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GSK-3β inhibitors

" in MedChemExpress (MCE) Product Catalog:

263

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3

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4

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7

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33

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6

Isotope-Labeled Compounds

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GMP Molecules

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-14872
    Tideglusib
    5+ Cited Publications

    NP031112

    		 GSK-3 Neurological Disease
    Tideglusib (NP031112) is an irreversible GSK-3 inhibitor with IC50s of 5 nM and 60 nM for GSK-3β WT (1 h preincubation) and GSK-3β C199A (1 h preincubation), respectively.
    Tideglusib
  • HY-16294
    LY2090314
    15+ Cited Publications

    		 GSK-3 Cancer
    LY2090314 is a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50 values of 1.5 nM and 0.9 nM for GSK-3α and GSK-3β, respectively.
    LY2090314
  • HY-10514
    BX795
    35+ Cited Publications

    		 PDK-1 IKK Autophagy Cancer
    BX795 is a potent and selective inhibitor of PDK1, with an IC50 of 6 nM. BX795 is also a potent and relatively specific inhibitor of TBK1 and IKKε, with an IC50 of 6 and 41 nM, respectively. BX795 blocks phosphorylation of S6K1, Akt, PKCδ, and GSK3β, and has lower selectivity over PKA, PKC, c-Kit, GSK3β etc. BX795 modulates autophagy .
    BX795
  • HY-12012
    SB 216763
    40+ Cited Publications

    		 GSK-3 Autophagy Neurological Disease Cancer
    SB 216763 is potent, selective and ATP-competitive GSK-3 inhibitor with IC50s of 34.3 nM for both GSK-3α and GSK-3β.
    SB 216763
  • HY-10590
    TWS119
    30+ Cited Publications

    		 Wnt GSK-3 Autophagy Neurological Disease Cancer
    TWS119 is an inhibitor of GSK-3β, with an IC50 of 30 nM, and activates the wnt/β-catenin pathway.
    TWS119
  • HY-12292
    IM-12
    5+ Cited Publications

    		 Wnt GSK-3 Cancer
    IM-12 is an inhibitor of GSK-3β, with an IC50 of 53 nM, and also enhances Wnt signalling.
    IM-12
  • HY-59090
    1-Azakenpaullone
    3 Publications Verification

    1-Akp

    		 GSK-3 Neurological Disease Metabolic Disease
    1-Azakenpaullone (1-Akp) is a highly selective and ATP-competitive inhibitor of glycogen synthase kinase-3 β (GSK-3β), with an IC50 value of 18 nM .
    1-Azakenpaullone
  • HY-15761
    AZD2858
    5+ Cited Publications

    		 GSK-3 Neurological Disease
    AZD2858 is a potent, orally active GSK-3 inhibitor, with IC50s of 0.9 and 5 nM for GSK-3α and GSK-3β, respectively, used in the research of fracture healing.
    AZD2858
  • HY-10512
    AR-A014418
    15+ Cited Publications

    AR 0133418; GSK 3β inhibitor VIII; AR 014418

    		 GSK-3 Metabolic Disease Cancer
    AR-A014418 is a potent, selective and ATP-competitive GSK3β inhibitor (IC50=104 nM; Ki=38 nM) .
    AR-A014418
  • HY-13862
    AZD1080
    5 Publications Verification

    		 GSK-3 Neurological Disease
    AZD1080 is a potent and selective GSK3 inhibitor. AZD1080 inhibits recombinant human GSK3α and GSK3β with pKi (IC50) of 8.2 (6.9 nM) and 7.5 (31 nM), respectively.
    AZD1080
  • HY-130795
    GSK-3β inhibitor 2
    1 Publications Verification

    		 GSK-3 Neurological Disease
    GSK-3β inhibitor 2 (Compound 3) is a potent, selective and orally active GSK-3β inhibitor with an IC50 of 1.1 nM. GSK-3β inhibitor 2 can cross the blood-brain barrier. GSK-3β inhibitor 2 has the potential for Alzheimer's disease .
    GSK-3β inhibitor 2
  • HY-11012
    TDZD-8
    10+ Cited Publications

