Search Result
Results for "
GSK-3 inhibitor
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
2
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-154851
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GSK-3
CDK
Tau Protein
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Neurological Disease
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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-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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- 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-10580
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6-Bromoindirubin-3'-oxime; BIO; MLS 2052
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GSK-3
CDK
Apoptosis
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Cancer
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GSK 3 Inhibitor IX (6-Bromoindirubin-3'-oxime; BIO) is a potent, selective, reversible and ATP-competitive inhibitor of GSK-3α/β and CDK1-cyclinB complex with IC50s of 5 nM/320 nM/80 nM for (GSK-3α/β)/CDK1/CDK5, respectively.
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- HY-30236
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Others
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Cancer
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5-Bromoindole is a chemical intermediate that can be used for the synthesis of GSK-3 inhibitors and anti-cancer agents .
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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-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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- 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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- HY-114903
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GSK-3 inhibitor X
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GSK-3
CDK
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Neurological Disease
Metabolic Disease
Cancer
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(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) .
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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-155989
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GSK-3
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Neurological Disease
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GSK3-IN-4 (compound 0715) is a potent GSK3 inhibitor. GSK3-IN-4 can be used for psychiatric disorder research .
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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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- 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-148329
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- HY-149542
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Tau Protein
Apoptosis
GSK-3
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Neurological Disease
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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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- HY-149054
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GSK-3
Tau Protein
AAK1
Pim
PKC
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Neurological Disease
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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-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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- HY-169024
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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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- 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-143260
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GSK-3
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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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- HY-153089
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GSK-3
Mitophagy
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Neurological Disease
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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 .
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- HY-156871
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Others
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Others
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CAMK1D-IN-1 is a potent inhibitor that targets the ATP-binding site of GSK-3, functioning as a GSK-3 inhibitor.
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- HY-162638
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- HY-120902
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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-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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- 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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- 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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- HY-153760
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- HY-107528
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β-catenin
GSK-3
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Cancer
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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 .
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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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- 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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- 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-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-112388
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GSK-3
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Neurological Disease
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GSK3β inhibitor XI is a potent inhibitor of glycogen synthase kinase 3β (GSK3β; Ki=25 nM). It is selective for GSK3β over a panel of 79 kinases at a concentration of 10 μM. GSK3β inhibitor XI inhibits GSK3β in HEK293 cells (EC50=32 nM).
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- HY-126144
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GSK-3
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Metabolic Disease
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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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- 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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- HY-107531
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GSK-3
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Cancer
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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 .
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- HY-P10605
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Akt
GSK-3
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Cancer
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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 .
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- HY-12012
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- HY-16294
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GSK-3
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Cancer
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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.
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- HY-15761
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GSK-3
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Neurological Disease
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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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- HY-107530
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- HY-15356
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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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- HY-111055
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GSK-3
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Neurological Disease
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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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- HY-134557
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GSK-3
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Cancer
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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 .
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- HY-13862
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AZD1080
5 Publications Verification
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GSK-3
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Neurological Disease
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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.
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- HY-13076
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GSK-3
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Metabolic Disease
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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-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-128879A
-
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Phosphodiesterase (PDE)
GSK-3
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Neurological Disease
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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-128879
-
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Phosphodiesterase (PDE)
GSK-3
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Neurological Disease
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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-153166
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PROTACs
GSK-3
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Neurological Disease
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PT-65 is a potent and selective GSK3 PROTAC degrader with the highest degradation capacity of GSK3α (DC50= 28.3 nM) and GSK3β (DC50= 34.2 nM) in SH-SY5Y cells. PT-65 can be used in Alzheimer's disease research .(Pink: GSK3 inhibitor (HY-15761); Black: linker; Blue: CRBN Ligand (HY-10984))
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- HY-156032
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GSK-3
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Neurological Disease
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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 .
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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-107815
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GSK-3
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Neurological Disease
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CHIR 98024 (Compound L) is a glycogen synthase kinase 3 (GSK3) inhibitor with an EC50 of 0.2566 μM .
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- HY-124607
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GSK-3
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Neurological Disease
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(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 .
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- HY-126125
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GSK-3
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Neurological Disease
Metabolic Disease
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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 .
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- HY-117739
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GSK-3
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Neurological Disease
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BRD1652 is a highly selective GSK3 inhibitor. BRD1652 can be used in the study of emotion-related diseases .
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- HY-134622
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CDK
GSK-3
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Neurological Disease
Cancer
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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 .
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- HY-162675
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GSK-3
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Infection
Neurological Disease
Metabolic Disease
Cancer
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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 .
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- HY-137472
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GSK-3
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Neurological Disease
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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) .
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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 .
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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 .
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- HY-100950
-
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GSK-3
CDK
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Inflammation/Immunology
Cancer
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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 .
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- HY-11012
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GSK-3β inhibitor I; NP 01139
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GSK-3
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Cancer
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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.
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- HY-10182
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CHIR-99021; CT99021
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Organoid
GSK-3
Wnt
β-catenin
Autophagy
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Metabolic Disease
Cancer
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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 .
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- HY-10182B
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CHIR-99021 trihydrochloride; CT99021 trihydrochloride
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Organoid
GSK-3
Wnt
β-catenin
Autophagy
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Cancer
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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 .
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- HY-10182A
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CHIR-99021 monohydrochloride; CT99021 monohydrochloride
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Organoid
GSK-3
Wnt
β-catenin
Autophagy
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Cancer
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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 .
