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GSK-3 inhibitors

" in MedChemExpress (MCE) Product Catalog:

149

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Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-154851

    GSK-3 CDK Tau Protein Neurological Disease
    GSK-3 inhibitor 3 is a selective, orally active and brain-penetrant inhibitor of GSK-3, with IC50s of 0.35 nM and 0.25 nM for GSK-3α and GSK-3β, respectively. GSK-3 inhibitor 3 lowers levels of tau protein phosphorylation at S396 in a triple-transgenic mouse Alzheimer’s disease model, with IC50 of 10 nM. GSK-3 inhibitor 3 can be used for neurological disease research .
    <em>GSK-3</em> <em>inhibitor</em> 3
  • HY-30236

    Others Cancer
    5-Bromoindole is a chemical intermediate that can be used for the synthesis of GSK-3 inhibitors and anti-cancer agents .
    5-Bromoindole
  • HY-112392

    GSK-3 Cancer
    GSK-3 Inhibitor XIII is a potent and ATP-competitive GSK-3 inhibitor with a Ki of 24 nM .
    <em>GSK-3</em> <em>Inhibitor</em> XIII
  • HY-154852

    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 .
    <em>GSK-3</em> <em>inhibitor</em> 4
  • HY-155989

    GSK-3 Neurological Disease
    GSK3-IN-4 (compound 0715) is a potent GSK3 inhibitor. GSK3-IN-4 can be used for psychiatric disorder research .
    GSK3-IN-4
  • HY-Q48328

    GSK-3 Metabolic Disease
    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 .
    GSK3-IN-1
  • HY-148329

    GSK-3 Metabolic Disease
    GSK3-IN-2 (compound 8) is a potent GSK3 inhibitor .
    GSK3-IN-2
  • HY-153089
    GSK3-IN-3
    1 Publications Verification

    GSK-3 Mitophagy Neurological Disease
    GSK3-IN-3 is a mitophagy inducer, inducing Parkin-dependent mitophagy. GSK3-IN-3 is also a GSK-3 inhibitor with an IC50 value of 3.01 μM. GSK3-IN-3 is non-ATP nor substrate competitive and is neuroprotective against 6-OHDA .
    GSK3-IN-3
  • HY-107528

    β-catenin GSK-3 Cancer
    FRATtide is a peptide derived from the GSK-3 binding protein that inhibits the phosphorylation of Axin and β-catenin. FRATtide inhibits GSK-3 binding to Axin .
    FRATtide
  • HY-13973A
    GSK-3 inhibitor 1
    1 Publications Verification

    GSK-3 Metabolic Disease
    GSK-3 inhibitor 1 (compound core 3) is a GSK-3 inhibitor that induces stem/progenitor cell self-renewal (e.g. induces stem/progenitor cell proliferation while maintaining the ability to differentiate into tissue cells in the progeny) .
    <em>GSK-3</em> <em>inhibitor</em> 1
  • HY-107531

    GSK-3 Cancer
    A 1070722 is a potent and selective glycogen synthase kinase 3 (GSK-3) inhibitor, with a Ki of 0.6 nM for both GSK-3α and GSK-3β. A 1070722 can penetrate the blood-brain barrier (BBB) and accumulates in brain regions, thus potential for PET radiotracer for the quantification of GSK-3 in brain .
    A 1070722
  • HY-12012
    SB 216763
    25+ 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-16294
    LY2090314
    10+ 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-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-107530

    GSK-3 Cardiovascular Disease Metabolic Disease Cancer
    3F8 is a potent and selective GSK-3β inhibitor that could be useful as new reagent and potential therapeutic candidate for GSK3 related diseases .
    3F8
  • HY-15356
    BIO-acetoxime
    1 Publications Verification

    BIA

    GSK-3 Apoptosis HSV Infection Neurological Disease Inflammation/Immunology
    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.
    BIO-acetoxime
  • HY-14872
    Tideglusib
    5 Publications Verification

    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-111055

    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-134557

    GSK-3 Cancer
    GS87 is a highly specific and potent GSK3 inhibitor with IC50s of 415nM and 521nM for GSK3α and GSK3β, respectively. GS87 induces differentiation of acute myeloid leukemia (AML) cell lines by effectively activating GSK3-dependent signaling components including MAPK signaling. GS87 modulates key GSK3 target proteins involved in cell proliferation and differentiation more effectively than Lithium and SB415285 (SB). GS87 has the potential for acting as a differentiation agent for non-promyelocytic AML research .
    GS87
  • 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-13076
    CHIR-98014
    3 Publications Verification