    GSK-3β Inhibitor I; NP 01139

    		 GSK-3 Cancer
    TDZD-8 is an inhibitor of GSK-3β, with an IC50 of 2 μM; TDZD-8 shows less potent activities against Cdk-1/cyclin B, CK-II, PKA, and PKC, with all IC50s of >100 μM.
    TDZD-8
  • HY-100207
    CP21R7
    5+ Cited Publications

    CP21

    		 GSK-3 Cancer
    CP21R7 is potent GSK-3β inhibitor, with an IC50 of 1.8 nM; CP21R7 also shows inhibitory activitiy against PKCα, with an IC50 of 1900 nM.
    CP21R7
  • HY-13076
    CHIR-98014
    5+ Cited Publications

    		 GSK-3 Metabolic Disease
    CHIR-98014 is a potent, cell-permeable GSK-3 inhibitor with IC50s of 0.65 and 0.58 nM for GSK-3α and GSK-3β, respectively; it shows less potent activities against cdc2 and erk2.
    CHIR-98014
  • HY-153166
    PT-65

    		PROTACs GSK-3 Tau Protein Neurological Disease
    PT-65 is a GSK3α and GSK3β PROTAC degrader with DC50 values of 28.3 nM and 34.2 nM, respectively. PT-65 inhibits excessive tau phosphorylation mediated by GSK3β, Aβ and Okadaic acid (HY-N6785). PT-65 is applicable for the research of Alzheimer's disease .
    PT-65
  • HY-131447
    KY19382
    4 Publications Verification

    A3051

    		 GSK-3 Wnt β-catenin Metabolic Disease
    KY19382 is a potent and orally active dual inhibitor of CXXC5-DVL and GSK3β, with IC50s of 19 and 10 nM, respectively. KY19382 activates Wnt/β-catenin signaling through inhibitory effects on both CXXC5-DVL interaction and GSK3β activity. KY19382 can be used for the research of high fat diet (HFD) induced metabolic diseases .
    KY19382
  • HY-126144
    GSK-3β inhibitor 1
    4 Publications Verification

    		 GSK-3 Metabolic Disease Cancer
    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 .
    GSK-3β inhibitor 1
  • HY-124607B
    BRD3731
    2 Publications Verification

    		 GSK-3 Neurological Disease Metabolic Disease
    BRD3731 is a selective GSK3β inhibitor, with IC50s of 15 nM and 215 nM for GSK3β and GSK3α, respectively. BRD3731 is potentail for the research of post-traumatic stress disorder (PTSD), psychiatric disorder, diabetes, and neurodegenerative disorders .
    BRD3731
  • HY-15438
    SB 415286
    5+ Cited Publications

    		 GSK-3 Apoptosis Metabolic Disease
    SB 415286 is a potent and selective cell permeable inhibitor of GSK-3α, with an IC50 of 77.5 nM, and a Ki of 30.75 nM; SB 415286 is equally effective at inhibiting human GSK-3α and GSK-3β.
    SB 415286
  • HY-149845
    PROTAC GSK-3β Degrader-1

    		PROTACs GSK-3 Neurological Disease
    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 Aβ25-35 peptide and CuSO4. PROTAC GSK-3β Degrader-1 can be used to research in Alzheimer's disease .
    PROTAC GSK-3β Degrader-1
  • HY-P10605
    GSK3β-peptide

    		Akt GSK-3 Cancer
    GSK3β-peptide is a substrate mimetic peptide of glycogen synthase kinase 3-β (GSK3-β) that can bind to the active site of GSK3-β and mimic the behavior of a real substrate. GSK3β-peptide can be used to develop substrate mimetic inhibitors of Akt as potential anticancer drugs .
    GSK3β-peptide
  • HY-122026
    PF-04802367

    PF-367

    		 GSK-3 Neurological Disease
    PF-04802367 (PF-367) 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. PF-04802367 shows desirable central nervous system (CNS) properties and potency. PF-04802367 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 .
    PF-04802367
  • HY-111930
    5-Iodo-indirubin-3'-monoxime