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- HY-10182R
-
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CHIR-99021 (Standard); CT99021 (Standard)
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Organoid
GSK-3
Autophagy
Wnt
β-catenin
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Cancer
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Laduviglusib (Standard) is the analytical standard of Laduviglusib. 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 .
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- HY-151575
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GSK-3
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Infection
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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 .
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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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- HY-N3542
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Glucosidase
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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 .
|
-
- 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 .
|
-
- HY-N12625
-
|
|
CDK
DYRK
GSK-3
|
Cancer
|
|
(R)-(+)-O-Demethylbuchenavianine is an inhibitor for Cyclin-dependent kinases (CDK). (R)-(+)-O-Demethylbuchenavianine inhibits CDK1, CDK5, glycogen synthase kinase-3 (GSK3), cdc2-like kinase (CLK1) and dual specificity tyrosine-phosphorylation-regulated kinase 1A (DYRK1A), with IC50s of 1.1, 0.95, >10, >10 and >10 μM, respectively .
|
-
- 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 .
|
-
- 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) .
|
-
- 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 .
|
-
- HY-10512S
-
-
- HY-15438
-
|
|
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.
|
-
- HY-W969907
-
|
|
Others
|
Others
|
|
GSK3a-IN-38 is a groundbreaking small molecule that effectively inhibits GSK-3a activity.
|
-
- HY-149845
-
|
|
GSK-3
PROTACs
|
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 .
|
-
- HY-161751
-
|
|
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
|
-
- HY-117194
-
|
|
HIV
GSK-3
|
Infection
|
|
18BIOder is a neuroprotective GSK-3β inhibitor, highly selectively inhibiting HIV-1 .
|
-
- HY-161667
-
|
|
GSK-3
HDAC
|
Neurological Disease
|
|
GSK-3β/HDAC-IN-1 (Compd 4) is a brain-penetrant and first in class dual non-ATP-competitive Glycogen Synthase Kinase 3β/Histone Deacetylases (GSK-3β/HDACs) Inhibitor with IC50s of 0.142, 0.03 and 0.045 μM against GSK-3β, HDAC2 and HDAC6, respectively. GSK-3β/HDAC-IN-1 can be used for Alzheimer’s disease research .
|
-
- HY-151260
-
|
|
Beta-secretase
Cholinesterase (ChE)
GSK-3
|
Neurological Disease
|
|
AChE/BACE1/GSK3β-IN-1 is an orally active triple inhibitor of AChE/BACE1/GSK3β. AChE/BACE1/GSK3β-IN-1 has effective inhibitory activity against AChE, BACE1 and GSK3β with IC50 values of 1.0 μM, 20 μM and 15 μM, respectively. AChE/BACE1/GSK3β-IN-1 has good blood-brain barrier penetrability, suitable bioavailability. AChE/BACE1/GSK3β-IN-1 can be used for the research of Alzheimer's disease (AD) .
|
-
- HY-12292
-
IM-12
5 Publications Verification
|
GSK-3
|
Cancer
|
|
IM-12 is an inhibitor of GSK-3β, with an IC50 of 53 nM, and also enhances Wnt signalling.
|
-
- HY-136679
-
|
|
GSK-3
|
Neurological Disease
Metabolic Disease
|
|
TD114-2 (cmpound 29) is a potent and highly selective inhibitor of glycogen synthase kinase-3β (GSK-3β) (IC50=48 nM). TD114-2 is associated with the hydrogen bond formation of arginine 141 (ARG141) specific to GSK-3β, an amino acid that is often a negatively charged residue in other kinases, which determines the high selectivity of GSK-3β. TD114-2 can be used in the study of diabetes, neurodegenerative diseases and other diseases associated with GSK-3β .
|
-
- HY-10590
-
-
- HY-117822
-
|
|
GSK-3
|
Neurological Disease
|
|
BRD0209 is a potent, selective and dual inhibitor of GSK3α/β inhibitor (GSK3α IC50 = 19 nM; GSK3β IC50 = 5 nM). BRD0209 is also a reversible ATP-competitive inhibitor with fast-off kinetics (Ki = 4.2 nM, respectively). BRD0209 is a tricyclic pyrazolotetrahydroquinolinone compound. BRD0209 has the potential for the research of mood disorder diseases .
|
-
- HY-110074
-
|
|
Others
|
Others
|
|
TWS119 TFA is a specific inhibitor of GSK-3β, with an IC50 of 30 nM, and activates the wnt/β-catenin pathway.
|
-
- HY-12524
-
Bikinin
1 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.
|
-
- HY-B0320A
-
-
- 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 .
|
-
- HY-119940
-
|
(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 .
|
-
- HY-124607B
-
BRD3731
1 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 .
|
-
- 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 .
|
-
- HY-133102
-
|
Lycoraminone
|
GSK-3
|
Neurological Disease
|
|
Dihydronarwedine (Lycoraminone) is the alkaloid. Dihydronarwedine inhibits 39% activity of glycogen synthase kinase-3β (GSK-3β) at a concentration of 10 μM .
|
-
- HY-161595
-
|
|
CDK
GSK-3
|
Cancer
|
|
CDK5-IN-4 (compound 4) is a potent multikinase type-II inhibitor targeting CDK5, with an IC50 of 9.8 μM. CDK5-IN-4 also inhibits GSK-3α, GSK-3β, CDK9, and CDK2, with IC50 values of 0.98, 4.00, 1.76, and 6.24 μM, respectively. CDK5-IN-4 can be used for glioblastoma research .
|
-
- HY-150537
-
|
|
Cholinesterase (ChE)
GSK-3
Microtubule/Tubulin
ROS Kinase
|
Neurological Disease
|
|
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 .
