Signaling Pathway

GSK-3

GSK-3

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GSK-3 (Glycogen synthase kinase 3) is a serine/threonine protein kinase that mediates the addition of phosphate molecules onto serine and threonine amino acid residues. In mammals GSK-3 is encoded by two known genes, GSK-3 alpha (GSK3A) and GSK-3 beta (GSK3B). GSK-3 has recently been the subject of much research because it has been implicated in a number of diseases, including Type II diabetes (Diabetes mellitus type 2), Alzheimer's Disease, inflammation, cancer, and bipolar disorder. Phosphorylation of a protein by GSK-3 usually inhibits the activity of its downstream target. GSK-3 is active in a number of central intracellular signaling pathways, including cellular proliferation, migration, inflammation and immune responses, glucose regulation, and apoptosis.

GSK-3 Inhibitors & Modulators (20)

Product Name Catalog No. Brief Description
AR-A014418

HY-10512

AR-A014418 is a selective and effective GSK3β inhibitor with an IC50 value of 104 +/- 27 nM; no significant inhibition on 26 other kinases.

AZD1080

HY-13862

AZD1080 is a selective, orally active, brain permeable GSK3 inhibitor of GSK3α and GSK3β with Ki of 6.9 nM and 31 nM, respectively, shows >14-fold selectivity against CDK2, CDK5, CDK1 and Erk2.

AZD2858

HY-15761

AZD2858 is a selective GSK-3 inhibitor with an IC50 of 68 nM, inhibits tau phosphorylation at the S396 site, activates Wnt signaling pathway.

Bikinin

HY-12524

Bikinin(Abrasin) is a potent inhibitor of plant GSK-3/Shaggy-like kinase; activates BR signaling downstream of the BR receptor.

BIO

HY-10580

6-BIO(6-Bromoindirubin-3'-oxime) is a potent and selective inhibitor of GSK-3 and CDK1–cyclinB complex with IC50 of 5 nM /320 nM/83 nM for GSK-3αβ/CDK1/CDK5 respectively.

CHIR-98014

HY-13076

CHIR-98014 is a selective GSK3 inhibitor with IC50s of 0.65 nM and 0.58 nM for GSK-3α and GSK-3β; potentiate insulin activation of glucose transport and utilization in vitro and in vivo.

CHIR-99021

HY-10182

CHIR-99021 (CT99021) is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM; > 500-fold selectivity for GSK-3 versus its closest homologs CDC2 and ERK2, as well as other protein kinases.

CHIR-99021 monohydrochloride

HY-10182A

CHIR-99021 monohydrochloride (CT99021) is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM; > 500-fold selectivity for GSK-3 versus its closest homologs CDC2 and ERK2, as well as other protein kinases.

CHIR-99021 trihydrochloride

HY-10182B

CHIR-99021 trihydrochloride (CT99021) is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM; > 500-fold selectivity for GSK-3 versus its closest homologs CDC2 and ERK2, as well as other protein kinases.

CP21R7

HY-100207

CP21R7 is a potent and selective GSK-3β inhibitor.

GSK-3 inhibitor 1

HY-13973A

GSK-3 inhibitor 1 is a potent GSK-3 inhibitor.

IM-12

HY-12292

IM-12 is a potent GSK-3β inhibitor with IC50 of 53 nM; shows a significant activity in several biological tests which was comparable or even outplayed the effects of the known SB-216763.

Indirubin-3'-monoxime

HY-19807

Indirubin-3'-monoxime is a powerful inhibitor of GSK-3β with IC50 of 22nM, also inhibits CDK1/5 (IC50 = 180/100 nM).

Kenpaullone

HY-12302

Kenpaullone is an ATP-competitive inhibitor of several CDKs as well as GSK-3β, with an IC50 value of 0.23 μM for GSK-3β and 0.4, 0.68, 0.85, and 0.47 μM for CDK1/cyclin B, CDK2/cyclin A, CDK5/p25, and lymphocyte kinase.

LY2090314

HY-16294

LY2090314  is a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50s of 1.5 nM and 0.9 nM for GSK-3α and GSK-3β respectively.

SB 216763

HY-12012

SB 216763 is potent and selective glycogen synthase kinase-3 (GSK-3) inhibitor (Ki = 9 nM); competes with ATP.

SB 415286

HY-15438

SB 415286 is a potent and selective cell-permeable, ATP-competitive inhibitor of GSK3α with an IC50 value of 78 nM (similar potency for GSK3β) and a Ki value of 31 nM.

TDZD-8

HY-11012

TDZD-8(NP 01139) is a selective inhibitor of GSK-3, a thiadiazolidinone derivative, non-ATP competitive inhibitor of GSK-3β (IC50 = 2 μM); does not inhibit Cdk-1/cyclin B, CK-II, PKA or PKC at >100 μM.

Tideglusib

HY-14872

Tideglusib(NP-031112) is an irreversible, non ATP-competitive GSK-3β inhibitor with IC50 of 60 nM.

TWS119

HY-10590

TWS119 is an inhibitor of glycogen synthase kinase-3β (IC50 = 30 nM).