    		GSK-3 CDK Cancer
    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 .
    5-Iodo-indirubin-3'-monoxime
  • HY-141480
    GSK-3β inhibitor 3
    1 Publications Verification

    		 GSK-3 Apoptosis Cancer
    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 .
    GSK-3β inhibitor 3
  • HY-14679
    GSK3β inhibitor II

    		GSK-3 Neurological Disease
    GSK3β inhibitor II is an inhibitor of GSK3β. GSK3β inhibitor II can be used for research of Alzheimer’s disease (AD) .
    GSK3β inhibitor II
  • HY-149054
    GSK-3β inhibitor 13

    		GSK-3 Tau Protein AAK1 Pim PKC Neurological Disease
    GSK-3β inhibitor 13 (compound 47) is an orally active and potent GSK-3β inhibitor with blood-brain permeability. GSK-3β inhibitor 13 inhibits GSK-3β and GSK-3α with IC50s of 0.73 nM and 0.35 nM, respectively. GSK-3β inhibitor 13 significantly decreases the phosphorylation of tau (IC50=58 nM), which leads the formation of the neurofibrillary tangles associated with Alzheimer's disease .
    GSK-3β inhibitor 13
  • HY-154852
    GSK-3 inhibitor 4

    		GSK-3 CDK Neurological Disease
    GSK-3 inhibitor 4 is an orally active and brain-penetrant inhibitor of GSK-3, CDK2, and CDK5, with IC50 values of 0.56 nM (GSK-3β), 0.45 nM (GSK-3α), 0.47 μM, and 0.68 μM, respectively. GSK-3 inhibitor 4 effectively reduces the phosphorylation level of Tau protein. GSK-3 inhibitor 4 can be used in Alzheimer's disease (AD) studies .
    GSK-3 inhibitor 4
  • HY-144290
    ARN25068

    		GSK-3 DYRK Neurological Disease
    ARN25068 is a sub-micromolar inhibitor of the three protein kinases, GSK-3β, FYN and DYRK1A to tackle tau hyperphosphorylation .
    ARN25068
  • HY-137472
    SAR502250

    		GSK-3 Neurological Disease
    SAR502250 is a potent, selective, ATP competitive, orally active and brain-penetrant inhibitor of GSK3, with an IC50 of 12 nM for human GSK-3β. SAR502250 displays antidepressant-like activity. SAR502250 can be used for the research of Alzheimer’s disease (AD) .
    SAR502250
  • HY-164907
    GSK-3β inhibitor 22

    		GSK-3 Neurological Disease
    GSK-3β inhibitor 22 (compound 20o) is a GSK-3β inhibitor with an IC50 of 3.1 nM. GSK-3β inhibitor 22 has the potential of the study of Alzheimer's disease .
    GSK-3β inhibitor 22
  • HY-N6580
    Ginsenoside Rg4

    		PI3K Akt GSK-3 Reactive Oxygen Species (ROS) TNF Receptor Interleukin Related Infection Metabolic Disease Inflammation/Immunology
    Ginsenoside Rg4 is an orally active protopanaxatriol type ginsenoside. Ginsenoside Rg4 can activate PI3K, AKT and GSK-3β signaling. Ginsenoside Rg4 can inhibit ROS and inflammatory cytokine levels. Ginsenoside Rg4 can be used for the researches of inflammation, infection and metabolic disease, such as sepsis and lung inflammation .
    Ginsenoside Rg4
  • HY-10096
    TCS2002

    		GSK-3 Neurological Disease
    TCS2002 (Compound 9b) is a highly selective, orally bioavailable and potent GSK-3β inhibitor with the IC50 of 35 nM. TCS2002 shows good pharmacokinetic profiles including favorable BBB penetration. TCS2002 can be used for the research of Alzheimer’s disease .
    TCS2002
  • HY-120902
    GSK-3β inhibitor 8

    		Wnt GSK-3 Inflammation/Immunology
    GSK-3β inhibitor 8, a thiophenacil derivative, is an effective and selective inhibitor of GSK-3β (IC50=64 nM). GSK-3β inhibitor 8 negatively regulated Wnt signaling pathway and stimulated β cell proliferation .
    GSK-3β inhibitor 8
  • HY-172171
    GSK3β-IN-2

