Search Result
Results for "
GSK3A+Inhibitors
" in MedChemExpress (MCE) Product Catalog:
2
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-126144A
-
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GSK-3
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Metabolic Disease
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(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 .
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-
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- HY-112392
-
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GSK-3
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Cancer
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GSK-3 Inhibitor XIII is a potent and ATP-competitive GSK-3 inhibitor with a Ki of 24 nM .
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-
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- HY-130795
-
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GSK-3
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Neurological Disease
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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 .
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-
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- HY-112388
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GSK-3
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Neurological Disease
Metabolic Disease
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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 .
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-
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- HY-164907
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GSK-3
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Neurological Disease
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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 .
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-
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- HY-147134
-
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GSK-3
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Neurological Disease
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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 .
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-
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- HY-126201
-
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GSK-3
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Neurological Disease
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GSK-3 inhibitor 7 (compound 22) is a glycogen synthase kinase-3 (GSK-3) inhibitor. GSK-3 inhibitor 7 can be used in nervous system research .
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-
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- HY-169024
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-
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- HY-169602
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-
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- HY-143260
-
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GSK-3
|
Metabolic Disease
Inflammation/Immunology
Cancer
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GSK-3β inhibitor 6 is a potent GSK-3β inhibitor with an IC50 value of 24.4 μM. GSK-3β inhibitor 6 shows high hepatocyte glucose uptake (38%). GSK-3β inhibitor 6 can be used in the research of numerous diseases like diabetes, inflammation, cancer, Alzheimer's disease, and bipolar disorder .
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-
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- HY-149542
-
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Tau Protein
Apoptosis
GSK-3
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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) .
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-
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- HY-168857
-
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GSK-3
Tau Protein
β-catenin
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Neurological Disease
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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 .
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-
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- HY-174272
-
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GSK-3
Amyloid-β
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Neurological Disease
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GSK-3β inhibitor 27 (Compound 1c) is a reversible and competitive GSK-3β inhibitor with an IC50 value of 2.2 μM. GSK-3β inhibitor 27 inhibits tau hyperphosphorylation, reduces Aβ protein aggregation and possesses metal chelation and neuroprotective potential. GSK-3β inhibitor 27 is promising for research of neurodegenerative diseases (such as Alzheimer’s disease) .
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-
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- HY-14679
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GSK-3
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Neurological Disease
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GSK3β inhibitor II is an inhibitor of GSK3β. GSK3β inhibitor II can be used for research of Alzheimer’s disease (AD) .
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- HY-148132
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GSK-3
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Neurological Disease
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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 .
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-
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- HY-153760
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-
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- HY-168079
-
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GSK-3
Tau Protein
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Neurological Disease
Inflammation/Immunology
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GSK-3β inhibitor 21 (compound 44) is an ATP-competitive GSK-3β inhibitor (IC50=6.06 μM) with anti-amyloid aggregation and tau phosphorylation inhibitory activities. GSK-3β inhibitor 21 can be used in the study of Alzheimer's disease .
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-
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- HY-161458
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GSK-3
Tau Protein
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Neurological Disease
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GSK-3β inhibitor 16 (compound 7c) is a GSK-3β inhibitor with the IC50 of 4.68 nM. GSK-3β inhibitor 16 decreases Tau hyperphosphorylated aggregate and alleviates cognitive impairments in the Scopolamin (HY-N0296)-induced model in mice .
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-
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- HY-163748
-
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GSK-3
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Inflammation/Immunology
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GSK-3β inhibitor 17 (compound 5 n) is a potent GSK-3β inhibitor. GSK-3β inhibitor 17 decreases cisplatin (HY-17394) induced p-p65, KIM-1 protein and mRNA expression. GSK-3β inhibitor 17 decreases cisplatin induced TNF-α, IL-1β, IL-6 and MCP-1 mRNA expression. GSK-3β inhibitor 17 shows anti-inflammation effect and has the potential for the research of acute kidney injury .