|
-
- 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 .
|
-
- HY-144316
-
|
|
Cholinesterase (ChE)
GSK-3
|
Neurological Disease
|
|
ZLWH-23 is a selective AChE inhibitor (IC50=0.27 μM) with GSK-3β inhibitory property (IC50=6.78 μM). ZLWH-23 possesses selectivity for AChE over BChE (IC50=20.82 μM) and for GSK-3β over multi-kinases. ZLWH-23 has the potential for the research of Alzheimer's disease .
|
-
- HY-59090
-
-
- HY-116830
-
BRD0705
1 Publications Verification
|
GSK-3
|
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 .
|
-
- HY-100207
-
CP21R7
5 Publications Verification
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.
|
-
- HY-151375
-
|
|
Others
|
Cancer
|
|
CDK9/10/GSK3β-IN-1 (compound 13c) is a kinase inhibitor (Flavopiridol (HY-10005) analogue) that effectively inhibits HsGSK3β (IC50=59 nM), HsCDK9/CyclinT (IC50=64 nM), HsCDK5/p25 (IC50=1.093 µM) and HsCDK2/CyclinA (IC50=1.725 µM). CDK9/10/GSK3β-IN-1 has anti-cancer cellular activity comparable to or higher than that of Flavopiridol. CDK9/10/GSK3β-IN-1 shows high anti-proliferative activity in vitro against up to seven cancer cell lines .
|
-
- HY-111931
-
|
|
CDK
GSK-3
|
Cancer
|
|
Indirubin-3'-monoxime-5-sulphonic acid is a potent and selective inhibitor of CDK1, CDK5, and GSK-3β with IC50s of 5 nM, 7 nM, and 80 nM, respectively .
|
-
- HY-B0320AR
-
|
Disodium Cromoglycate (Standard); FPL-670 (Standard)
|
Calcium Channel
GSK-3
|
Inflammation/Immunology
|
|
Cromolyn (sodium) (Standard) is the analytical standard of Cromolyn (sodium). This product is intended for research and analytical applications. Cromolyn sodium (Disodium Cromoglycate; FPL-670) is an antiallergic agent. Cromolyn sodium is a GSK-3β inhibitor with an IC50 of 2.0 μM.
|
-
- 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 .
|
-
- HY-116830A
-
|
|
GSK-3
|
Cancer
|
|
(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) .
|
-
- HY-116830B
-
|
(R)-BRD0705
|
GSK-3
|
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) .
|
-
- HY-10182G
-
|
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.
|
-
- HY-77493
-
|
(rel)-ARQ 197; (rel)-(3R,4R)-ARQ 198
|
Others
|
Cancer
|
|
(rel)-Tivantinib is a potent and highly selective inhibitor of the receptor tyrosine kinase c-MET. (rel)-Tivantinib has two novel targets, GSK3α and GSK3β, which play an important role in the cellular mechanism of non-small cell lung cancer (NSCLC) .
|
-
- 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 .
|
-
- 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 .
|
-
- 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 .
|
-
- HY-107529
-
|
|
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 .
|
-
- 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 .
|
-
- HY-19807
-
|
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.
|
-
- HY-117025A
-
|
Keramamine A hydrochloride
|
GSK-3
CDK
Parasite
Proton Pump
HSV
Autophagy
|
Infection
Neurological Disease
Cancer
|
|
Manzamine A hydrochloride, an orally active beta-carboline alkaloid, inhibits specifically GSK-3β and CDK-5 with IC50s of 10.2 μM and 1.5 μM, respectively. Manzamine A hydrochloride targets vacuolar ATPases and inhibits autophagy in pancreatic cancer cells. Manzamine A hydrochloride has antimalarial and anticancer activities. Manzamine A hydrochloride also shows potent activity against HSV-1 .
|
-
- HY-117025
-
|
Keramamine A
|
GSK-3
CDK
Parasite
Proton Pump
HSV
Autophagy
|
Infection
Neurological Disease
Cancer
|
|
Manzamine A, an orally active beta-carboline alkaloid, inhibits specifically GSK-3β and CDK-5 with IC50s of 10.2 μM and 1.5 μM, respectively. Manzamine A targets vacuolar ATPases and inhibits autophagy in pancreatic cancer cells. Manzamine A has antimalarial and anticancer activities. Manzamine A also shows potent activity against HSV-1 .
|
-
- HY-50687
-
|
(3S,4S)-ARQ 197; ARQ 198
|
Others
|
Cancer
|
|
(3S,4S)-Tivantinib is a potent and highly selective inhibitor of the receptor tyrosine kinase c-MET. (3S,4S)-Tivantinib has two novel targets, GSK3α and GSK3β, which play an important role in the cellular mechanism of non-small cell lung cancer (NSCLC) .
|
-
- HY-10514
-
|
|
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 .
|
-
- HY-108359
-
|
9-Nitropaullone; NSC 705701
|
CDK
GSK-3
Apoptosis
|
Cancer
|
|
Alsterpaullone (9-Nitropaullone) is a potent CDK inhibitor, with IC50s of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also competes with ATP for binding to GSK-3alpha/GSK-3beta with IC50s of both 4 nM. Alsterpaullone has antitumor activity, and possesses potential for the study in neurodegenerative and proliferative disorders . Alsterpaullone induces apoptosis in leukemia cell line .