    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-122026

    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-128879A
    VP3.15 dihydrobromide
    1 Publications Verification

    Phosphodiesterase (PDE) GSK-3 Neurological Disease
    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. VP3.15 dihydrobromide has neuroprotective and neuroreparative activities, thus as potential combined anti-inflammatory and pro-remyelinating therapies for multiple sclerosis (MS) .
    VP3.15 dihydrobromide
  • HY-128879

    Phosphodiesterase (PDE) GSK-3 Neurological Disease
    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) .
    VP3.15
  • HY-156032

    GSK-3 Neurological Disease
    PIMPC is a compound with antioxidant and metal-chelating properties. PIMPC is a novel inhibitor of glycogen synthase kinase 3 (GSK-3). PIMPC has potential anti-Alzheimer's disease effect .
    PIMPC
  • HY-12074

    GSK-3 Metabolic Disease
    Cazpaullone is a glycogen synthase kinase-3 (GSK-3) inhibitor. Cazpaullone can activate pancreatic beta cell protection and replication. Cazpaullone can be used for the research of diabetes .
    Cazpaullone
  • HY-107815

    GSK-3 Neurological Disease
    CHIR 98024 (Compound L) is a glycogen synthase kinase 3 (GSK3) inhibitor with an EC50 of 0.2566 μM .
    CHIR 98024
  • HY-124607

    GSK-3 Neurological Disease
    (R)-BRD3731 is a GSK3 inhibitor extracted from patent US20160375006A1, compound example 273, has IC50s of 1.05 and 6.7 μM for GSK3β and GSK3α, respectively .
    (R)-BRD3731
  • HY-126125

    GSK-3 Neurological Disease Metabolic Disease
    CHIR-98023 is a potent, selective and reversible inhibitor of GSK3, with IC50s of 10 nM and 6.7 nM for GSK3α and GSK3β, respectively. CHIR-98023 can improve insulin action and glucose metabolism .
    CHIR-98023
  • HY-134622

    CDK GSK-3 Neurological Disease Cancer
    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 .
    GSK-3/CDK5/CDK2-IN-1
  • HY-137472

    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-13867
    Bisindolylmaleimide I
    30+ Cited Publications

    GF109203X; Go 6850

    PKC GSK-3 Metabolic Disease Cancer
    Bisindolylmaleimide I (GF109203X) is a cell-permeable and reversible PKC inhibitor (IC50 of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ. Bisindolylmaleimide I is also a GSK-3 inhibitor .
    Bisindolylmaleimide I
  • HY-13867A

    GF109203X hydrochloride; Go 6850 hydrochloride

    PKC GSK-3 Metabolic Disease Cancer
    Bisindolylmaleimide I (GF109203X) hydrochloride is a cell-permeable and reversible PKC inhibitor (IC50 of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ. Bisindolylmaleimide I hydrochloride is also a GSK-3 inhibitor .
    Bisindolylmaleimide I hydrochloride
  • HY-100950

    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 .
    ABC1183
  • HY-114903

    GSK-​3 Inhibitor X

    GSK-3 CDK Neurological Disease Metabolic Disease Cancer
    (E/Z)-BIO-acetoxime (GSK-3 Inhibitor X) is a potent and selective GSK-3α/β inhibitor, with an IC50 of 10 nM. (E/Z)-BIO-acetoxime shows more than 200-flod selectivity over CDK5/p25, CDK2/cyclin A and CDK1/cyclin B (IC50=2.4, 4.3, 63 μM) .
    (E/Z)-BIO-acetoxime
  • HY-10182
    Laduviglusib
    140+ Cited Publications

    CHIR-99021; CT99021

    Organoid GSK-3 Wnt β-catenin Autophagy Metabolic Disease Cancer
    Laduviglusib (CHIR-99021) is a potent, selective and orally active GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. Laduviglusib shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. Laduviglusib is also a potent Wnt/β-catenin signaling pathway activator. Laduviglusib enhances mouse and human embryonic stem cells self-renewal. Laduviglusib induces autophagy .
    Laduviglusib
  • HY-10182B
    Laduviglusib trihydrochloride
    140+ Cited Publications

    CHIR-99021 trihydrochloride; CT99021 trihydrochloride

    Organoid GSK-3 Wnt β-catenin Autophagy Cancer
    Laduviglusib (CHIR-99021) trihydrochloride is a potent and selective GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. Laduviglusib trihydrochloride shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. Laduviglusib trihydrochloride is also a potent Wnt/β-catenin signaling pathway activator. Laduviglusib trihydrochloride enhances mouse and human embryonic stem cells self-renewal. Laduviglusib trihydrochloride induces autophagy .
    Laduviglusib trihydrochloride
  • HY-10182A
    Laduviglusib monohydrochloride
    140+ Cited Publications