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- HY-143261
-
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GSK-3
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Metabolic Disease
Inflammation/Immunology
Cancer
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GSK-3β inhibitor 7 is a GSK-3β inhibitor with an IC50 value of 5.25 μM. GSK-3β inhibitor 7 is inserted into the ATP-binding binding pocket of GSK-3β and forms hydrogen-bond. GSK-3β inhibitor 7 shows high hepatocyte glucose uptake (83.5%), and can be used in the research of numerous diseases like diabetes, inflammation, cancer, Alzheimer's disease, and bipolar disorder .
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- HY-175850
-
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GSK-3
Apoptosis
NF-κB
c-Myc
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Cancer
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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 .
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- HY-149054
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GSK-3
Tau Protein
AAK1
Pim
PKC
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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 .
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- HY-162722
-
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GSK-3
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Others
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GSK-3 inhibitor 6 (2) is a CNS penetrated GSK-3 inhibitor, with IC50 values of 29 nM and 24 nM for GSK-3α and GSK-3β, respectively .
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-
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- HY-148133
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GSK-3
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Neurological Disease
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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 .
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- HY-13973A
-
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GSK-3
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Metabolic Disease
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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) .
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- HY-154852
-
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GSK-3
CDK
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Neurological Disease
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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 .
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- HY-126144
-
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GSK-3
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Metabolic Disease
Cancer
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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 .
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-
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- 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 .
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-
-
- HY-120902
-
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Wnt
GSK-3
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Inflammation/Immunology
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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 .
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- HY-141480
-
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GSK-3
Apoptosis
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Cancer
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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 .
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-
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- HY-170491
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GSK-3
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Infection
Neurological Disease
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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) .
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- HY-117194
-
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HIV
GSK-3
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Infection
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18BIOder is a neuroprotective GSK-3β inhibitor, highly selectively inhibiting HIV-1 .
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-
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- HY-10512
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AR 0133418; GSK 3β inhibitor VIII; AR 014418
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GSK-3
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Metabolic Disease
Cancer
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AR-A014418 is a potent, selective and ATP-competitive GSK3β inhibitor (IC50=104 nM; Ki=38 nM) .
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-
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- HY-162638
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-
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- HY-162913
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GSK-3
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Neurological Disease
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GSK-3β inhibitor 20 (compound 3A) is an potent inhibitor of GSK-3β with an IC50 value of 74.4 nM .
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-
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- HY-107530
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-
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- HY-12074
-
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GSK-3
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Metabolic Disease
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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 .
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- HY-Q48328
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GSK-3
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Metabolic Disease
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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 .
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-
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- HY-12012
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-
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- HY-100207
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CP21
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GSK-3
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Cancer
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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.
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-
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- HY-15356
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-
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- HY-169606
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-
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- HY-30236
-
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Drug Intermediate
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Cancer
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5-Bromoindole is a chemical intermediate. 5-Bromoindole derivatives have anticancer activity against breast cancer. 5-Bromoindole can be used to synthesize GSK-3 inhibitors and anticancer active molecules .
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- HY-15761
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GSK-3
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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.
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-
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- HY-169632
-
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GSK-3
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Neurological Disease
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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 .
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- HY-13867A
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GF109203X hydrochloride; Go 6850 hydrochloride
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PKC
GSK-3
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Metabolic Disease
Cancer
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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 [3].
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-
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- HY-14872
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NP031112
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GSK-3
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Neurological Disease
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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.
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-
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- HY-111055
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GSK-3
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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 .
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-
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- HY-13867
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GF109203X; Go 6850
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PKC
GSK-3
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Metabolic Disease
Cancer
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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 [3].
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-
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- HY-124607B
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BRD3731
2 Publications Verification
|
GSK-3
|
Neurological Disease
Metabolic Disease
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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 .