|
-
- HY-145669
-
DIF-3
1 Publications Verification
|
CDK
GSK-3
|
Cancer
|
|
DIF-3 reduces the expression levels of cyclin D1 and c-Myc by facilitating their degradation via activation of GSK-3β. DIF-3 inhibits Wnt/β-catenin signaling pathway-related proteins in DLD-1 cells. DIF-3 exerts a strong antiproliferative effect on the human cervical cancer cell line HeLa by inducing cyclin D1 degradation and inhibiting cyclin D1 mRNA expression .
|
-
- HY-N6973
-
Boldine
1 Publications Verification
|
RANKL/RANK
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Boldine is an apomorphine isoquinoline alkaloid extracted from the root of the pheasant pepper (Litsea cubeba). Boldine is an oral effective antioxidant, anti-inflammatory, antitumor agent, and can inhibit osteoclast formation. Boldine induces apoptosis of human bladder cancer cells by regulating ERK, AKT and GSK-3β. Boldine ameliorates bone destruction by down-regulating the OPG/RANKL/RANK signaling pathway. It can be used in rheumatoid arthritis research .
|
-
- HY-131447
-
KY19382
1 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 .
|
-
- HY-12302
-
|
9-Bromopaullone; NSC-664704
|
CDK
GSK-3
|
Cancer
|
|
Kenpaullone is a potent inhibitor of CDK1/cyclin B and GSK-3β, with IC50s of 0.4 μM and 23 nM, and also inhibits CDK2/cyclin A, CDK2/cyclin E, and CDK5/p25 with IC50s of 0.68 μM, 7.5 μM, 0.85 μM, respectively. Kenpaullone, a small molecule inhibitor of KLF4, reduces self-renewal of breast cancer stem cells and cell motility in vitro.
|
-
- HY-113914
-
|
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 .
|
-
- HY-145244
-
|
|
Akt
|
Cancer
|
|
APN/AKT-IN-1 is a potent and dual inhibitor of APN and AKT with IC50s of 0.21 and 0.27 μM, respectively. APN/AKT-IN-1 can effectively inhibit the phosphorylation of GSK3β, the intracellular substrate of AKT .
|
-
- HY-15504A
-
|
|
CDK
GSK-3
MEK
JAK
|
Cancer
|
|
RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
|
-
- HY-15504
-
|
|
CDK
GSK-3
MEK
JAK
|
Cancer
|
|
RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
|
-
- HY-136848
-
|
|
MAP3K
Src
FGFR
Ribosomal S6 Kinase (RSK)
LIM Kinase (LIMK)
|
Cancer
|
|
SM1-71 (compound 5) is a potent TAK1 inhibitor, with a Ki of 160 nM, it also can covalently inhibit MKNK2, MAP2K1/2/3/4/6/7, GAK, AAK1, BMP2K, MAP3K7, MAPKAPK5, GSK3A/B, MAPK1/3, SRC, YES1, FGFR1, ZAK (MLTK), MAP3K1, LIMK1 and RSK2. SM1-71 can inhibit proliferation of multiple cancer cell lines .
|
-
- HY-18676
-
|
|
Integrin
Autophagy
Apoptosis
|
Cancer
|
|
OSU-T315 (ILK-IN-1) is a small Integrin-linked kinase (ILK) inhibitor with an IC50 of 0.6 μM, inhibiting PI3K/AKT signaling by dephosphorylation of AKT-Ser473 and other ILK targets (GSK-3β and myosin light chain) . OSU-T315 abrogates AKT activation by impeding AKT localization in lipid rafts and triggers caspase-dependent apoptosis in an ILK-independent manner . OSU-T315 causes cell death through apoptosis and autophagy .
|
-
- HY-111932
-
|
|
CDK
GSK-3
|
Cancer
|
|
Indirubin-5-sulfonate is a cyclin-dependent kinase (CDK) inhibitor, with IC50 values of 55 nM, 35 nM, 150 nM, 300 nM and 65 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK4/cyclin D1, and CDK5/p35, respectively . Indirubin-5-sulfonate also shows inhibitory activity against GSK-3β .
|
-
- HY-W140760
-
|
|
Others
|
Infection
Inflammation/Immunology
Cancer
|
|
Ceftriaxone sodium is a versatile broad-spectrum β-lactam tertiary cephalosporin antibiotic that exhibits anti-inflammatory, antitumor, antibacterial, and antioxidant properties, and functions as a covalent inhibitor of GSK3β and Aurora B, making it valuable in research related to sepsis and infective endocarditis.
|
-
- HY-N1472
-
|
|
Apoptosis
Reactive Oxygen Species
PPAR
GSK-3
Tau Protein
Ras
TGF-β Receptor
|
Infection
Neurological Disease
Inflammation/Immunology
|
|
Levistolide A is an apoptosis inducer and a PEDV virus inhibitor. Levistolide A can induce apoptosis in colon cancer cells and suppress the replication of porcine epidemic diarrhea virus (PEDV) by promoting ROS generation. Levistolide A activates peroxisome proliferator-activated receptor γ (PPARγ) in N2a/APP695swe cells and reduces excessive phosphorylation of tau through the GSK3α/β pathway, improving symptoms in Alzheimer’s mice. Levistolide A improves kidney damage in 5/6 nephrectomy (Nx) mice by inhibiting the RAS,TGF-β1/Smad, and MAPK pathways .
|
-
- HY-126771
-
|
Chr-A
|
Antibiotic
Bacterial
Akt
GSK-3
β-catenin
c-Myc
|
Infection
Cancer
|
|
Chrysomycin A (Chr-A), an antibiotic, can be obtained from Streptomyces. Chrysomycin A exhibits antitumor and anti-tuberculous and MRSA activities. As for glioblastoma, Chrysomycin A inhibits the proliferation, migration, and invasion of cancer cells through the Akt/GSK-3β/β-catenin signaling pathway .
