gsk-3

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

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 triple inhibitor of GSK-3, CDK2 and CDK5 with inhibitory effects on GSK-3β, GSK-3α, CDK2 and CDK5, with IC50 values of 0.56 nM, 0.45 nM, 0.47 μM, 0.68 μM, respectively.GSK-3 inhibitor 4 can effectively reduce Tau protein levels. GSK-3 inhibitor 4 can effectively reduce the level of Tau protein.GSK-3 inhibitor 4 can be used in the study of Alzheimer's disease.

GSK-3 inhibitor 1 is a GSK-3 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 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.

GSK-3β inhibitor 3 is a covalent inhibitor (IC50: 6.6 μM) of glycogen synthase kinase 3β (GSK-3β) that is potent, selective, and irreversible.GSK-3β inhibitor 3 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.

Losmapimod (GSK-AHAB) (GW856553X; SB856553; GSK-AHAB) is a specific, potent, and orally active p38 MAPK inhibitor (pKi: 8.1/7.6 for p38α/β).

GSK 789472 hydrochloride is both a dopamine D3 receptor antagonist and a D2 partial agonist.

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.

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

BIO-acetoxime (GSK-3 Inhibitor X) is a potent dual GSK3α/β inhibitor with IC50 of 10 nM, >240-fold selectivity over CDK5/p25, CDK2/cyclin A and CDK1/cyclin B.

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 and demonstrates high antidiabetic efficacy.

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. It demonstrates neuroprotective properties against Aβ 1-42-induced neurotoxicity, indicating its potential utility in Alzheimer's disease (AD) research [1].

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

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

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

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.

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.

1,1'-(Heptane-1,7-diyl)diguanidine dihydrochloride is a potent and selective small molecule inhibitor of glycogen synthase kinase-3 (GSK-3). It is used in studies of stem cell differentiation, tumors and neurodegenerative diseases.

GS87 is a highly specific inhibitor of GSK3 (glycogen synthase kinase 3) that induces extensive differentiation of AML 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.

4-Chloro-2'-bromoacetophenone against glycogen synthase kinase-3 (GSK-3beta).

(Rac)-BRD0705 is a less active racemate of BRD0705. BRD0705 is an effective and selective inhibitor of GSK3α.

GSK 2833503A is a potent and selective TRPC6 and TRPC3 antagonist (IC50 = 3-16 nM and 21-100 nM, respectively). GSK 2833503A exhibits >63-fold selectivity over other ion channels, including other TRP channels, CaV1.2, hERG and NaV1.5. GSK 2833503A suppresses angiotensin II or endothelin-1-induced cardiac hypertrophy signaling in HEK293 cellsin vitroand in cardiomyocytes.

GSK2292767 is a potent and selective PI3Kδ inhibitor.This compound is unstable in powder form and other related salt forms are recommended.

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 (IC50s: 9, 20 and 25 nM).

R547 (Ro 4584820) is a potent ATP-competitive inhibitor of CDK1/2/4 with Ki of 2 nM/3 nM/1 nM. It is less potent to CDK7 and GSK3α/β, while inactive to other kinases. Phase 1.

GSK840 (GSK'840) is a receptor-interacting protein kinase 3 (RIP3 or RIPK3) inhibitor, which binds the RIP3 kinase domain (IC50: 0.9 nM), and inhibits kinase activity (IC50: 0.3 nM).

1. Linarin (Acacetin-7-O-rutinoside) (acacetin-7-O-β-d-rutinoside) shows selective dose dependent inhibitory effect on acetylcholinesterase. 2. Linarin alleviates GalN/LPS-induced liver injury by suppressing TNF-α-mediated apoptotic pathways. 3. Linarin prevents A beta-induced neurotoxicity through the activation of PI3K/Akt, which subsequently inhibits GSK-3b and up-regulates Bcl-2. 4. The piperine significantly enhanced the oral absorption of Linarin in rats by inhibiting P-glycoprotein mediated cellular efflux during the intestinal absorption and likely simultaneously by inhibiting the metabolism of Linarin.

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

CHIR-99021 HCl (Laduviglusib HCl) is a highly potent and selective inhibitor of GSK-3α/β, with IC50 values of 10 nM and 6.7 nM respectively. It demonstrates remarkable selectivity for GSK-3, with over 500-fold selectivity over CDC2, ERK2, and other protein kinases. Additionally, CHIR-99021 HCl serves as a robust activator of the Wnt/β-catenin signaling pathway. Moreover, it exhibits the ability to enhance self-renewal in both mouse and human embryonic stem cells. Furthermore, CHIR-99021 HCl induces autophagy [1] [2] [3].

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

GSK-690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. Phase 1.

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].

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

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.

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

GSK-LSD1, an LSD1 inhibitor, decreases food consumption and body weight while enhancing insulin sensitivity and glycemic regulation in murine obesity models. Additionally, it mitigates non-alcoholic fatty liver disease (NAFLD) and suppresses cytokine release induced by SARS-CoV-2 in COVID-19 peripheral blood mononuclear cells (PBMCs). Furthermore, GSK-LSD1 inhibits the proliferation and spread of cancer [1] [2] [3].

FRATtide inhibits the phosphorylation of Axin and β-catenin, inhibits GSK-3 binding to Axin, and is a peptide derived from the GSK-3 binding protein.

GSK3-IN-1 is a GSK3B-glycogen synthase kinase-3 beta inhibitor.

Manzamine A is a GSK-3 inhibitor and vacuolar ATPase uncoupler found in marine sponges. It inhibits autophagy and tumor growth in cancer models, suppresses foam cell formation in macrophages, prevents growth of gram negative and gram positive bacteria, an

GSK3β inhibitor II is a GSK3β inhibitor. GSK3β inhibitor II exhibits the research potential of Alzheimer's disease (AD).

PF-04802367 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. It shows desirable central nervous system (CNS) properties and potency. It 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.