gsk-3β

GSK-3 inhibitor 1 is a GSK-3 inhibitor.

GSK-3 Inhibitor 5 (4-Cyanophenacyl bromide) is a ketone derivative that is used as an intermediate in pharmaceuticals and organic synthesis, and inhibits glycogen synthase kinase 3 (GSK-3).

GSK-3 inhibitor 3 is a selective, orally active, brain-permeable GSK-3 inhibitor that inhibits GSK-3α and GSK-3β with IC50s of 0.35 nM and 0.25 nM, respectively.GSK-3 inhibitor 3 reduces the phosphorylation level of tau protein S396 with an IC50 of 10 nM in a triple transgenic mouse model of Alzheimer's disease. GSK-3 inhibitor 3 reduced the phosphorylation level of tau protein S396 in a triple transgenic mouse model of Alzheimer's disease, with an IC50 of 10 nM.GSK-3 inhibitor 3 can be used for the study of neurological diseases.

GSK-3 inhibitor 4 is an orally active and brain-permeable compound that acts as a triple inhibitor of GSK-3, CDK2, and CDK5, with IC50 values of 0.56 nM (GSK-3β), 0.45 nM (GSK-3α), 0.47 μM (CDK2), and 0.68 μM (CDK5). It effectively reduces Tau protein levels and can be used in the study of Alzheimer's disease.

GSK-3 Inhibitor XIII, an ATP-competitive GSK-3 inhibitor (Ki: 24 nM), can be used to study diabetes and obesity.

GSK-3β inhibitor 3 is a potent, selective, and irreversible covalent inhibitor of glycogen synthase kinase 3β (GSK-3β) with an IC50 of 6.6 μM, and can be used to study acute promyelocytic leukemia.

GSK-3 CDK5 CDK2-IN-1 is an imidazole derivative compound that inhibits cdk5, cdk2, and GSK-3.it has demonstrated applications in cancer research and the study of neurodegenerative diseases [1].

GSK-3β inhibitor 12 is a selective GSK-3β inhibitor.GSK-3β inhibitor 12 inhibits 49.11% of 25 μM GSK-3β activity and 37.11% of 50 μM GSK-3β activity.GSK-3β inhibitor 12 can be used for the study of Parkinson's in the presence of lipopolysaccharide induction.

GSK-3β inhibitor 8 (GSK3β Inhibitor XVIII) is a potent and selective GSK-3β inhibitor with an IC50 value of 64 nM.GSK-3β inhibitor 8 is a thienopyrimidine derivative that negatively regulates the Wnt signaling pathway and stimulates β-cell proliferation.

AR-A014418 (GSK 3β inhibitor VIII) is an ATP-competitive, and selective GSK3β inhibitor.

GSK 3 Inhibitor IX (6-BIO) is a selective reversible, ATP-competitive inhibitor of GSK-3α/β and CDK1-cyclinB complex. It inhibits (GSK-3α/β)/CDK1/CDK5 activity with IC50 values of 5 nM/320 nM/83 nM, respectively.

GSK-3β inhibitor 10 has skin-whitening, anti-oxidizing and PPAR activities.

GSK-3β inhibitor 1 is an inhibitor of GSK-3β( IC50 of 4.9 nM) and demonstrates high antidiabetic efficacy.

(E Z)-GSK-3β inhibitor 1 is a glycogen synthase kinase 3β (GSK-3β) inhibitor demonstrating high antidiabetic efficacy.

GSK-3β inhibitor 14 (1,5-Benzothiazepin-4(5H)-one, 2,3-dihydro-2-methyl-5-(phenylmethyl)-) is a weak GSK-3β inhibitor, IC50﹥ 100μM.

TDZD-8 (NP 01139) is an inhibitor of GSK-3β, with an IC50 of 2 μM; minimal inhibitory effect observed on CDK1, casein kinase II, PKA and PKC.

GSK-3β inhibitor 15 (Compound 54), with an IC50 of 3.4 nM, effectively suppresses Aβ 1-42-induced phosphorylation of GSK-3β and tau protein, as well as LPS-induced iNOS expression, demonstrating neuroprotective properties against Aβ 1-42-induced neurotoxicity and indicating potential utility in Alzheimer's disease (AD) research [1].

