GSK-3α Inhibitor

Laduviglusib (CHIR-99021) is a potent, selective and orally active GSK-3α/β inhibitor with IC₅₀s of 10 nM and 6.7 nM. Laduviglusib shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. Laduviglusib is also a potent Wnt/β-catenin signaling pathway activator. Laduviglusib enhances mouse and human embryonic stem cells self-renewal. Laduviglusib induces autophagy.

LY2090314 is a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC₅₀ values of 1.5 nM and 0.9 nM for GSK-3α and GSK-3β, respectively.

SB 216763 is potent, selective and ATP-competitive GSK-3 inhibitor with IC₅₀s of 34.3 nM for both GSK-3α and GSK-3β.

Laduviglusib (CHIR-99021) monohydrochloride is a potent and selective GSK-3α/β inhibitor with IC₅₀s of 10 nM and 6.7 nM. Laduviglusib monohydrochloride shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. Laduviglusib monohydrochloride is also a potent Wnt/β-catenin signaling pathway activator. Laduviglusib monohydrochloride enhances mouse and human embryonic stem cells self-renewal. Laduviglusib monohydrochloride induces autophagy.

Laduviglusib (CHIR-99021) trihydrochloride is a potent and selective GSK-3α/β inhibitor with IC₅₀s of 10 nM and 6.7 nM. Laduviglusib trihydrochloride shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. Laduviglusib trihydrochloride is also a potent Wnt/β-catenin signaling pathway activator. Laduviglusib trihydrochloride enhances mouse and human embryonic stem cells self-renewal. Laduviglusib trihydrochloride induces autophagy.

Multitarget AD-IN-7 is an orally active multi-target anti-AD compound. Multitarget AD-IN-7 exhibits inhibitory activity against GSK-3β and GSK-3α (IC₅₀ = 0.66, 0.83 nM). Multitarget AD-IN-7 upregulates the expression of p-GSK-3β-Ser9, inhibits the phosphorylation of tau-Ser396, targets Aβ_1-42, chelates pathogenic metal ions, scavenges ABTS•+, upregulates the expression of β-catenin and neurogenesis biomarkers, and promotes neurite outgrowth. Multitarget AD-IN-7 improves motor ability in Alzheimer's disease zebrafish. Multitarget AD-IN-7 is applicable to research related to Alzheimer's disease.

BiS3 is a selective hyperbivalent macrocyclic peptide GSK3β inhibitor, with a K_d of 0.28 nM and an IC₅₀ of 4.8 nM against GSK3β. BiS3 is applicable to studies related to GSK3β signaling and colorectal cancer.

GSK 3 Inhibitor IX (6-Bromoindirubin-3'-oxime; BIO) is a potent, selective, reversible and ATP-competitive inhibitor of GSK-3α/β and CDK1-cyclinB complex with IC₅₀s of 5 nM/320 nM/80 nM for (GSK-3α/β)/CDK1/CDK5, respectively.

Laduviglusib (CHIR-99021) (GMP) is Laduviglusib (HY-10182) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Laduviglusib is a potent, orally active and selective GSK-3α/β inhibitor.

AZD2858 is a potent, orally active GSK-3 inhibitor, with IC₅₀s of 0.9 and 5 nM for GSK-3α and GSK-3β, respectively, used in the research of fracture healing.

CHIR-98014 is a potent, cell-permeable GSK-3 inhibitor with IC₅₀s of 0.65 and 0.58 nM for GSK-3α and GSK-3β, respectively; it shows less potent activities against cdc2 and erk2.

SLK/STK10-IN-1 is a potent and selective inhibitor of SLK and STK10 with antitumor activity.

AZD1080 is a potent and selective GSK3 inhibitor. AZD1080 inhibits recombinant human GSK3α and GSK3β with pK_i (IC₅₀) of 8.2 (6.9 nM) and 7.5 (31 nM), respectively.

BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC₅₀ of 66 nM and a K_d 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.

R547 is a potent, selective and orally active ATP-competitive CDK inhibitor, with K_is of 2 nM, 3 nM and 1 nM for CDK1/cyclin B, CDK2/cyclin E and CDK4/cyclin D1, respectively.

Alsterpaullone (9-Nitropaullone) is a potent CDK inhibitor, with IC₅₀s of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also competes with ATP for binding to GSK-3alpha/GSK-3beta with IC₅₀s of both 4 nM. Alsterpaullone has antitumor activity, and possesses potential for the study in neurodegenerative and proliferative disorders. Alsterpaullone induces apoptosis in leukemia cell line.

SB 415286 is a potent and selective cell permeable inhibitor of GSK-3α, with an IC₅₀ of 77.5 nM, and a K_i of 30.75 nM; SB 415286 is equally effective at inhibiting human GSK-3α and GSK-3β.

BIO-acetoxime (BIA) is a potent and selective GSK-3 inhibitor, with IC₅₀s of both 10 nM for GSK-3α/β. BIO-acetoxime has anticonvulsant and anti-infection activity.

PF-04802367 (PF-367) 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. PF-04802367 shows desirable central nervous system (CNS) properties and potency. PF-04802367 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.

A 1070722 is a potent and selective glycogen synthase kinase 3 (GSK-3) inhibitor, with a K_i of 0.6 nM for both GSK-3α and GSK-3β. A 1070722 can penetrate the blood-brain barrier (BBB) and accumulates in brain regions, thus potential for PET radiotracer for the quantification of GSK-3 in brain. A 1070722 decreases spontaneous locomotion.