GSK-3β

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.

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 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.

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.

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.

Citric acid trilithium salt tetrahydrate (Lithium citrate tribasic tetrahydrate) , the active component of Lithium, is a medicine used in the therapy of psychiatric disease. It has shown the effects of signaling pathways and metabolic in the brain based on the particular disease and clinical condition model. According to the reports, Citric acid trilithium salt tetrahydrate was used as a mood stabilizer when treating bipolar mood disorders (BD) and lower the risk of self-harm in BD patient. In addition,Citric acid trilithium salt tetrahydrate has been the choice drug in the therapy of acute manic episodes.Citric acid trilithium salt tetrahydrate also could dissolve uric acid crystals in urine achieved from patients with gout. Besides,Citric acid trilithium salt tetrahydrate have some dose-dependent side-effects. The the main side-effects of Lithium Citrate is the tendency to inhibit the prostatic acid phosphatase enzyme (PAP), which result in the accumulation of PAP.

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

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.

TBB (NSC-231634)(NSC-231634) is a highly selective, ATP GTP-competitive inhibitor of casein kinase-2 (CK2).

AT7519 is a CDK1 2 4 6 9 inhibitor (IC50: 10-210 nM). It is less effective to CDK3 and little active to CDK7.

PHA-767491 (CAY10572) is a potent ATP-competitive dual Cdc7 CDK9 inhibitor with IC50 of 10 nM and 34 nM, respectively.

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

A-443654, a pan-Akt inhibitor, exhibits equal potency against Akt1, Akt2, and Akt3 within cells (Ki=160 pM).

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.

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

GSK-3β inhibitor20 (compound 3A) is an effective inhibitor of GSK-3β, exhibiting an IC50 value of 74.4 nM.

GSK-3β inhibitor22 (compound 20o) is a GSK-3β inhibitor with an IC50 of 3.1 nM, showing potential for Alzheimer's disease research.

hAChE hBuChE GSK-3β-IN-1 (Compound 6c) is a multi-target compound designed for Alzheimer's treatment capable of crossing the blood-brain barrier. It inhibits hAChE with an IC50 of 28.88 nM, hBuChE with an IC50 of 131.90 nM, and GSK-3β with an IC50 of 51.42 nM. Additionally, it acts as an inhibitor of tau protein and Aβ protein aggregation.

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.

GSK-3β inhibitor24 (Compound 41) is a potent GSK-3β inhibitor with an IC50 of 0.22 nM. It increases GSK-3β phosphorylation at the Ser9 site in a dose-dependent manner and inhibits tau protein hyperphosphorylation by reducing the abundance of p-tau-Ser396. The compound upregulates β-catenin and neurogenesis-related markers (GAP43 and MAP-2), demonstrating significant anti-Alzheimer's disease (AD) activity.

GSK-3β inhibitor25 (Compound 6h) exhibits weak inhibitory activity against GSK-3β with an IC50 greater than 100 μM.

GSK-3β inhibitor26 (Compound D14) is a GSK-3β inhibitor with an IC50 of 18.23 μM. This compound is applicable in research related to cancer, inflammation, and neurodegenerative diseases.

CHIR-98014 (CT98014) is a selective GSK3 inhibitor; potentiate insulin activation of glucose transport and utilization in vitro and in vivo.