    CHIR-99021 monohydrochloride; CT99021 monohydrochloride

    Organoid GSK-3 Wnt β-catenin Autophagy Cancer
    Laduviglusib (CHIR-99021) monohydrochloride is a potent and selective GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. Laduviglusib monohydrochloride shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. Laduviglusib monohydrochloride is also a potent Wnt/β-catenin signaling pathway activator. Laduviglusib monohydrochloride enhances mouse and human embryonic stem cells self-renewal. Laduviglusib monohydrochloride induces autophagy .
    Laduviglusib monohydrochloride
  • HY-151575

    GSK-3 Infection
    PfGSK3/PfPK6-IN-2 is a potent dual PfGSK3/PfPK6 (Plasmodium falciparum GSK3/PK6) inhibitor (IC50: 172 nM and 11 nM respectively). PfGSK3/PfPK6-IN-2 can be used in the research of Malaria .
    PfGSK3/PfPK6-IN-2
  • HY-P1173

    Myristoylated L 803; GSK-3β Inhibitor XIII

    GSK-3 Amyloid-β Neurological Disease
    L803-mts (Myristoylated L 803) is a selective and substrate-competitive GSK-3 peptide inhibitor (IC50: 40 μM). L803-mts also reduces Aβ deposits and ameliorates cognitive deficits in 5XFAD mice. L803-mts shows antidepressive effect in the forced swimming test .
    L803-mts
  • HY-N3542

    Glucosidase Cancer
    Carpachromene is a potent α-glucosidase enzyme inhibitor. Carpachromene ameliorates insulin resistance in HepG2 cells via modulating IR/IRS1/PI3k/Akt/GSK3/FoxO1 pathway .
    Carpachromene
  • HY-112336

    CDK GSK-3 Neurological Disease
    Aloisine RP106 (compound 38) is a potent inhibitor of Cdk1/cyclin B, Cdk5/p25, and GSK3 with IC50s of 0.70µM, 1.5µM, 0.92 µM, respectively .
    Aloisine RP106
  • HY-121629

    PDK-1 Cancer
    PS210 is a potent and selective PDK1 activator with a Kd of 3 μM and targets the PIF-binding pocket of PDK1. PS210 is inactive against other protein kinases, including PDK1 downstream signaling components such as S6K, PKB/Akt or GSK3. In cells, the prodrug of PS210 (PS423) acts as a substrate-selective inhibitor of PDK1, inhibiting the phosphorylation and activation of S6K .
    PS210
  • HY-155723

    CDK DYRK Others
    Leucettinib-92 (compound 92) is an inhibitor of DYRK/CLK kinase, The IC50s are 147 nM (CLK1), 39 nM (CLK2), 5.2 nM (CLK4), 0.8 μM (CLK3), 124 nM (DYRK1A), 204 nM (DYRK1B), 0.16 μM (DYRK2), respectively. 1.0 μM (DYRK3), 0.52 μM (DYRK4), 2.78 μM (GSK3) .
    Leucettinib-92
  • HY-141685

    CDK GSK-3 VEGFR FGFR Cancer
    3-Methylthienyl-carbonyl-JNJ-7706621 is a potent and selective inhibitor of cyclin-dependent kinase (CDK), with IC50s of 6.4 nM and 2 nM for CDK1/cyclin B and CDK2/cyclin A, respectively. 3-Methylthienyl-carbonyl-JNJ-7706621 also shows potent inhibition of GSK-3 (IC50=0.041 μM) and modest potency against CDK4, VEGF-R2, and FGF-R2 (IC50=0.11, 0.13, 0.22 μM, respectively). 3-Methylthienyl-carbonyl-JNJ-7706621 can be used for the research of cancer .
    3-Methylthienyl-carbonyl-JNJ-7706621
  • HY-148133

    GSK-3 Neurological Disease
    GSK-3β inhibitor 12 (compound 15) is an inhibitor of GSK-3β. GSK-3β inhibitor 12 inhibits 49.11% and 37.11% activity of 25 μM and 50 μM GSK-3β, respectively. GSK-3β inhibitor 12 can be used for the research of neurodegenerative diseases .
    GSK-3β inhibitor 12
  • HY-149542

    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 inhibits1-42-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-149054

    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-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-147134

    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

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