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GSK-3

Glycogen synthase kinase 3 is a serine/threonine protein kinase that mediates the addition of phosphate molecules onto serine and threonine amino acid residues. First discovered in 1980 as a regulatory kinase for its namesake, Glycogen synthase, GSK-3 has since been identified as a kinase for over 100 different proteins in a variety of different pathways. In mammals GSK-3 is encoded by two paralogous genes, GSK-3 alpha (GSK3A) and GSK-3 beta (GSK3B). GSK-3 has recently been the subject of much research because it has been implicated in a number of diseases, including Type II diabetes (diabetes mellitus type 2), Alzheimer's disease, inflammation, cancer, and bipolar disorder.

  • CHIR-99021
    T2310252917-06-9
    CHIR-99021 (CT99021) is an activator of the Wnt/β-catenin signaling pathway and a GSK-3α/β inhibitor (IC50=10/6.7 nM) with selective and oral activity.CHIR-99021 induces cellular autophagy, which enhances self-renewal in mouse and human embryonic stem cells.
    • $36
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  • GSK-3 Inhibitor XIII
    T78578404828-14-4In house
    GSK-3 Inhibitor XIII, an ATP-competitive GSK-3 inhibitor (Ki: 24 nM), can be used to study diabetes and obesity.
    • $169
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  • GSK3a-IN-38
    T776711062138-03-7
    GSK3a-IN-38 is a novel small molecule compound that has inhibitory effects on GSK-3a.
    • $195
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  • PHA-767491
    T6206845714-00-3
    PHA-767491 (CAY10572) is a potent ATP-competitive dual Cdc7/CDK9 inhibitor with IC50 of 10 nM and 34 nM, respectively.
    • $30
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  • GS87
    T8605919936-70-2
    GS87 is a highly specific inhibitor of GSK3 (glycogen synthase kinase 3) that induces extensive differentiation of AML cells.
    • $133
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  • MBM-55S
    T119612083624-07-9In house
    MBM-55S is an effective inhibitor of Nek2 with an IC50 of 1 nM. MBM-55S indecus cell cycle arrest and apoptosis thereby inhibiting the proliferation of cancer cells. MBM-55S shows antitumor activities.
    • $195
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  • GSK-3 inhibitor 3
    T773422227279-84-5In house
    GSK-3 inhibitor 3 is a selective, orally active, brain-permeable GSK-3 inhibitor that inhibits GSK-3α and GSK-3β with IC50s of 0.35 nM and 0.25 nM, respectively.GSK-3 inhibitor 3 reduces the phosphorylation level of tau protein S396 with an IC50 of 10 nM in a triple transgenic mouse model of Alzheimer's disease. GSK-3 inhibitor 3 reduced the phosphorylation level of tau protein S396 in a triple transgenic mouse model of Alzheimer's disease, with an IC50 of 10 nM.GSK-3 inhibitor 3 can be used for the study of neurological diseases.
    • $195
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  • GSK-3 Inhibitor 5
    T7755420099-89-2
    GSK-3 Inhibitor 5 (4-Cyanophenacyl bromide) is a ketone derivative that is used as an intermediate in pharmaceuticals and organic synthesis, and inhibits glycogen synthase kinase 3 (GSK-3).
    • $29
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  • 4-Chloro-2'-bromoacetophenone
    T8908536-38-9
    4-Chloro-2'-bromoacetophenone against glycogen synthase kinase-3 (GSK-3beta).
    • $50
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  • GSK3-IN-2
    T73270380450-97-5
    GSK3-IN-2 is a potent GSK3 inhibitor for the treatment of diabetes and neurodegenerative diseases.
    • $72
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  • GSK-3 inhibitor 4
    T773412227279-83-4In house
    GSK-3 inhibitor 4 is an orally active and brain-permeable triple inhibitor of GSK-3, CDK2 and CDK5 with inhibitory effects on GSK-3β, GSK-3α, CDK2 and CDK5, with IC50 values of 0.56 nM, 0.45 nM, 0.47 μM, 0.68 μM, respectively.GSK-3 inhibitor 4 can effectively reduce Tau protein levels. GSK-3 inhibitor 4 can effectively reduce the level of Tau protein.GSK-3 inhibitor 4 can be used in the study of Alzheimer's disease.