|
-
- HY-112700
-
|
|
Phosphatase
|
Neurological Disease
|
|
SHIP2-IN-1 is a potent SHIP2 inhibitor, inhibits SHIP2 activity, with an IC50 of 2 µM. SHIP2-IN-1 blocks GSK3β activation by phosphorylation at the Ser9 residue. SHIP2-IN-1 is used in the research of Alzheimer’s disease .
|
-
- HY-139324
-
|
|
GSK-3
Amyloid-β
|
Neurological Disease
Cancer
|
|
Cu(II)GTSM, a cell-permeable Cu-complex, significantly inhibits GSK3β. Cu(II)GTSM inhibits Amyloid-β oligomers (AβOs) and decreases tau phosphorylation. Cu(II)GTSM also decreases the abundance of Amyloid-β trimers. Cu(II)GTSM is a potential anticancer and antimicrobial agent .
|
-
- HY-W094474
-
|
hydrate/monohydrateortrihydrate
|
GSK-3
Apoptosis
|
Infection
Neurological Disease
|
|
Lithium chloride hydrate, an orally active mood stabilizer, is a potent virus inhibitor and effective immunomodulatory agent. Lithium chloride hydrate has antidepressant activity by inhibiting GSK3β and promoting neurogenesis. Lithium chloride hydrate alleviates cognition dysfunction and the symptoms of acute mania and depression. Lithium chloride hydrate can also be used for research of virus infection and Alzheimer's disease .
|
-
- HY-10012
-
|
|
CDK
|
Cancer
|
|
AZD-5438 is a potent CDK1, CDK2, and CDK9 inhibitor, with IC50s of 16 nM, 6 nM, and 20 nM in cell-free assays, respectively. AZD-5438 shows less inhibition activity against GSK3β, CDK5 and CDK6
.
|
-
- HY-101569
-
|
LXS196; IDE196
|
PKC
|
Cancer
|
|
Darovasertib (LXS196) is a potent, selective and orally active protein kinase C (PKC) inhibitor, with IC50 values of 1.9 nM, 0.4 nM and 3.1 μM for PKCα, PKCθ and GSK3β, respectively. Darovasertib has the potential for uveal melanoma research .
|
-
- HY-108264
-
|
NIBR3049
|
JAK
PKC
GSK-3
|
Cancer
|
|
TCS 21311 (NIBR3049) is a potent, highly selective JAK3 inhibitor with an IC50 of 8 nM, it displays >100-fold selectivity over JAK1, JAK2 and TYK2. TCS 21311 (NIBR3049) inhibits PKCα, PKCθ, and GSK3β with IC50s of 13, 68, and 3 nM, respectively .
|
-
- HY-103381
-
|
|
CDK
GSK-3
|
Cancer
|
|
NSC693868 is a selective inhibitor of CDK1 and CDK5 with IC50s of 600 nM and 400 nM, respectively. NSC693868 less potently inhibits GSK3β with an IC50 of 1 µM) and does not block CDC25 activity. NSC693868 is used to help define the roles of CDK1 and CDK5 in various signaling pathways .
|
-
- HY-161362
-
|
|
PI3K
|
Cancer
|
|
SR-3-65 (compound 6) is a Indisulam (HY-13650) derivative,and inhibits the migration of gastric cancer cells. SR-3-65 attenuates PI3K/AKT/GSK-3β/β-catenin signaling pathway .
|
-
- HY-158017
-
|
|
PI3K
|
Cancer
|
|
WXM-1-170 (compound 10) is a Indisulam (HY-13650) derivative,and inhibits the migration of gastric cancer cells. WXM-1-170 attenuates PI3K/AKT/GSK-3β/β-catenin signaling pathway .
|
-
- HY-137894A
-
|
PF-07104091 hydrate
|
CDK
GSK-3
|
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).
|
-
- HY-121983
-
|
|
Phospholipase
|
Cancer
|
|
CAY10594 is a potent phospholipase D2 (PLD2) inhibitor both in vitro (IC50=140 nM) and in cells (IC50=110 nM) . CAY10594 strongly inhibits the invasive migration of breast cancer cells in vitro and ameliorates acetaminophen-induced acute liver injury by regulating the phosphorylated-GSK-3β/JNK axis .
|
-
- HY-155366
-
|
|
Cholinesterase (ChE)
GSK-3
|
Neurological Disease
|
|
hAChE-IN-6 (compound 51) is a brain penetrant AChE inhibitor with an IC50 of 0.16 μM. hAChE-IN-6 also inhibits hBuChE and GSK3β with IC50 values of 0.69 μM and 0.26 μM, respectively. hAChE-IN-6 inhibits tau protein and Aβ1-42 self-aggregation, and can be used for Alzheimer's disease (AD) research .
|
-
- HY-108442
-
JW67
1 Publications Verification
|
Wnt
|
Cancer
|
|
JW67 inhibits the canonical Wnt signaling with an IC50 of 1.17μM . JW67 affects the multiprotein complex consisting of β-catenin/GSK-3β/AXIN/APC/CK1 that rapidly reduces active β-catenin with a subsequent downregulation of Wnt target genes. JW67 also inhibits colorectal cancer cell growth .
|
-
- HY-128221
-
|
|
SGK
|
Inflammation/Immunology
|
|
SGK1-IN-5 (Compound 1) is an inhibitor for serum and glucocorticoid regulated kinase SGK 1 with an IC50 of 3 nM. SGK1-IN-5 inhibits SGK-1 dependent phosphorylation of GSK3β in U2OS cells with an IC50 of 1.4 μM. SGK1-IN-5 can be used in research about osteoarthritis or rheumatism .
