Catalog No.
Product Name
Application
Product Information
Citations
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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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GSK-3 inhibitor
CHIR-98014 is a very potent, selective, cell-permeable reversible inhibitor of GSK-3. -
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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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
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-3β inhibitor
1-Azakenpaullone is a potent and selective GSK-3β inhibitor with IC50 of 18 nM, >100-fold selectivity over CDK1/cyclin B and CDK5/p25. -
GSK-3 inhibitor
BIO-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. -
GSK-3β inhibitor
Indirubin-3'-monoxime is a powerful inhibitor of GSK-3β with IC50 of 22nM, also inhibits CDK1/5 (IC50 = 180/100 nM). -
dual PDE7/GSK-3 inhibitor
VP3.15 is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE)7- glycogen synthase kinase (GSK)3 inhibitor, with IC50s of 1.59 μM and 0.88 μM for PDE7 and GSK-3, respectively. VP3.15 has neuroprotective and neuroreparative activities, thus as potential combined anti-inflammatory and pro-remyelinating therapies for multiple sclerosis (MS). -
GSK-3β inhibitor
GSK-3β inhibitor 1 (compound 3a) is a glycogen synthase kinase 3β (GSK-3β) inhibitor and demonstrates high antidiabetic efficacy, with an IC50 of 4.9 nM. -
CDK1, CDK5, and GSK-3βinhibitor
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. -
GSK-3β, CDK5/P25 and CDK1/cyclin B inhibitor
5-Iodo-indirubin-3'-monoxime is a potent GSK-3β, CDK5/P25 and CDK1/cyclin B inhibitor, competing with ATP for binding to the catalytic site of the kinase, with IC50s of 9, 20 and 25 nM, respectively. -
GSK-3α/β inhibitor
CHIR-99021 monohydrochloride (CT99021 monohydrochloride) is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM; > 500-fold selectivity for GSK-3 versus its closest homologs CDC2 and ERK2, as well as other protein kinases. -
GSK-3α/β inhibitor
CHIR-99021 trihydrochloride (CT99021 trihydrochloride) is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM. -
PDE7/GSK3 inhibitor
VP3.15 dihydrobromide is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE)7- glycogen synthase kinase (GSK)3 inhibitor, with IC50s of 1.59 μM and 0.88 μM for PDE7 and GSK-3, respectively. -
GSK-3 inhibitor
GSK3 Inhibitor XIII (GSK3i XIII) is an ATP-binding site inhibitor of GSK-3. -
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. -
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. -
DYRK1A/GSK3β Inhibitor
GNF4877 is a potent dual inhibitor of DYRK1A and GSK3β, demonstrating IC50 values of 6 nM and 16 nM, respectively. This inhibition results in the blockade of nuclear export of nuclear factor of activated T-cells (NFATc) and promotes β-cell proliferation, with an EC50 of 0.66 μM in mouse β (R7T1) cells. GNF4877 serves as a valuable tool in research related to diabetes and T-cell signaling pathways. -
GSK3 Inhibitor
GSK3-IN-10 is a potent inhibitor of glycogen synthase kinase 3 (GSK3) isoforms α and β, demonstrating IC50 values of 1.0 nM and 2.0 nM, respectively. This compound effectively inhibits the activation of β-catenin, thereby promoting neuronal survival and providing a protective effect against endoplasmic reticulum stress. GSK3-IN-10 is valuable for research applications focused on neuroprotection and cellular stress response mechanisms. -
GSK3β Inhibitor
GSK3β-IN-2 is a potent GSK3β inhibitor with an IC50 of 0.35 nM. This compound activates the Wnt/β-catenin signaling pathway, leading to enhanced neurogenesis and neurite outgrowth. Additionally, GSK3β-IN-2 effectively inhibits Aβ-induced tau hyperphosphorylation at Ser396 and reduces neurofibrillary tangle formation. Its efficacy in ameliorating Alzheimer's disease has been demonstrated in zebrafish models, making it a valuable tool for neurological research. -
GSK-3 Inhibitor
Laduviglusib dihydrochloride is a selective inhibitor of glycogen synthase kinase-3 (GSK-3), an enzyme involved in numerous cellular processes including glycogen synthesis, cell differentiation, and apoptosis. By inhibiting GSK-3, Laduviglusib dihydrochloride promotes cell survival and has been extensively studied in the context of neurodegenerative diseases, diabetes, and cancer research. This compound serves as a valuable tool for elucidating the role of GSK-3 in various signaling pathways and therapeutic applications. -
GSK3β Inhibitor
BRD1172 is a selective inhibitor of glycogen synthase kinase 3 beta (GSK3β), exhibiting an IC50 of 24 nM. This compound effectively inhibits GSK3β-mediated Tau phosphorylation in SH-SY5Y cells and alleviates the negative regulation of GSK3β on β-catenin degradation and TCF/LEF promoter activity. BRD1172 is applicable in research related to Alzheimer’s disease, cardiac hypertrophy, and various cancers. -
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. -
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. -
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. -
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. -
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.