    • $350
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  • Aloisine B
    T69188496864-14-3In house
    Aloisine B (AloisineB) inhibited cyclin-dependent kinase and glycogen synthase kinase with IC50 values of 0.85 µM and 0.75 µM, respectively. Aloisine B has antiviral activity and can be used to study Alzheimer's, diabetes, HIV and Parkinson's.
    • $350
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  • GSK-3β inhibitor 12
    T60472784170-07-6
    GSK-3β inhibitor 12 is a selective GSK-3β inhibitor.GSK-3β inhibitor 12 inhibits 49.11% of 25 μM GSK-3β activity and 37.11% of 50 μM GSK-3β activity.GSK-3β inhibitor 12 can be used for the study of Parkinson's in the presence of lipopolysaccharide induction.
    • $83
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  • Ceftriaxone Sodium
    T66175958633-51-7
    Ceftriaxone Sodium is a broad-spectrum β-lactam tertiary cephalosporin antibiotic with anti-inflammatory, antitumor, antibacterial, and antioxidant activities.Ceftriaxone Sodium is a covalent GSK3β and Aurora B inhibitor used in the study of sepsis and infective endocarditis.
    • $39
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  • 3F8
    T22180159109-11-2In house
    3F8 is a selective GSK-3β inhibitor that can be used as a new tool and potential therapeutic candidate compound for GSK3-related diseases, and can be used in the study of neurological disorders and cancer.
    • $115
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  • CDK8-IN-12
    T720482613307-67-6In house
    CDK8-IN-12 is a selective, potent and orally active inhibitor of CDK8 (Ki: 14 nM) and is an anti-cancer agent. CDK8-IN-12 inhibits GSK-3α, GSK-3β and PCK-θ with Ki of 13 nM, 4 nM and 109 nM respectively. CDK8-IN-12 showed anti-proliferative activity against MV4-11 cells.
    • $79
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  • GSK3-IN-4
    T64366748145-19-9
    GSK3-IN-4 is a GSK-3 inhibitor with IC50 of 0.101-1 μM of GSK-3α and GSK-3β in Calipe Assay.
    • $117
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  • GSK-3 inhibitor 1
    T11468603272-51-1In house
    GSK-3 inhibitor 1 is a GSK-3 inhibitor.
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  • GSK-3β inhibitor 8
    T355561139875-74-3In house
    GSK-3β inhibitor 8 (GSK3β Inhibitor XVIII) is a potent and selective GSK-3β inhibitor with an IC50 value of 64 nM.GSK-3β inhibitor 8 is a thienopyrimidine derivative that negatively regulates the Wnt signaling pathway and stimulates β-cell proliferation.
    • $110
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  • ARN25068
    T613602649882-80-2In house
    ARN25068 is a potent inhibitor of GSK-3β, FYN, and DYRK1A protein kinases, exerting its activity in the sub-micromolar range. This compound effectively addresses tau hyperphosphorylation [1].
    • $115
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  • 5-Iodo-indirubin-3'-monoxime
    T10172331467-03-9In house
    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 (IC50s: 9, 20 and 25 nM).
    • $297
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  • EHT 1610
    T152041425945-60-3In house
    EHT 1610 (EHT 5372) is a potent inhibitor of DYRK, with an IC50 of 0.36 nM and 0.59 nM for DYRK1A and DYRK1B, respectively. EHT 1610 has an inhibitory effect on leukemia, regulating cell cycle and inducing cell apoptosis.
    • $147
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  • R547
    T6312741713-40-6In house
    R547 (Ro 4584820) is a potent ATP-competitive inhibitor of CDK1 2 4 with Ki of 2 nM 3 nM 1 nM. It is less potent to CDK7 and GSK3α β, while inactive to other kinases. Phase 1.
    • $45
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  • CHIR-99021 HCl
    T2310L1797989-42-4
    CHIR-99021 HCl (Laduviglusib HCl) is a highly potent and selective inhibitor of GSK-3α β, with IC50 values of 10 nM and 6.7 nM respectively. It demonstrates remarkable selectivity for GSK-3, with over 500-fold selectivity over CDC2, ERK2, and other protein kinases. Additionally, CHIR-99021 HCl serves as a robust activator of the Wnt β-catenin signaling pathway. Moreover, it exhibits the ability to enhance self-renewal in both mouse and human embryonic stem cells. Furthermore, CHIR-99021 HCl induces autophagy [1] [2] [3].
