GSK-3

GSK-3β inhibitor, potent

Mast cell membrane stabilizer

WAY-119064 is a potent glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC50 value of 80.5 nM.

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, with IC50s of 9, 20 and 25 nM, respectively.

GSK-3 inhibitor 1 is an inhibitor of GSK-3.

GSK-3β inhibitor 1 (compound 3a) is a glycogen synthase kinase 3β (GSK-3β) inhibitor and demonstrates high antidiabetic efficacy, with an IC50 of 4.9 nM.

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

Indirubin-5-sulfonate is a cyclin-dependent kinase (CDK) inhibitor, with IC50 values of 55 nM, 35 nM, 150 nM, 300 nM and 65 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK4/cyclin D1, and CDK5/p35, respectively. Indirubin-5-sulfonate also shows inhibitory activity against GSK-3β.

A multi-kinase inhibitor

A multi-kinase inhibitor

VP3.15 is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE)7- glycogen synthase kinase (GSK)3 inhibitor, with IC50s of 1.59 μM and 0.88 μM for PDE7 and GSK-3, respectively.

VP3.15 dihydrobromide is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE)7- glycogen synthase kinase (GSK)3 inhibitor, with IC50s of 1.59 μM and 0.88 μM for PDE7 and GSK-3, respectively.

GNF4877 is a potent DYRK1A and GSK3β inhibitor with IC50s of 6?nM and 16?nM, respectively, which leads to blockade of nuclear factor of activated T-cells (NFATc) nuclear export and increased β-cell proliferation (EC50 of 0.66?μM for mouse β (R7T1) cells).

BIP-135 is a potent and selective ATP-competitive GSK-3 inhibitor, with IC50s of 16 nM and 21 nM for GSK-3α and GSK-3β, respectively.

9-ING-41 is a selective and potent GSK-3β inhibitor with an IC 50 value of 0.71μM.

BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50 of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML) research.

Phospho-Glycogen Synthase Peptide-2 (substrate) is peptide substrate?for glycogen synthase kinase-3 (GSK-3) and can be used for affinity purification of protein-serine kinases.

GSK-3β inhibitor 11 (compound 21) is a glycogen synthase kinase-3β (GSK-3β) inhibitor (IC50=10.02 μM). GSK-3β inhibitor 11 can be used in neurodegenerative disease research.

GSK3-IN-1 (compound 11) is a GSK-3 inhibitor with an IC50 value of 12 μM. GSK3-IN-1 can be used in the research of diabetes.

ABC1183 is a selective dual inhibitor of GSK3 and CDK9 with oral activity. Its IC50 values for GSK3β, GSK3α, and CDK9/cyclin T1 are 657 nM, 327 nM, and 321 nM respectively. ABC1183 has anti-inflammatory properties as well as anti-tumor activity.

BRD0209 is an effective, selective, and dual inhibitor of GSK3α/β (GSK3α IC50 = 19 nM; GSK3β IC50 = 5 nM). It is also a reversible ATP-competitive inhibitor with fast kinetics (Ki values of 4.2 nM for both isoforms). BRD0209 is a tricyclic pyrazolone-fused tetrahydroquinoline compound. It has potential in researching mood disorders.

GSK3-IN-3 is a mitophagy inducer that can induce Parkin-dependent mitochondrial autophagy. It is also a GSK-3 inhibitor with an IC50 value of 3.01 μM. GSK3-IN-3 has non-ATP and non-substrate competitive properties and has neuroprotective effects on 6-OHDA.