    		GSK-3 β-catenin Wnt Neurological Disease
    GSK3β-IN-2 (Compound S01) is the inhibitor for GSK3β with an IC50 of 0.35 nM. GSK3β-IN-2 activates Wnt/β-catenin signaling pathway, promotes neurogenesis and neurite growth. GSK3β-IN-2 inhibits Aβ-induced tau hyperphosphorylation at Ser396, reduces the formation of neurofibrillary tangles. GSK3β-IN-2 ameliorates Alzheimer's Disease in zebrafish model .
    GSK3β-IN-2
  • HY-111055
    BIP-135

    		GSK-3 Neurological Disease
    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 .
    BIP-135
  • HY-162675
    COB-187

    		GSK-3 Infection Neurological Disease Metabolic Disease Cancer
    COB-187 is a potent, ATP-competitive and selective inhibitor of GSK-3β. COB-187 inhibits GSK-3 through a reversible and Cysteine (Cys)-199-dependent mechanism. COB-187 inhibits LPS induced cytokine production and SARS-CoV-2 spike protein-induced CXCL10 production .
    COB-187
  • HY-147134
    GSK-3β inhibitor 10

    		GSK-3 Neurological Disease
    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 .
    GSK-3β inhibitor 10
  • HY-126144A
    (E/Z)-GSK-3β inhibitor 1

    		GSK-3 Metabolic Disease
    (E/Z)-GSK-3β inhibitor 1 is a racemic compound of (E)-GSK-3β inhibitor 1 and (Z)-GSK-3β inhibitor 1 isomers. 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 .
    (E/Z)-GSK-3β inhibitor 1
  • HY-144826
    ZDWX-25

    		GSK-3 Neurological Disease
    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 .
    ZDWX-25
  • HY-176287
    ARN25657

    		Dopamine Receptor GSK-3 PKA P-glycoprotein Neurological Disease
    ARN25657 is a dual-acting D3R/GSK-3β modulator. ARN25657 has both partial D3R agonist activity (EC50 = 15.2 nM, Ki =1.5 nM) and potent GSK-3β inhibitor activity (IC50 = 19.3 nM). ARN25657 exhibits excellent GSK-3β selectivity over FYN, PKA, and CDK5/p35. ARN25657 inhibits P-glycoprotein (P-gP)-mediated acetoxymethyl calcein efflux and improves in vitro ADME properties while maintaining a balanced dual-target profile. ARN25657 is useful for studying bipolar disorder and related neuropsychiatric disorders .
    ARN25657
  • HY-179496
    ChE/GSK-3β-IN-1

    		GSK-3 Cholinesterase (ChE) Amyloid-β Neurological Disease
    ChE/GSK-3β-IN-1 (compound 18o) is a potent dual ChE/GSK-3β inhibitor. ChE/GSK-3β-IN-1 exhibits dual inhibition of AChE (IC50 = 1.7 μM), butyrylcholinesterase (BChE) (IC50 = 5.3 μM), and GSK-3β (IC50 = 5.7 μM). ChE/GSK-3β-IN-1 inhibits Aβ1-42 self-aggregation. ChE/GSK-3β-IN-1 can be used for Alzheimer’s disease (AD) research .
    ChE/GSK-3β-IN-1
  • HY-149542
    GSK-3β inhibitor 15

    		Tau Protein Apoptosis GSK-3 Neurological Disease
    GSK-3β inhibitor 15 (Compound 54) is a GSK-3β inhibitor (IC50: 3.4 nM). GSK-3β inhibitor 15 inhibits Aβ1-42-induced GSK-3β and tau protein phosphorylation. GSK-3β inhibitor 15 inhibits LPS-induced iNOS expression. GSK-3β inhibitor 15 has neuroprotective effects on Aβ1-42-induced neurotoxicity. GSK-3β inhibitor 15 can be used for research of Alzheimer’s disease (AD) .
    GSK-3β inhibitor 15
  • HY-168857
    GSK-3β inhibitor 24