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- HY-10512S
-
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- HY-P1385
-
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GSK-3
p38 MAPK
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Neurological Disease
|
TCS 183, a peptide, is a GSK-3β inhibitor. TCS 183 blocks GSK-3β autoinhibition and decreases the level of AMPK phosphorylation. TCS 183 can be used for neuropathological diseases, particularly Alzheimer’s disease, research .
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- HY-10512R
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AR 0133418 (Standard); GSK 3β inhibitor VIII (Standard); AR 014418 (Standard)
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Reference Standards
GSK-3
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Metabolic Disease
Cancer
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AR-A014418 (Standard) is the analytical standard of AR-A014418. This product is intended for research and analytical applications. AR-A014418 is a potent, selective and ATP-competitive GSK3β inhibitor (IC50=104 nM; Ki=38 nM) .
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- HY-13076
-
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GSK-3
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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.
|
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- HY-10096
-
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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 .
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- HY-12012R
-
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GSK-3
Autophagy
|
Neurological Disease
Cancer
|
SB 216763 (Standard) is the analytical standard of SB 216763. This product is intended for research and analytical applications. SB 216763 is potent, selective and ATP-competitive GSK-3 inhibitor with IC50s of 34.3 nM for both GSK-3α and GSK-3β.
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- HY-137894A
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PF-07104091 hydrate
|
CDK
GSK-3
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Cancer
|
PF-07104091 hydrate is a potent and selective CDK2/cyclin E1 and GSK3β inhibitor, with Kis of 1.16 and 537.81 nM, respectively. PF-07104091 hydrate has anti-tumor activity for cyclin E1-amplified cancers. (patent WO2020157652A2).
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- HY-116830
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BRD0705
1 Publications Verification
|
GSK-3
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Cancer
|
BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50 of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML) research .
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- HY-129492
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GNF4877
1 Publications Verification
|
DYRK
GSK-3
|
Metabolic Disease
|
GNF4877 is a potent DYRK1A and GSK3β inhibitor with IC50s of 6 nM and 16 nM, respectively, which leads to blockade of nuclear factor of activated T-cells (NFATc) nuclear export and increased β-cell proliferation (EC50 of 0.66 μM for mouse β (R7T1) cells) .
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- HY-153089
-
|
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 [3].
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- HY-13867AR
-
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PKC
GSK-3
|
Metabolic Disease
Cancer
|
Bisindolylmaleimide I (hydrochloride) (Standard) is the analytical standard of Bisindolylmaleimide I (hydrochloride). This product is intended for research and analytical applications. 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 [3].
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- HY-107529
-
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GSK-3
|
Neurological Disease
Metabolic Disease
|
TC-G 24 (Compound 24) is a potent, selective glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC50 of 17.1 nM. TC-G 24 can cross the BBB and can be used for studying many diseases such as type 2 diabetes mellitus, stroke, Alzheimer, and other related diseases .
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- HY-13867R
-
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PKC
GSK-3
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Metabolic Disease
Cancer
|
Bisindolylmaleimide I (Standard) is the analytical standard of Bisindolylmaleimide I. This product is intended for research and analytical applications. 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 [3].
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- HY-P1173
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Myristoylated L 803; GSK-3β Inhibitor XIII
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GSK-3
Amyloid-β
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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 .
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- HY-W098905
-
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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) .
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- HY-107531
-
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GSK-3
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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 .
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- HY-116830A
-
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GSK-3
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Cancer
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(Rac)-BRD0705 is a less active racemate of BRD0705. BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50 of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML) .
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- HY-116830B
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(R)-BRD0705
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GSK-3
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Cancer
|
BRD5648 ((R)-BRD0705) is a negative control of BRD0705. BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50 of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML) .
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- HY-19807
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Indirubin-3'-oxime
|
GSK-3
CDK
Lipoxygenase
|
Cancer
|
Indirubin-3'-monoxime is a potent GSK-3β inhibitor, and weakly inhibits 5-Lipoxygenase, with IC50s of 22 nM and 7.8-10 µM, respectively; Indirubin-3'-monoxime also shows inhibitory activities against CDK5/p25 and CDK1/cyclin B, with IC50s of 100 and 180 nM.