|
-
- HY-149143
-
|
|
TRP Channel
|
Inflammation/Immunology
|
|
JNJ-28583113 is an TRPM2 antagonist with brain permeability. JNJ-28583113 inhibits TRPM2 blocked phosphorylation of GSK3α and β subunits. JNJ-28583113 protects cells from oxidative stress induced cell death. JNJ-28583113 also suppresses cytokine release in response to pro-inflammatory stimuli in microglia .
|
-
- HY-129492
-
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) .
|
-
- HY-143898
-
|
|
Pim
|
Cancer
|
|
PIM1-IN-4 (Compound 8) is a potent inhibitor of PIM1. PIM1-IN-4 reveals strong inhibition of five other enzymes, i.e., SGK-1, PKA, CaMK-1, GSK3β, and MSK1. PIM1-IN-4 has the potential for the research of cancer diseases .
|
-
- HY-112809
-
|
|
Syk
Src
LRRK2
GSK-3
JAK
VEGFR
Aurora Kinase
|
Inflammation/Immunology
|
|
GSK2646264 (Compound 44) is a potent and selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.1. GSK2646264 also inhibits other kinases with pIC50 values of 5.4, 5.4, 5.3, 5, 4.5, <4.6 and <4.3 against LCK, LRRK2, GSK3β, JAK2, VEGFR2, Aurora B and Aurora A, respectively. GSK2646264 is penetrable into the epidermis and dermis of the skin .
|
-
- HY-N6064
-
|
|
Apoptosis
IAP
|
Cancer
|
|
Polygalacin D (PGD) is a bioactive compound isolated from Platycodon grandiflorum with anticancer and anti-proliferative properties.
PGD suppresses the expression of the IAP family of proteins including survivin, cIAP-1 and cIAP-2 and blocks the PI3K/Akt pathway by inhibiting the phosphorylation of GSK3β, Akt and the expression of PI3K. Polygalacin D induces apoptosis
|
-
- HY-B0712
-
|
Ro 13-9904 free acid
|
Bacterial
Antibiotic
GSK-3
Aurora Kinase
|
Infection
Inflammation/Immunology
Cancer
|
|
Ceftriaxone (Ro 13-9904 free acid) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone is a covalent inhibitor of GSK3β with IC50 value of 0.78 μM. Ceftriaxone is an inhibitor of Aurora B. Ceftriaxone has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone can be used in the study of bacterial infections and meningitis .
|
-
- HY-B0712A
-
|
Ro 13-9904 sodium hydrate
|
Bacterial
Antibiotic
GSK-3
Aurora Kinase
|
Infection
Cancer
|
|
Ceftriaxone sodium hydrate (Ro 13-9904 sodium hydrate) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone sodium hydrate is a covalent inhibitor of GSK3β with IC50 value of 0.78 μM. Ceftriaxone sodium hydrate is an inhibitor of Aurora B. Ceftriaxone sodium hydrate has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone sodium hydrate can be used in the study of bacterial infections and meningitis .
|
-
- HY-B0712B
-
|
Ro 13-9904
|
Antibiotic
GSK-3
Bacterial
Aurora Kinase
|
Infection
Inflammation/Immunology
Cancer
|
|
Ceftriaxone sodium salt (Ro 13-9904) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone sodium salt is a covalent inhibitor of GSK3β with IC50 value of 0.78 μM. Ceftriaxone sodium salt is an inhibitor of Aurora B. Ceftriaxone sodium salt has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone sodium salt can be used in the study of bacterial infections and meningitis .
|
-
- HY-142295
-
|
|
DYRK
|
Metabolic Disease
|
|
GNF2133 is a potent, selective and orally active DYRK1A inhibitor with IC50s of 0.0062, >50 µM for DYRK1A and GSK3β, respectively. GNF2133 shows good proliferation potency and efficacy on rat and human primary β-cell. GNF2133 significantly improves glucose disposal capacity and increases insulin secretion. GNF2133 has the potential for the research of type 1 diabetes .
|
-
- HY-142295A
-
|
|
DYRK
|
Metabolic Disease
|
|
GNF2133 hydrochloride is a potent, selective and orally active DYRK1A inhibitor with IC50s of 0.0062, >50 µM for DYRK1A and GSK3β, respectively. GNF2133 hydrochloride shows good proliferation potency and efficacy on rat and human primary β-cell. GNF2133 hydrochloride significantly improves glucose disposal capacity and increases insulin secretion. GNF2133 hydrochloride has the potential for the research of type 1 diabetes .
|
-
- HY-155705
-
|
|
TGF-β Receptor
GSK-3
β-catenin
|
Others
|
|
BMP agonist 1 (compound 2 b) is a small-molecule agonist of bone morphogenic protein (BMP). BMP induces C2C12 cell differentiation with BMP and highly depends on active BMP signaling. BMP agonist 1 inhibits GSK3β, increases β-catenin signaling and synergistically regulates Id2and Id3 expression. BMP agonist 1 is used in diseases and defects of the skeleton research .
|
-
- HY-135366
-
|
|
IKK
|
Inflammation/Immunology
|
|
HPN-01 is a potent and selective IKK inhibitor, with pIC50 values of 6.4, 7.0 and <4.8 for IKK-α, IKK-β and IKK-ε, respectively. HPN-01 displays greater 50-fold selectivity over a panel of more than 50 other kinases, including ALK5, CDK-2, EGFR, ErbB2, GSK3β, PLK1, Src, and VEGFR-2 .