GSK-3β inhibitor 11 (compound 21) is a potent glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC50 of 10.02 μM, demonstrating potential utility in neurodegenerative disease research [1].

GSK-3β inhibitor 6 is a highly potent inhibitor of GSK-3β with an IC50 value of 24.4 μM, significantly enhancing hepatocyte glucose uptake (38%). This compound holds great potential for studying diseases such as diabetes, inflammation, cancer, Alzheimer's disease, and bipolar disorder [1].

GSK-3β inhibitor 7 is a GSK-3β inhibitor (IC50: 5.25 μM) that acts by inserting into the ATP-binding pocket of GSK-3β and forming hydrogen bonds. It exhibits a high rate of glucose uptake by hepatocytes (83.5%) and can be used to study various diseases such as cancer, diabetes, inflammation, Alzheimer's disease, and bipolar disorder.

AChE/GSK-3β-IN-1 is a potent dual AChE/GSK-3β inhibitor that crosses the blood-brain barrier and acts on hAChE (IC50: 1.2 nM), hBChE (IC50: 149.8 nM) and hGSK-3β (IC50: 22.4 nM). AChE/GSK-3β-IN-1 is able to occupy the ATP binding site of DYRK1A. aChE/GSK-3β-IN-1 exhibits high kinase selectivity for the CMGC kinase family. aChE/GSK-3β-IN-1 inhibits ROS expression and reduces oxidative stress. aChE/GSK-3β-IN-1 can be used to study Alzheimer's disease.

GSK-3β inhibitor 2 (5-Thiazolecarboxamide,2-[2-[(cyclopropylcarbonyl)amino]-4-pyridinyl]-4-methoxy-) is a BBB-crossing and selective inhibitor of GSK-3β (IC50 = 1.1 nM). GSK-3β inhibitor 2 can be used in studies about Alzheimer's disease.

GSK-3β Inhibitor 17 (compound 5 n) reduces the expression of p-p65 and KIM-1 proteins in a dose-dependent manner (16, 32, 64 µM) induced by cisplatin. Additionally, at a concentration of 32 µM, it decreases the levels of TNF-α, IL-1β, IL-6, and MCP-1 mRNA in an acute kidney injury (AKI) model of HK-2 cells triggered by cisplatin.

GSK J5 HCl is the hydrochloride form of GSK J5. GSK J5 is an inactive isomer of GSK J4 and a cell-permeable ester derivative of inactive control GSK J2.

CHIR-99021 (CT99021) is an activator of the Wnt/β-catenin signaling pathway and a GSK-3α/β inhibitor (IC50=10/6.7 nM) with selective and oral activity.CHIR-99021 induces cellular autophagy, which enhances self-renewal in mouse and human embryonic stem cells.

GNF4877 is a potent inhibitor of DYRK1A and GSK3β (IC50s: 6 nM and 16 nM, respectively), resulting in the blockade of nuclear export of nuclear factor of activated T-cells (NFATc) and increased β-cell proliferation.

EHT 1610 (EHT 5372) is a potent inhibitor of DYRK, with an IC50 of 0.36 nM and 0.59 nM for DYRK1A and DYRK1B, respectively. EHT 1610 has an inhibitory effect on leukemia, regulating cell cycle and inducing cell apoptosis.

3F8 is a selective GSK-3β inhibitor that can be used as a new tool and potential therapeutic candidate compound for GSK3-related diseases, and can be used in the study of neurological disorders and cancer.

Cromolyn sodium (FPL-670) is a chromone complex that acts by inhibiting the release of chemical mediators from sensitized mast cells.

A-674563 2HCl is an Akt1 inhibitor with Ki of 11 nM, modest potent to PKA and >30-fold selective for Akt1 over PKC.

A-674563 is an orally available, ATP-competitive, and reversible inhibitor of Akt (Ki: 11 nM for Akt1) [1]. It exhibits inhibitory activity against PKA and Cdk2 (IC50: 16 46 nM) but is 10- to >1, 800-fold selective for Akt1 versus additional kinases in th

MBM-55S is an effective inhibitor of Nek2 with an IC50 of 1 nM. MBM-55S indecus cell cycle arrest and apoptosis thereby inhibiting the proliferation of cancer cells. MBM-55S shows antitumor activities.

