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GSK3-IN-3

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製品番号 製品名 Target 研究分野 構造式
  • 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-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-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-10182G
    Laduviglusib
    2 Publications Verification

    CHIR-99021; CT99021

    GSK-3 Wnt β-catenin Autophagy Metabolic Disease Cancer
    Laduviglusib (CHIR-99021) (GMP) is Laduviglusib (HY-10182) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Laduviglusib is a potent, orally active and selective GSK-3α/β inhibitor.
    Laduviglusib
  • 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-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-12524
    Bikinin
    2 Publications Verification

    AbrasIN

    GSK-3 Others
    Bikinin is a non-steroidal, ATP-competitive inhibitor of plant GSK-3/Shaggy-like kinases and activates BR (brassinosteroids) signaling.
    Bikinin
  • 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-153089
    GSK3-IN-3
    4 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-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-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-107531

    GSK-3 Neurological Disease 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 decreases spontaneous locomotion .
    A 1070722
  • 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-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-119940
    MC180295
    1 Publications Verification

    (rel)-MC180295

    CDK Cancer
    MC180295 ((rel)-MC180295) is a potent and selective CDK9-Cyclin T1 inhibitor, with an IC50 of 5 nM, at least 22-fold more selective for CDK9 over other CDKs. MC180295 also inhibits GSK-3α and GSK-3β. MC180295 ((rel)-MC180295) has potent anti-tumor effect .
    MC180295
  • HY-15356
    BIO-acetoxime
    2 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-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 .
    GSK-3 inhibitor 3
  • HY-P10605

    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-149845

    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-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-148561

    CDK GSK-3 PKC Cancer
    CDK8-IN-12 is an orally active, potent CDK8 inhibitor with a Ki of 14 nM. CDK8-IN-12 has off-target kinase inhibition on GSK-3α, GSK-3β, PCK-θ with Kis of 13 nM, 4 nM, 109 nM, respectively. CDK8-IN-12 shows potent anti-proliferative effects selectively on MV4-11 cell. CDK8-IN-12 is an anti-cancer agent .
    CDK8-IN-12
  • HY-111930

    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-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-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-112388
    GSK-3b Inhibitor XI
    1 Publications Verification

    GSK-3 Neurological Disease Metabolic Disease
    GSK-3b Inhibitor XI (Compound 33) is a potent and selective GSK3β inhibitor, with a Ki value of 25 nM. GSK-3b Inhibitor XI increases glycogen synthase (GS) activity. GSK-3b Inhibitor XI can be used for research on type 2 diabetes and Alzheimer’s disease .
    GSK-3b Inhibitor XI
  • HY-144290

    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-111379

    DYRK CDK GSK-3 Neurological Disease Metabolic Disease Cancer
    EHT 5372 is a highly potent and selective inhibitor of DYRK's family kinases with IC50s of 0.22, 0.28, 10.8, 93.2, 22.8, 88.8, 59.0, 7.44, and 221 nM for DYRK1A, DYRK1B, DYRK2, DYRK3, CLK1, CLK2, CLK4, GSK-3α, and GSK-3β, respectively .
    EHT 5372
  • 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 .
    GSK-3 inhibitor 4
  • 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-155805

    CDK Cancer
    CAF-382 (compound B1) is an analog of SNS-032 and a CDKL5 and pan-CDK inhibitor with a weak GSK3α/β affinity (>1.8 μM) and inhibitory activity. CAF-382 inhibits CDKL5 and blocks the phosphorylation of the CDKL5 E2 domain .
    SGC-CAF382-1
  • HY-164907

    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-120902

    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-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-W969907

    GSK-3 Others
    GSK3a-IN-38 is a groundbreaking small molecule that effectively inhibits GSK-3a activity.
    GSK3-IN-7
  • HY-10096

    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-134393B

    N6-Methyl-ATP trisodium solution (100 mM)

    GSK-3 Others
    6-Me-ATP (N6-Methyl-ATP) trisodium solution (100 mM) is a N 6-modified ATP derivative. 6-Me-ATP trisodium shows excellent binding affinity to GSK3, serving as the phosphate group donor for GSK3β-catalyzed phosphorylation of its substrate peptide .
    6-Me-ATP trisodium solution (100 mM)
  • 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
  • HY-144826

    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-126144A

    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-176287

    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-112363

    RP107

    CDK GSK-3 ERK JNK CFTR Inflammation/Immunology Cancer
    Aloisine A (RP107) is a a potent cyclin-dependent kinase (CDK) inhibitor with IC50s of 0.15 μM, 0.12 μM, 0.4 μM, 0.16 μM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK5/p35, respectively. Aloisine A ininhibits GSK-3α (IC50=0.5 μM) and GSK-3β (IC50=1.5 μM). Aloisine A stimulates wild-type CFTR and mutated CFTR, with submicromolar affinity by a cAMP-independent mechanism. Aloisine A has the potential for CFTR-related diseases, including cystic fibrosis research .
    Aloisine A
  • 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 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-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-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-170491

    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-148132

    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-W098905

    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 aggregates in the CL2006 strain, and can be used to research Alzheimer's disease (AD) .
    GSK3β-IN-3

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