|
-
- HY-13866
-
|
Ro 31-8220 methanesulfonate; Bisindolylmaleimide IX mesylate
|
PKC
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Ro 31-8220 mesylate is a potent PKC inhibitor, with IC50s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC50s, 3, 8, 15, and 38 nM, respectively), with no effect on MKK3, MKK4, MKK6 and MKK7.
|
-
- HY-13866A
-
|
Bisindolylmaleimide IX
|
PKC
|
Cardiovascular Disease
Neurological Disease
|
|
Ro 31-8220 is a potent PKC inhibitor, with IC50s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC50s, 3, 8, 15, and 38 nM, respectively), with no effect on MKK3, MKK4, MKK6 and MKK7.
|
-
- HY-10256
-
Adezmapimod
Maximum Cited Publications
453 Publications Verification
SB 203580; RWJ 64809
|
Organoid
p38 MAPK
Autophagy
Mitophagy
|
Inflammation/Immunology
Cancer
|
|
Adezmapimod (SB 203580) is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod does not disrupt JNK activity and is an autophagy and mitophagy activator .
|
-
- HY-10256A
-
|
SB 203580 hydrochloride; RWJ 64809 hydrochloride
|
Organoid
p38 MAPK
Autophagy
Mitophagy
|
Inflammation/Immunology
Cancer
|
|
Adezmapimod (SB 203580; RWJ 64809) hydrochloride is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod hydrochloride inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod hydrochloride does not disrupt JNK activity and is an autophagy and mitophagy activator .
|
-
- HY-B0712AR
-
|
|
Bacterial
Antibiotic
GSK-3
Aurora Kinase
|
Infection
Cancer
|
|
Ceftriaxone (sodium hydrate) (Standard) is the analytical standard of Ceftriaxone (sodium hydrate). This product is intended for research and analytical applications. Ceftriaxone sodium hydrate (Ro 13-9904 sodium hydrate) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone sodium hydrate is a covalent inhibitor of GSK3β with IC50 value of 0.78 μM. Ceftriaxone sodium hydrate is an inhibitor of Aurora B. Ceftriaxone sodium hydrate has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone sodium hydrate can be used in the study of bacterial infections and meningitis .
|
-
- HY-163896
-
|
|
β-catenin
|
Cancer
|
|
β-Catenin modulator-7 (Compound 5) is a modulator for β-catenin. β-Catenin modulator-7 inhibits the expression of β-catenin in HCT-116 cytoplasm and nucleus, suppresses the phosphorylation of GSK 3β. β-Catenin modulator-7 promotes NO release in HCT-116, and inhibits the proliferation of cancer cell HCT-116 with IC50 of 0.6-0.9 μM. β-Catenin modulator-7 can be used in reasearch about colon cancer .
|
-
- HY-139254
-
|
IDR3O; I3O
|
CDK
GSK-3
JNK
|
Neurological Disease
|
|
Indirubin-3′-oxime (IDR3O), a synthetic derivative of indirubin, is a potent inhibitor of cyclin-dependent kinases (CDKs) and glycogen synthase kinase 3β (GSK3β). Indirubin-3′-oxime directly inhibits the activity of all three isoforms of JNK (JNK1, JNK2, and JNK3), with IC50s of 0.8 μM, 1.4 μM, and 1.0 μM, respectively. Indirubin-3′-oxime can enhance height growth via activation of Wnt/β-catenin signaling in chondrocytes .
|
-
- HY-N7676
-
Marein
1 Publications Verification
|
AMPK
HDAC
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
|
|
Marein has the neuroprotective effect due to a reduction of damage to mitochondria function and activation of the AMPK signal pathway. Marein improves insulin resistance induced by high glucose in HepG2 cells through CaMKK/AMPK/GLUT1 to promote glucose uptake, through IRS/Akt/GSK-3β to increase glycogen synthesis, and through Akt/FoxO1 to decrease gluconeogenesis. Marein is a HDAC inhibitor with an IC50 of 100 µM. Marein has beneficial antioxidative, antihypertensive, antihyperlipidemic and antidiabetic effects .
|
-
- HY-126049
-
|
(S)-(-)-Oxiracetam; (S)-ISF2522
|
Apoptosis
|
Neurological Disease
|
|
(S)-oxiracetam (S-ORC) is an inhibitor targeting apoptosis. S-ORC reduces brain infarct size and lessens neurological dysfunction in middle cerebral artery occlusion/reperfusion (MCAO/R) models. S-ORC prevents neuronal apoptosis via activating PI3K/Akt/GSK3β signaling pathway via α7 nAChR after ischemic stroke. S-ORC can prevent neuronal death after ischemic stroke .
|
-
- HY-155365
-
|
|
Cholinesterase (ChE)
GSK-3
Amyloid-β
|
Neurological Disease
|
|
hAChE-IN-5 (compound 49) is a potent hAChE and hBuChE inhibitor with IC50 values of 0.17 μM and 0.17 μM, respectively. hAChE-IN-5 shows potent GSK3β inhibition with an IC50 value of 0.21 μM. hAChE-IN-5 is used as tau protein aggregation and Aβ1-42 self-aggregation inhibitor. hAChE-IN-5 can bind virtually with the PAS affecting Aβ aggregation, thus preventing Aβ-dependent neurotoxicity. hAChE-IN-5 can penetrate BBB and has the potential for multi-targeted anti-Alzheimer's agents research .
