GSK 3β inhibitor 3

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 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.

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.

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).

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.

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.

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

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.

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

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

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

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.

BRD0705 is a potent, orally active GSK3α inhibitor with high selectivity (IC50: 66 nM; Kd: 4.8 μM), demonstrating an 8-fold higher selectivity for GSK3α compared to GSK3β (IC50: 515 nM).

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

Indirubin-3'-monoxime-5-sulphonic acid is a potent and selective inhibitor of GSK-3β, CDK5, and CDK1, with IC50s of 80 nM, 5 nM, and 7 nM, respectively.

9-ING-41 is a glycogen synthase kinase-3 inhibitor.

BIP-135 is a potent and selective ATP-competitive GSK-3 inhibitor, with IC50 values of 16 nM and 21 nM for GSK-3α and GSK-3β, respectively, and exhibits neuroprotective effects [1].

TCS 21311 (NIBR3049) is an effective and highly selective inhibitor of JAK3 (IC50: 8 nM). TCS 21311 inhibits PKCα, PKCθ, and GSK3β (IC50s: 13, 68, and 3 nM, respectively). It displays >100-fold selectivity over JAK1, JAK2, and TYK2.

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

LY2090314, an effective GSK-3α/β inhibitor (IC50: 1.5 nM/0.9 nM), may improve the efficacy of platinum-based chemotherapy regimens. LY2090314 has been used in trials studying the treatment of Leukemia, Advanced Cancer, and Pancreatic Cancer.

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

AZD2858 is a selective GSK-3 inhibitor, inhibiting tau phosphorylation at the S396 site and activating Wnt signaling pathway.

TFGF-18 is a GSK-3β inhibitor with an IC50 of 0.59 μM. It suppresses microglial activation and the release of pro-inflammatory mediators induced by LPS by inhibiting GSK-3β and downstream p65 NF-κB signaling. TFGF-18 also prevents neuronal apoptosis and oxidative stress, reduces the expression of Bax, caspase-3, and cleaved-caspase-3, while increasing Bcl-2 expression. It offers neuroprotection by inhibiting neuroinflammation and alleviating cognitive impairment.

GSK-3β inhibitor23 (Compound 11726169) is an inhibitor of glycogen synthase kinase 3 (GSK-3), effectively inhibiting GSK-3β and GSK-3α with IC50 values of 12.1 nM and 18.8 nM, respectively. It demonstrates antiviral activity against HIV1 and exhibits good metabolic stability in mouse and human liver microsomes and plasma, although it has poor permeability in Caco-2 cells, indicating potentially low oral bioavailability.