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- HY-128879
-
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Phosphodiesterase (PDE)
GSK-3
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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) .
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- HY-128879A
-
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Phosphodiesterase (PDE)
GSK-3
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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) .
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- HY-B1619
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Cromoglycate; Cromoglicic acid; FPL-670 free acid
|
GSK-3
NF-κB
Amyloid-β
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
Cromolyn (Cromoglycate) is an orally active GSK-3β inhibitor with an IC50 of 2.0 μM. Cromolyn is also a mast cell stabilizer that can inhibit the release of mediators from mast cells, regulate reflex bronchoconstriction, and reduce non-specific bronchial hyperreactivity, and Cromolyn can be used in the research of bronchial asthma. In addition, Cromolyn has multiple activities such as anti-inflammatory, anti-allergic, anti-histamine, anti-cancer, and neuroprotective effects [3] .
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- HY-114903
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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) .
|
-
- HY-113914
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Elraglusib
|
GSK-3
Apoptosis
Autophagy
|
Cancer
|
9-ING-41 (Elraglusib) is a maleimide-based ATP-competitive and selective glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC50 of 0.71 μM. 9-ING-41 significantly leads to cell cycle arrest, autophagy and apoptosis in cancer cells. 9-ING-41 has anticancer activity and has the potential for enhancing the antitumor effects of chemotherapeutic agents [3] .
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-
- HY-B0320A
-
Cromoglycate disodium; Cromoglicic acid disodium; FPL-670
|
GSK-3
NF-κB
Amyloid-β
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
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Cromolyn (Cromoglycate) disodium is an orally active GSK-3β inhibitor with an IC50 of 2.0 μM. Cromolyn disodium is also a mast cell stabilizer that can inhibit the release of mediators from mast cells, regulate reflex bronchoconstriction, and reduce non-specific bronchial hyperreactivity, and Cromolyn disodium can be used in the research of bronchial asthma. In addition, Cromolyn disodium has multiple activities such as anti-inflammatory, anti-allergic, anti-histamine, anti-cancer, and neuroprotective effects [3] .
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- HY-B1619R
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GSK-3
NF-κB
Amyloid-β
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Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
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Cromolyn (Standard) is the analytical standard of Cromolyn. This product is intended for research and analytical applications. Cromolyn (Cromoglycate) is an orally active GSK-3β inhibitor with an IC50 of 2.0 μM. Cromolyn is also a mast cell stabilizer that can inhibit the release of mediators from mast cells, regulate reflex bronchoconstriction, and reduce non-specific bronchial hyperreactivity, and Cromolyn can be used in the research of bronchial asthma. In addition, Cromolyn has multiple activities such as anti-inflammatory, anti-allergic, anti-histamine, anti-cancer, and neuroprotective effects [3] .
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- HY-B1619S
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Cromoglycate-d5; Cromoglicic acid-d5; FPL-670-d5 free acid
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Isotope-Labeled Compounds
GSK-3
NF-κB
Amyloid-β
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Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
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Cromolyn-d5 (Cromoglycate-d5) is the deuterium labeled Cromolyn (HY-B1619). Cromolyn (Cromoglycate) is an orally active GSK-3β inhibitor with an IC50 of 2.0 μM. Cromolyn is also a mast cell stabilizer that can inhibit the release of mediators from mast cells, regulate reflex bronchoconstriction, and reduce non-specific bronchial hyperreactivity, and Cromolyn can be used in the research of bronchial asthma. In addition, Cromolyn has multiple activities such as anti-inflammatory, anti-allergic, anti-histamine, anti-cancer, and neuroprotective effects .