|
-
- HY-121035
-
|
7-Bromoindirubin-3-Oxime
|
CDK
GSK-3
|
Neurological Disease
|
|
7BIO (7-Bromoindirubin-3-Oxime) is the derivate of indirubin. 7BIO (7-Bromoindirubin-3-Oxime) has inhibitory effects against cyclin-dependent kinase-5 (CDK5) and glycogen synthase kinase-3β (GSK3β). 7BIO (7-Bromoindirubin-3-Oxime) inhibits Aβ oligomer-induced neuroinflammation, synaptic impairments, tau hyper-phosphorylation, activation of astrocytes and microglia, and attenuates Aβ oligomer-induced cognitive impairments in mice [1].
|
-
- HY-B0712S1
-
|
Ro 13-9904-13C2,d3 triethylammonium salt
|
Antibiotic
Aurora Kinase
GSK-3
Bacterial
Isotope-Labeled Compounds
|
Infection
Inflammation/Immunology
Cancer
|
|
Ceftriaxone- 13C2,d3 triethylammonium salt is 13C and deuterated labeled Ceftriaxone (HY-B0712). Ceftriaxone (Ro 13-9904 free acid) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone is a covalent inhibitor of GSK3β with IC50 value of 0.78 mM. Ceftriaxone is an inhibitor of Aurora B. Ceftriaxone has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone can be used in the study of bacterial infections and meningitis .
|
-
- HY-164476
-
|
|
EGFR
GSK-3
PD-1/PD-L1
|
Cancer
|
|
ES-072 is an orally effective selective EGFR mutant (EGFR-T790M) inhibitor. ES-072 activates GSK3α by inhibiting EGFR-T790M activity, which promotes phosphorylation of PD-L1 at Ser279 and Ser283. The phosphorylated PD-L1 recruits the E3 ubiquitin ligase ARIH1, leading to ubiquitination and proteasomal degradation of PD-L1. This mechanism not only reduces cancer cell growth but also enhances anti-tumor immune response by lowering PD-L1 levels. ES-072 can be used to inhibit proliferation in non-small cell lung cancer (NSCLC) cells .
|
-
- HY-124068
-
|
|
Apoptosis
GSK-3
MMP
Reactive Oxygen Species
|
Infection
Inflammation/Immunology
Cancer
|
LQB-118 is an orally active compound derived from sandalwood. LQB-118 can inhibit the migration of glioblastoma cells and induce cell death. LQB-118 can suppress the migration and invasion of prostate cancer cells by regulating the AKT/GSK3β pathway and the expression of the MMP-9/reck genes. LQB-118 can also inhibit yeast polysaccharide-induced inflammation both in vivo and in vitro. Additionally, LQB-118 selectively induces ROS-triggered and mitochondrial-dependent apoptosis in Leishmania amazonensis. LQB-118 can be used in studies related to inflammation, infections, and cancer diseases .
|
-
-
-
HY-L020
-
|
|
377 compounds
|
|
The developmental proteins Hedgehog, Notch and Wnt are key regulators of cell fate, proliferation, migration and differentiation in several tissues. Their related signaling pathways are frequently activated in tumors, and particularly in the rare subpopulation of cancer stem cells.
The Wnt signaling pathway is a conserved pathway in animals. Deregulated Wnt signaling has catastrophic consequences for the developing embryo and it is now well appreciated that defective Wnt signaling is a causative factor for a number of pleiotropic human pathologies, including cancer. Hedgehog signaling pathway is linked to tumorigenesis and is aberrantly activated in a variety of cancers. The Notch signaling pathway is a highly conserved cell signaling system present in most animals. It plays an important role in cell-cell communication, and further regulates embryonic development.
MCE designs a unique collection of 377 Wnt/Hedgehog/Notch signaling pathway-related small molecules. Wnt/Hedgehog/Notch Compound Library serves as a useful tool for stem cell research and anti-cancer drug screening.
|
-
-
HY-L017
-
|
|
1,870 compounds
|
|
Adult stem cells are important for tissue homeostasis and regeneration due to their ability to self-renew and generate multiple types of differentiated daughters. Self-renewal is reflected by their capacity to undergo multiple/limitless divisions. Several signaling pathways are involved in self-renewal of stem cells, that is, Notch, Wnt, and Hedgehog pathways or Polycomb family proteins. Recent studies mainly focus on cancer stem cell (CSCs), induced pluripotent stem cell (iPSCs), neural stem cell and maintenance of embryonic stem cell pluripotency. Among them, CSCs have been believed to be responsible for tumor initiation, growth, and recurrence that have implications for cancer therapy.
MCE owns a unique collection of 1,870 compounds that can be used for stem cell regulatory and signaling pathway research.
|
| Cat. No. |
Product Name |
Type |
-
- HY-10182G
-
|
CHIR-99021 (GMP); CT99021 (GMP)
|
Fluorescent Dye
|
|
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.
|
| Cat. No. |
Product Name |
Type |
-
- HY-10182G
-
|
CHIR-99021 (GMP); CT99021 (GMP)
|
Biochemical Assay Reagents
|
|
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.
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- 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 .
|
-
- 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 .
|
-
- HY-P10605
-
|
|
Akt
GSK-3
|
Cancer
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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 .
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Chemical Structure |
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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)[1].
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- HY-B0712S1
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Ceftriaxone- 13C2,d3 triethylammonium salt is 13C and deuterated labeled Ceftriaxone (HY-B0712). Ceftriaxone (Ro 13-9904 free acid) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone is a covalent inhibitor of GSK3β with IC50 value of 0.78 mM. Ceftriaxone is an inhibitor of Aurora B. Ceftriaxone has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone can be used in the study of bacterial infections and meningitis .
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