    		GSK-3 Tau Protein β-catenin Neurological Disease
    GSK-3β inhibitor 24 (Compound 41) is a potent GSK-3β inhibitor with an IC50 of 0.22 nM. GSK-3β inhibitor 24 increases GSK-3β phosphorylation at Ser9 site dose-dependently. GSK-3β inhibitor 24 inhibits the hyperphosphorylation of tau protein by decreasing the p-tau-Ser396 abundance. GSK-3β inhibitor 24 up-regulates β-catenin and neurogenesis-related markers (GAP43 and MAP-2). GSK-3β inhibitor 24 demonstrates remarkable anti-Alzheimer's disease (AD) effects .
    GSK-3β inhibitor 24
  • HY-175850
    GSK-3β-IN-28

    		GSK-3 Apoptosis NF-κB c-Myc Cancer
    GSK-3β inhibitor 28 is selective and non-competitivea glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC50 of 14.82 nM. GSK-3β inhibitor 28 can upregulate the expression level of phosphorylated GSK-3β and downregulate the expression of p-NF-κB, P65, C-myc and Cyclin D1. GSK-3β inhibitor 28 can induce cells apoptosis, G1 phase arrest and inhibit migration. GSK-3β inhibitor 28 can be used for the research of cancer, such as colorectal cancer .
    GSK-3β-IN-28
  • HY-148132
    GSK-3β inhibitor 11

    		GSK-3 Neurological Disease
    GSK-3β inhibitor 11 (compound 21) is a glycogen synthase kinase-3β (GSK-3β) inhibitor (IC50=10.02 μM). GSK-3β inhibitor 11 can be used in neurodegenerative disease research .
    GSK-3β inhibitor 11
  • HY-170491
    GSK-3β inhibitor 23

    		GSK-3 Infection Neurological Disease
    GSK-3β inhibitor 23 (Compound 11726169) is the inhibitor for glycogen synthase kinase-3, that inhibits GSK-3β and GSK-3α with IC50 of 12.1 nM and 18.8 nM. GSK-3β inhibitor 23 exhibits antiviral activity against HIV 1. GSK-3β inhibitor 23 exhibits good metabolic stablility in mouse/human liver microsomes and plasma, but poor Caco-2 permeability (which predicts low oral bioavailability) .
    GSK-3β inhibitor 23
  • HY-W098905
    GSK3β-IN-3

    		GSK-3 Cytochrome P450 Amyloid-β Tau Protein Neurological Disease
    GSK3β-IN-3 is an ATP-competitive GSK-3β inhibitor (IC50 = 0.90 μM). GSK3β-IN-3 can reduce the phosphorylation level of tau protein in the BR5706 strain and reduce the deposition of Aβ aggregates in the CL2006 strain, and can be used to research Alzheimer's disease (AD) .
    GSK3β-IN-3
  • HY-120917
    BRD1172

    ML320

    		 GSK-3 β-catenin Cardiovascular Disease Neurological Disease Cancer
    BRD1172 (ML320) is a selectivity GSK3β inhibitor with an IC50 of 24 nM for GSK3β over CDK5. BRD1172 significantly inhibits GSK3β-mediated Tau phosphorylation in SH-SY5Y cells, and relieves negative regulation by GSK3β on β-catenin degradation and TCF/LEF promoter activities. BRD1172 can be used for Alzheimer’s disease, cardiac hypertrophy and cancers research .
    BRD1172
  • HY-169632
    GSK3β-IN-1

    		GSK-3 Neurological Disease
    GSK3β-IN-1 (compound 1) is a glycogen synthase kinase-3β (GSK-3β) inhibitor (IC50=65 nM), which can be used in the study of Alzheimer's disease .
    GSK3β-IN-1
  • HY-161751
    MJ34

    		GSK-3 Cancer
    MJ34 is a potent inhibitor of GSK-3β and GSK-3α, with the IC50s of 15.4 nM and 31.5 nM, respectively. MJ34 plays an important role in cancer research
    MJ34

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