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- HY-171031
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GSK-3
Apoptosis
Caspase
Bcl-2 Family
Reactive Oxygen Species (ROS)
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Neurological Disease
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TFGF-18 is a GSK-3β inhibitor (IC50: 0.59 μM). TFGF-18 inhibits LPS-induced microglia activation and proinflammatory mediators release via inhibiting GSK-3β and downstream p65/NF-κB signaling. TFGF-18 inhibits neuronal apoptosis and oxidative stress, inhibits expressions of Bax, caspase3 and cleaved-caspase3 and increases the expression of Bcl-2. TFGF-18 has neuroprotection effect, inhibit neuroinflammation and attenuates cognitive impairment .
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- HY-122026
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PF-367
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GSK-3
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Neurological Disease
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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 .
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- HY-B0320AR
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Cromoglycate disodium (Standard); Cromoglicic acid disodium (Standard); FPL-670 (Standard)
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Reference Standards
GSK-3
NF-κB
Amyloid-β
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Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
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Cromolyn disodium (Standard) (Cromoglycate disodium (Standard)) is the analytical standard of Cromolyn disodium (HY-B0320A). This product is intended for research and analytical applications. Cromolyn (Cromoglycate) disodium is an orally active GSK-3β inhibitor with an IC50 of 2.0 μM. Cromolyn disodium is also a mast cell stabilizer that can inhibit the release of mediators from mast cells, regulate reflex bronchoconstriction, and reduce non-specific bronchial hyperreactivity, and Cromolyn disodium can be used in the research of bronchial asthma. In addition, Cromolyn disodium has multiple activities such as anti-inflammatory, anti-allergic, anti-histamine, anti-cancer, and neuroprotective effects [3].
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- HY-149845
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GSK-3
PROTACs
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Neurological Disease
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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 .
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- HY-176287
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Dopamine Receptor
GSK-3
PKA
P-glycoprotein
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Neurological Disease
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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 .
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- HY-150537
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Cholinesterase (ChE)
GSK-3
Microtubule/Tubulin
ROS Kinase
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Neurological Disease
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AChE/GSK-3β-IN-1 (compound GT15) is a potent, dual AChE/GSK-3β inhibitor with IC50 values of 1.2, 149.8 and 22.4 nM for hAChE , hBChE and hGSK-3β, respectively. AChE/GSK-3β-IN-1 penetrates the blood-brain barrier (BBB). AChE/GSK-3β-IN-1 has high kinase selectivity profiles for the CMGC kinase family. AChE/GSK-3β-IN-1 occupies the ATP binding site of DYRK1A. AChE/GSK-3β-IN-1 inhibits ROS expression and reduces oxidative stress. AChE/GSK-3β-IN-1 can be used for Alzheimer’s disease research .
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P1173
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Myristoylated L 803; GSK-3β Inhibitor XIII
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GSK-3
Amyloid-β
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Neurological Disease
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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 .
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- HY-P1385
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GSK-3
p38 MAPK
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Neurological Disease
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TCS 183, a peptide, is a GSK-3β inhibitor. TCS 183 blocks GSK-3β autoinhibition and decreases the level of AMPK phosphorylation. TCS 183 can be used for neuropathological diseases, particularly Alzheimer’s disease, research .
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Cat. No. |
Product Name |
Chemical Structure |
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- HY-10512S
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AR-A014418-d3 is the deuterium labeled AR-A014418. AR-A014418 is a potent, selective, and ATP-competitive GSK3β inhibitor (IC50=104 nM; Ki=38 nM) .
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- HY-B1619S
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Cromolyn-d5 (Cromoglycate-d5) is the deuterium labeled Cromolyn (HY-B1619). Cromolyn (Cromoglycate) is an orally active GSK-3β inhibitor with an IC50 of 2.0 μM. Cromolyn is also a mast cell stabilizer that can inhibit the release of mediators from mast cells, regulate reflex bronchoconstriction, and reduce non-specific bronchial hyperreactivity, and Cromolyn can be used in the research of bronchial asthma. In addition, Cromolyn has multiple activities such as anti-inflammatory, anti-allergic, anti-histamine, anti-cancer, and neuroprotective effects .
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