC50 of 0.2566 μM. This compound modulates various signaling pathways, contributing to cellular processes such as proliferation, differentiation, and metabolism. CHIR 98024 is utilized in research exploring its therapeutic potential in neurodegenerative diseases, cancer, and other disorders associated with GSK3 dysregulation. -
GSK3β Inhibitor
GSK-3β Inhibitor XI is a selective inhibitor of glycogen synthase kinase 3 beta (GSK-3β) with a potent Ki value of 25 nM. This compound enhances glycogen synthase (GS) activity, making it valuable for investigations into metabolic disorders such as type 2 diabetes and neurodegenerative diseases, including Alzheimer’s disease. Its specificity and potency render it a useful tool for elucidating the role of GSK-3β in various biological processes and therapeutic contexts. -
GSK-3
GSK3-IN-7 is a selective inhibitor of glycogen synthase kinase 3 (GSK-3). This small molecule exhibits potent GSK-3 inhibition, which is critical for modulating cellular signaling pathways involved in glucose metabolism and neurodegenerative diseases. GSK3-IN-7 is utilized in research applications focused on the development of therapeutic strategies for conditions such as diabetes, Alzheimer's disease, and cancer. -
GSK3 Inhibitor
SAR502250 is a potent and selective ATP-competitive inhibitor of glycogen synthase kinase 3 (GSK3) with an IC50 of 12 nM for human GSK-3β. This compound is orally active and exhibits the ability to penetrate the blood-brain barrier. SAR502250 demonstrates antidepressant-like activity and is applicable for research into Alzheimer's disease and related neurological conditions. -
GSK3/CDK9 Inhibitor
ABC1183 is a selective dual inhibitor targeting GSK3 and CDK9, effectively inhibiting GSK3β, GSK3α, and CDK9/cyclin T1 with IC50 values of 657 nM, 327 nM, and 321 nM, respectively. This compound exhibits notable anti-inflammatory and anti-tumor activities, making it a valuable tool for cancer research and inflammation-related studies. Its ability to modulate critical signaling pathways positions ABC1183 as a promising candidate for further investigation in therapeutic applications. -
GSK-3 Inhibitor
GSK3-IN-1 is a selective inhibitor of glycogen synthase kinase 3 (GSK-3) with an IC50 value of 12 μM. This compound is involved in various signaling pathways and plays a critical role in glucose metabolism and insulin signaling. GSK3-IN-1 is particularly relevant for research applications focused on diabetes and other metabolic disorders. -
GSK3β Inhibitor
GSK3β Inhibitor II is a selective inhibitor targeting glycogen synthase kinase 3 beta (GSK3β). This compound exhibits significant activity in modulating GSK3β activity, making it a valuable tool for studying signaling pathways implicated in neurodegenerative diseases such as Alzheimer’s disease. Its use facilitates research aimed at elucidating the roles of GSK3β in cellular processes and potential therapeutic strategies for AD. -
GSK-3/CDK5/CDK2 Inhibitor
GSK-3/CDK5/CDK2-IN-1 is a potent inhibitor targeting GSK-3, CDK5, and CDK2. This imidazole derivative has demonstrated effectiveness in modulating pathways relevant to tumorigenesis and neurodegenerative disorders. Its ability to inhibit these kinases makes it a valuable tool for investigating mechanisms underlying cancer proliferation and neurodegeneration. -
GSK-3β Inhibitor
(E/Z)-GSK-3β inhibitor 1 is a racemic mixture comprising both (E)- and (Z)-isomers targeting glycogen synthase kinase 3β (GSK-3β). This compound exhibits significant antidiabetic activity, with an IC50 value of 4.9 nM, making it a valuable tool for studying pathways related to glucose metabolism and insulin signaling. Its inhibition of GSK-3β provides insights into potential therapeutic strategies for diabetes and related metabolic disorders. -
GSK-3 Inhibitor
L803-mts is a selective, substrate-competitive inhibitor of glycogen synthase kinase 3 (GSK-3) with an IC50 of 40 μM. This compound has been shown to significantly reduce amyloid-beta (Aβ) deposits and improve cognitive deficits in the 5XFAD mouse model of Alzheimer's disease. Additionally, L803-mts exhibits antidepressant-like effects, as demonstrated in the forced swimming test, making it a valuable tool for studying neurodegenerative and mood disorders. -
GSK-3β Inhibitor
