gsk-3 β

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.

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.

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.

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.

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

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

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).

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).

SNS-032 (BMS-387032) is a selective inhibitor of CDK2 (IC50: 48 nM), exhibiting 10- and 20-fold selectivity over CDK1 and CDK4, respectively. It is also sensitive to CDK7 (IC50: 62 nM) and CDK9 (IC50: 4 nM), with no effect on CDK6.

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.

GSK3a-IN-38 is a novel small molecule compound that has inhibitory effects on GSK-3a.

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

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

CHIR 98024 is a potent GSK-3α β inhibitor with IC50 of 0.65 nM 0.58 nM in cell-free assays, with the ability to distinguish GSK-3 from its closest homologs Cdc2 and ERK2.

1-Azakenpaullone (azakenpaullone) is a potent and selective GSK-3β inhibitor with IC50 of 18 nM, >100-fold selectivity over CDK1 cyclin B and CDK5 p25.

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.

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.

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