    • $30
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  • Tideglusib
    T3067865854-05-3
    Tideglusib (NP031112), a non-ATP competitive inhibitor of glycogen synthase kinase 3 (GSK-3), is with anti-inflammatory and neuroprotective activities.
    • $39
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  • AR-A014418
    T1881487021-52-3
    AR-A014418 (GSK 3β inhibitor VIII) is an ATP-competitive, and selective GSK3β inhibitor.
    • $45
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  • SB 216763
    T3077280744-09-4
    SB 216763 (SB216763) is an effective and specific GSK-3α/β inhibitor (IC50: 34.3 nM).
    • $33
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  • AZD1080
    T1741612487-72-6
    AZD1080 is a selective, orally active, brain permeable GSK3 inhibitor.
    • $36
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  • TBB
    T269517374-26-4
    TBB (NSC-231634)(NSC-231634) is a highly selective, ATP/GTP-competitive inhibitor of casein kinase-2 (CK2).
    • $38
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  • SNS-032
    T6049345627-80-7
    SNS-032 (BMS-387032) is a selective inhibitor of CDK2 (IC50: 48 nM ) and is 10- and 20-fold selective over CDK1 CDK4. It is also sensitive to CDK7 9 (IC50: 62 nM 4 nM), and no effect on CDK6.
    • $43
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  • KenPaullone
    T2247142273-20-9
    KenPaullone (9-Bromopaullone), a potent CDK1, CDK2 and CDK5 inhibitor, as new enhancer for iTreg cell differentiation. Kenpaullone promotes iTreg cell differentiation through increased and prolonged transcription of foxp3 gene by enhancing TGFβ-Smad3 signaling pathway.
    • $32
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  • AT7519
    T6205844442-38-2
    AT7519 is a CDK1 2 4 6 9 inhibitor (IC50: 10-210 nM). It is less effective to CDK3 and little active to CDK7.
    • $52
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  • GSK 3 Inhibitor IX
    T1917667463-62-9
    GSK 3 Inhibitor IX (6-BIO) is a selective reversible, ATP-competitive inhibitor of GSK-3α/β and CDK1-cyclinB complex. It inhibits (GSK-3α/β)/CDK1/CDK5 activity with IC50 values of 5 nM/320 nM/83 nM, respectively.
    • $37
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  • Excisanin A
    TN404678536-37-5
    ExcisaninA may be a potent inhibitor of AKT signaling pathway in tumor cells, it can inhibit invasion by suppressing MMP-2 and MMP-9 expression, it may be a potential anti-metastatic chemotherapeutic agent for the treatment of breast cancer. Excisanin A shows comparable inhibitory effects on the LPS-induced production of NO and PGE2, and activation of NF-kappaB without affecting cell viability.Excisanin A induces apoptosis in colon cancer cell line SW620 as determined by Annexin V staining, the cleavage of caspase-3 and the proteolytic degradation of poly (ADP-ribose) polymerase (PARP).
    • $980
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  • GSK-3β inhibitor 14
    T67856863004-48-2
    GSK-3β inhibitor 14 (1,5-Benzothiazepin-4(5H)-one, 2,3-dihydro-2-methyl-5-(phenylmethyl)-) is a weak GSK-3β inhibitor, IC50﹥ 100μM.
    • $147
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  • Isoangustone A
    TN4263129280-34-8
    Isoangustone A has antitumor activity, it can induce G1 cycle arrest in DU145 human prostate and 4T1 murine mammary cancer cells, it inhibits cell proliferation by targeting PI3K, MKK4, and MKK7 in human melanoma. Isoangustone A dampens mesangial sclerosis associated with inflammation in response to high glucose through hindering TGF-β and NF-κB signaling. Isoangustone A also shows strong ferric reducing activities and effectively scavenged DPPH, ABTS(+), and singlet oxygen radicals.
    • $540
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  • GSK3-IN-1
    T9987478482-74-5
    GSK3-IN-1 is a GSK3B-glycogen synthase kinase-3 beta inhibitor.
    • $44
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  • 5-Bromoindole
    T747310075-50-0
    5-bromoindole is a potential inhibitor of glycogen synthase kinase 3 (GSK-3)and an important pharmaceutical chemical intermediate
    • $39
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  • 2-Methoxystypandrone
    TN277585122-21-0
    2-Methoxystypandrone displays an immunomodulatory effect in a cellular model, it blocks inflammatory responses by impairing NF-κB signaling to limit the inflammation and oxidative stress for preservation of BBB integrity. 2-Methoxystypandrone concomitant
    • $520
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  • GSK3β inhibitor II
    T21956478482-75-6
    GSK3β inhibitor II is a GSK3β inhibitor. GSK3β inhibitor II exhibits the research potential of Alzheimer's disease (AD).