GSK-3β inhibitor 8 is a selective inhibitor of glycogen synthase kinase 3 beta (GSK-3β) with an IC50 value of 64 nM. This thiophenacil derivative targets the Wnt signaling pathway, leading to its negative regulation and promoting β-cell proliferation. GSK-3β inhibitor 8 is valuable for research involving cell signaling, diabetes, and regenerative medicine applications. -
GSK-3β Inhibitor
COB-187 is a selective and potent ATP-competitive inhibitor of Glycogen Synthase Kinase 3 beta (GSK-3β). This compound operates through a reversible mechanism dependent on Cysteine (Cys)-199, effectively inhibiting GSK-3β activity. COB-187 is shown to reduce cytokine production induced by lipopolysaccharides (LPS) and decreases CXCL10 production triggered by SARS-CoV-2 spike protein, making it relevant for research in inflammation and viral response studies. -
GSK-3 Inhibitor
GSK-3 Inhibitor XIII is a potent ATP-competitive inhibitor of glycogen synthase kinase 3 (GSK-3), exhibiting a Ki value of 24 nM. It effectively modulates GSK-3 activity, making it a valuable tool for studying various biological processes, including cell growth, differentiation, and metabolism. This inhibitor is particularly relevant for research in cancer, neurodegenerative diseases, and diabetes, as it plays a critical role in signaling pathways associated with these conditions. -
GSK-3β Inhibitor
TCS2002 is a potent and selective inhibitor of GSK-3β, demonstrating an IC50 of 35 nM. This compound exhibits favorable pharmacokinetic properties, including efficient blood-brain barrier penetration. TCS2002 is valuable for research related to Alzheimer’s disease and the investigation of associated neurodegenerative mechanisms. -
GSK-3 Inhibitor
BIP-135 is a selective ATP-competitive inhibitor of glycogen synthase kinase 3 (GSK-3) with IC50 values of 16 nM for GSK-3α and 21 nM for GSK-3β. This compound demonstrates neuroprotective effects, making it a valuable tool in research focused on neurodegenerative diseases and related pathways. Its specificity and potency position BIP-135 as a significant reagent for studying GSK-3-related biological processes. -
GSK-3/CDK2/CDK5 Inhibitor
GSK-3 Inhibitor 4 is a potent inhibitor of Glycogen Synthase Kinase 3 (GSK-3), Cyclin-Dependent Kinase 2 (CDK2), and Cyclin-Dependent Kinase 5 (CDK5), demonstrating IC50 values of 0.56 nM for GSK-3β, 0.45 nM for GSK-3α, 0.47 μM for CDK2, and 0.68 μM for CDK5. This compound effectively attenuates the phosphorylation of Tau protein, making it a valuable tool for investigating mechanisms underlying Alzheimer's disease. Its oral bioavailability and ability to penetrate the blood-brain barrier further enhance its utility in neuropharmacological research. -
GSK-3β Inhibitor
GSK-3β inhibitor 10 is a potent inhibitor of glycogen synthase kinase 3 beta (GSK-3β) with an IC50 value of 80.5 nM. This compound is valuable for studies investigating the role of GSK-3β in various neurodegenerative disorders, particularly Alzheimer’s disease. Its inhibitory action on GSK-3β may contribute to understanding the molecular mechanisms underlying these conditions and aid in the development of targeted therapeutic strategies. -
GSK-3
5-Bromo-3-indoxylacetate is a potent inhibitor of glycogen synthase kinase 3 (GSK-3) with a reported pIC50 of 3.39. This compound exhibits significant biological activity, making it a valuable tool for research focused on signal transduction pathways involved in various diseases, including cancer and neurodegenerative disorders. Its inhibitory effects on GSK-3 can be utilized to explore cellular processes such as glycogen metabolism, cell differentiation, and proliferation. -
GSK3 Inhibitor
(R)-BRD3731 is a selective glycogen synthase kinase 3 (GSK3) inhibitor. It demonstrates inhibitory activity with IC50 values of 1.05 μM for GSK3β and 6.7 μM for GSK3α. This compound is utilized in research focused on understanding GSK3's role in various cellular processes and diseases, including diabetes, neurodegenerative disorders, and cancer. As a valuable tool for studying GSK3 modulation, (R)-BRD3731 facilitates the exploration of therapeutic strategies that target this kinase. -
GSK-3β Inhibitor
GSK-3β Inhibitor 11 is a specific inhibitor of glycogen synthase kinase-3β (GSK-3β) with an IC50 value of 10.02 μM. This compound plays a significant role in modulating signaling pathways involved in neurodegenerative diseases, making it a valuable tool for research in this area. Its ability to selectively inhibit GSK-3β enables investigations into its potential therapeutic effects on associated pathological mechanisms.