CDK8-IN-12 is a selective, potent and orally active inhibitor of CDK8 (Ki: 14 nM) and is an anti-cancer agent. CDK8-IN-12 inhibits GSK-3α, GSK-3β and PCK-θ with Ki of 13 nM, 4 nM and 109 nM respectively. CDK8-IN-12 showed anti-proliferative activity against MV4-11 cells.

GSK3-IN-4 is a GSK-3 inhibitor with IC50 of 0.101-1 μM of GSK-3α and GSK-3β in Calipe Assay.

ARN25068 is a potent inhibitor of GSK-3β, FYN, and DYRK1A protein kinases, exerting its activity in the sub-micromolar range. This compound effectively addresses tau hyperphosphorylation [1].

5-Iodo-indirubin-3'-monoxime is a potent inhibitor of GSK-3β, CDK5 P25, and CDK1 cyclin B, competing with ATP for binding to the catalytic site of the kinase (IC50s: 9, 20, and 25 nM).

Tideglusib (NP031112), a non-ATP competitive inhibitor of glycogen synthase kinase 3 (GSK-3), is with anti-inflammatory and neuroprotective activities.

CAY10594 is a potent phospholipase D2(PLD2) inhibitor. CAY10594 ameliorates acetaminophen-induced acute liver injury by regulating the phosphorylated-GSK-3β JNK axis.

KenPaullone (9-Bromopaullone), a potent CDK1, CDK2 and CDK5 inhibitor, as new enhancer for iTreg cell differentiation. Kenpaullone promotes iTreg cell differentiation through increased and prolonged transcription of foxp3 gene by enhancing TGFβ-Smad3 signaling pathway.

Adezmapimod (SB 203580) is a selective, ATP-competitive p38 MAPK inhibitor (IC50=0.3-0.5 μM) that activates autophagy and mitochondrial autophagy, with more than 100-fold higher selectivity over PKB, LCK, and GSK-3β.

AZD1080 is a selective, orally active, brain permeable GSK3 inhibitor.

SB 216763 (SB216763) is an effective and specific GSK-3α/β inhibitor (IC50: 34.3 nM).

DIF-3 is a chemical compound that acts by activating GSK-3β to facilitate the degradation of cyclin D1 and c-Myc, resulting in reduced expression levels of these proteins. In addition, DIF-3 inhibits Wnt β-catenin signaling pathway-related proteins in DLD-1 cells. This compound exerts a potent antiproliferative effect on the HeLa human cervical cancer cell line by inducing cyclin D1 degradation and inhibiting cyclin D1 mRNA expression [1].

Isolongifolene ((-)-Isolongifolene), a tricyclic sesquiterpene isolated from Murraya koenigii, exhibits antioxidant, anti-inflammatory, anticancer, and neuroprotective properties. It mitigates Rotenone-induced oxidative stress, mitochondrial dysfunction, and apoptosis by modulating the PI3K AKT GSK-3β signaling pathways.

Marein shows neuroprotective effect on PC12 cell damage induced by methylglyoxal, which is due to a reduction of damage to mitochondria function and activation of the AMPK signal pathway, it may be a potent compound for preventing counteracting diabetic e

AT7519 Hydrochloride (AT7519 HCl) is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9.

KY19382 (2H-Indol-2-one, 5,6-dichloro-3-[1,3-dihydro-3-(methoxyimino)-2H-indol-2-ylidene]-1,3-dihydro-Ky19382) is a potent and orally active dual inhibitor of CXXC5-DVL and GSK3β( IC50s of 19 and 10 nM, respectively). It 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.

A 1070722 is a potent and selective GSK-3 inhibitor, exhibiting high affinity for both GSK-3α (Ki = 0.6 nM) and GSK-3β (Ki = 0.6 nM). It can penetrate the blood-brain barrier (BBB) and accumulate in brain regions, indicating potential use as a PET radiotracer for quantifying GSK-3 in the brain.