    • $43
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  • Neogrifolin
    TN463723665-96-5
    Neogrifolin is a potential candidate for osteosarcoma, it can induce concentration- and time-dependent suppression of proliferation and induce apoptosis in U2OS and MG63 osteosarcoma cell lines; it exhibits inhibitory activity against nitric oxide (NO) production stimulated by lipopolysaccharide (LPS) in RAW 264.7 cells with the IC50value of 23.3 microM. Neogrifolin possesses antimicrobial activities against Bacillus cereus and Enterococcus faecalis, the MIC values of 20 and 0.5 microg/mL, respectively.
    • $1,790
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  • hAChE-IN-5
    T82243
    hAChE-IN-5 (compound 49) is a dual inhibitor of human acetylcholinesterase (hAChE) and human butyrylcholinesterase (hBuChE), exhibiting inhibitory potency with IC50 values of 0.17 μM for both enzymes. Additionally, it demonstrates potent glycogen synthase kinase 3 beta (GSK3β) inhibition with an IC50 of 0.21 μM. The compound is an effective inhibitor of tau protein and Aβ1-42 peptide self-aggregation. It can virtually bind the peripheral anionic site (PAS), preventing amyloid-beta (Aβ)-induced neurotoxicity. hAChE-IN-5's ability to cross the blood-brain barrier (BBB) underpins its utility in the development of multitargeted anti-Alzheimer’s agents [1].
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  • 9-Hydroxycanthin-6-one
    TN3319138544-91-9
    9-Hydroxycanthin-6-one might be the active component that contributed to the aphrodisiac effect of E. longifolia by antagonizing the smooth muscle tone of CC as well as SV probably through interfering with Ca2+ mobilization.9-Hydroxycanthin-6-one inhibits Wnt signaling through the activation of GSK3β independent of CK1α.
    • $2,298
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  • Charantin
    T1078657126-62-2
    Charantin is a steroidal saponin isolated from Momordica charantia. It increases the release of insulin and slowing down gluconeogenesis. Charantin can inhibit GSK-3.
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  • 4,10-Aromadendranediol
    TN299570051-38-6
    4,10-Aromadendranediol exhibits neurite outgrowth-inducing activity in neurons via activation of the ERK signaling pathway, which may be beneficial to the treatment of brain diseases.
    • $620
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  • PF-04802367
    T96111962178-27-3
    PF-04802367 is a highly selective GSK-3 inhibitor with an IC50 of 2.1 nM based on a recombinant human GSK-3β enzyme assay and 1.1 nM based on ADP-Glo assay. It shows desirable central nervous system (CNS) properties and potency. It is equally effective at inhibition of the two known GSK-3 isoforms (GSK-3α and GSK-3β) with IC50 values of 10.0 and 9.0 nM in mobility shift assays, respectively.
    • $74
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  • C-Peptide 1 (rat)
    T8012441475-27-8
    C-Peptide 1 (rat), a β-catenin/GSK-3β activator and regulator of the Wnt/β-catenin signaling pathway, is utilized in cancer research [1].
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  • CHIR 98024
    T3074556813-39-9
    CHIR 98024 is a potent GSK-3α/β inhibitor with IC50 of 0.65 nM/0.58 nM in cell-free assays, with the ability to distinguish GSK-3 from its closest homologs Cdc2 and ERK2.
    • $37
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  • BRD0209
    T268941597439-87-6
    BRD0209 is a highly selective and potent GSK3 inhibitor.
    • $58
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  • Dehydroglyasperin D
    TMA0291517885-72-2
    Dehydroglyasperin D exhibits anticancer, anti-inflammatory, anti-obesity, antioxidant and anti-aldose reductase effects, it inhibits the proliferation of HT-29 human colorectal cancer cells through direct interaction with phosphatidylinositol 3-kinase; it also mediates suppression of both COX-2 expression and the MLK3 signalling pathway through direct binding and inhibition of MLK3. Dehydroglyasperin D shows strong ferric reducing activities and effectively scavenged DPPH, ABTS(+), and singlet oxygen radicals.
    • $1,670
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