glycogen synthase kinase 3

RIP2 Kinase Inhibitor 3 is a potent and selective inhibitor of RIP2 with an IC50 of 1 nM.

Phospho-Glycogen Synthase Peptide-2, a substrate for glycogen synthase kinase-3 (GSK-3), serves as a peptide substrate effective in the affinity purification of protein-serine kinases.

Phospho-Glycogen Synthase Peptide-2 (substrate) serves as a peptide substrate for glycogen synthase kinase-3 (GSK-3) and is utilized for the affinity purification of protein-serine kinases [1].

Chitin Synthase Inhibitor 3 (Compound 2d) is a potent inhibitor of chitin synthase, exhibiting an IC50 value of 0.16 mM and demonstrating antifungal activity with a minimum inhibitory concentration (MIC) of 1 μg/mL against Candida albicans [1].

[Glycogen Synthase (1-12) Ala9,10, Lys11,12] is a selective substrate for protein kinase C (PKC) phosphorylation. It serves to assess PKC activity [1].

Multi-kinase-IN-3 (compound 2) is a potent inhibitor of angiokinase and inhibits VEGFR-2 (IC50: 58.3 nM) and PDGFRβ (IC50: 55 nM).

MET kinase-IN-3 is a potent, orally active MET inhibitor (IC50: 9.8 nM) that exhibits good broad-spectrum anti-proliferative effects on cancer cells.

TIE-2/VEGFR-2 kinase-IN-3, a benzimidazole derivative, serves as a potent inhibitor of the tyrosine kinase receptors TIE-2 and VEGFR-2, exhibiting IC50 values of 6.9 nM and 3.5 nM, respectively. This compound is useful for angiogenesis research [1].

Aurora kinase inhibitor-3 (Aurora Kinase Inhibitor III) is a potent inhibitor of Aurora A kinase (IC50 = 42 nM).1 It is selective for Aurora A over BMX, BTK, IGF-1R, c-Src, TRKB, SYK, and EGFR.

Polyketide synthase 13-IN-3 (compound 41) is a potent inhibitor of polyketide synthase 13, demonstrating a minimum inhibitory concentration (MIC) range of 0.0625-0.125 μg/mL against the M. tuberculosis strain H37Rv.

Casein kinase 1δ-IN-3 (Casein kinase 1δ-IN-3) (Compound 23a) is a casein kinase 1 delta (CK1d) inhibitor with a pIC50 of 6.5376 M.

Pim-1 kinase inhibitor 3 (Compound H5) is a potent inhibitor of Pim-1 kinase, demonstrating an inhibitory concentration (IC50) of 35.13 nM [1].

Glucosylceramide synthase-IN-3 (compound BZ1) is a highly potent, brain-penetrant, and orally active inhibitor of glucosylceramide synthase (GCS), exhibiting an IC50 value of 16 nM for human GCS. This compound, designated as Glucosylceramide synthase-IN-3, finds potential applications in Gaucher's disease research [1] [2].

IRE1α kinase-IN-3 is a potent, ATP-competitive inhibitor of IRE1α (Ki: 480 nM).

Casein Kinase Substrates 3 is a substrate of casein kinase.

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.

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).

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

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.

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.

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

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

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.

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.

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

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

hAChE-IN-5 (compound 49) is a dual inhibitor of human acetylcholinesterase (hAChE) and human butyrylcholinesterase (hBuChE), exhibiting inhibitory potency with IC50 values of 0.17 μM for both enzymes. Additionally, it demonstrates potent glycogen synthase kinase 3 beta (GSK3β) inhibition with an IC50 of 0.21 μM. The compound is an effective inhibitor of tau protein and Aβ1-42 peptide self-aggregation. It can virtually bind the peripheral anionic site (PAS), preventing amyloid-beta (Aβ)-induced neurotoxicity. hAChE-IN-5's ability to cross the blood-brain barrier (BBB) underpins its utility in the development of multitargeted anti-Alzheimer’s agents [1].

6-Me-ATP (N6-Methyl-ATP), a N6-modified adenosine triphosphate (ATP) derivative, exhibits strong binding affinity for glycogen synthase kinase 3 (GSK3) and acts as the phosphate group donor in GSK3β-catalyzed phosphorylation of its substrate peptide [1].

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.

hAChE-IN-6 (compound 51) is a brain-penetrant acetylcholinesterase (AChE) inhibitor exhibiting an IC50 of 0.16 μM. It also demonstrates inhibitory effects on human butyrylcholinesterase (hBuChE) and glycogen synthase kinase 3 beta (GSK3β), with IC50 values of 0.69 μM and 0.26 μM, respectively. Additionally, hAChE-IN-6 impedes the self-aggregation of tau protein and amyloid-beta 1-42 (Aβ1-42), rendering it useful for Alzheimer's disease (AD) research [1].

Crosstide is a peptide analog of glycogen synthase kinase-3 (GSK-3) that functions as a natural substrate for Akt/PKB.

5-bromoindole is a potential inhibitor of glycogen synthase kinase 3 (GSK-3)and an important pharmaceutical chemical intermediate

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

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.

TDZD-8 (NP 01139) is an inhibitor of GSK-3β, with an IC50 of 2 μM; minimal inhibitory effect observed on CDK1, casein kinase II, PKA and PKC.

A 1070722 is a potent and selective GSK-3 inhibitor, with a Ki of 0.6 nM for both GSK-3α and GSK-3β. It can penetrate the blood-brain barrier (BBB) and accumulates in brain regions, thus potential for PET radiotracer for the quantification of GSK-3 in bra

KY19382 (2H-Indol-2-one, 5,6-dichloro-3-[1,3-dihydro-3-(methoxyimino)-2H-indol-2-ylidene]-1,3-dihydro-Ky19382) is a potent and orally active dual inhibitor of CXXC5-DVL and GSK3β( IC50s of 19 and 10 nM, respectively). It activates Wnt/β-catenin signaling through inhibitory effects on both CXXC5-DVL interaction and GSK3β activity. KY19382 can be used for the research of high fat diet (HFD) induced metabolic diseases.

Cazpaullone is an inhibitor of glycogen synthase kinase-3 (GSK-3). It also shows transient stimulation of the mRNA expression of the beta cell transcription factor Pax4.

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.

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

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.

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

MeBIO is an agonist of aryl hydrocarbon receptor, with IC50 of 44 and 55 μM for GSK-3 and CDK1/CyclinB, respectively. MeBIO does not affect GSK-3β.

Alsterpaullone is a Cyclin-Dependent Kinase Inhibitor, Mediated Toxicity in HeLa Cells Through Apoptosis-Inducing Effec

PIMPC, a compound endowed with antioxidant and metal-chelating properties, acts as a novel inhibitor of glycogen synthase kinase 3 (GSK-3), and exhibits potential therapeutic effects for Alzheimer's disease [1].

IM-12, an effective GSK-3β inhibitor(IC50=53 nM), regulates Wnt signalling.