glycogen synthase kinase 3 beta | GSK subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

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glycogen synthase kinase 3 beta

target has curated data in GtoImmuPdb

Target id: 2030

Nomenclature: glycogen synthase kinase 3 beta

Abbreviated Name: GSK3B

Family: GSK subfamily

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 420 3q13.3 GSK3B glycogen synthase kinase 3 beta
Mouse - 420 16 B4 Gsk3b glycogen synthase kinase 3 beta
Rat - 420 11 q21 Gsk3b glycogen synthase kinase 3 beta
Previous and Unofficial Names
GSK3 | GSK-3 beta | tau phosphorylating kinase I [21]
Database Links
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
RefSeq Nucleotide
RefSeq Protein
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  GSK-3 Beta complexed with Indirubin-3'-monoxime
PDB Id:  1Q41
Resolution:  2.1Å
Species:  Human
References:  5
Image of receptor 3D structure from RCSB PDB
PDB Id:  1I09
Resolution:  2.7Å
Species:  Human
References:  42
Enzyme Reaction
EC Number:

Download all structure-activity data for this target as a CSV file

Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
AZD2858 Hs Inhibition 8.3 pKi 4
pKi 8.3 (Ki 4.9x10-9 M) [4]
GSK-3 inhibitor XIII Hs Inhibition 7.7 pKi 3
pKi 7.7 (Ki 2.2x10-8 M) [3]
GSK-3beta inhibitor XI Oc Inhibition 7.6 pKi 31
pKi 7.6 (Ki 2.5x10-8 M) [31]
AZD1080 Hs Inhibition 7.5 pKi 20
pKi 7.5 (Ki 3.1x10-8 M) [20]
GSK-3beta inhibitor VIII Hs Inhibition 7.4 pKi 8
pKi 7.4 (Ki 3.8x10-8 M) [8]
tideglusib Hs Irreversible inhibition 7.3 pKi 14
pKi 7.3 (Ki 5x10-8 M) [14]
CHIR-98014 Hs Inhibition 9.2 pIC50 36
pIC50 9.2 (IC50 5.8x10-10 M) [36]
alsterpaullone 2-cyanoethyl Hs Inhibition 9.1 pIC50 17
pIC50 9.1 (IC50 8x10-10 M) [17]
LY2090314 Hs Inhibition 9.0 pIC50 16
pIC50 9.0 (IC50 1.1x10-9 M) [16]
Description: Inhibition of GSK-3β-mediated phosphoryaltion of phosph0-CREB
GSK-3β inhibitor 3 [PMID: 25845281] Hs Inhibition 9.0 pIC50 40
pIC50 9.0 (IC50 1.1x10-9 M) [40]
Description: In vitro GSK-3β inhibitory activity
RGB-286638 Hs Inhibition 8.5 pIC50 9
pIC50 8.5 (IC50 3x10-9 M) [9]
alsterpaullone Hs Inhibition 8.4 pIC50 26
pIC50 8.4 (IC50 4x10-9 M) [26]
GSK-3 inhibitor IX Pig Inhibition 8.3 pIC50 28,35
pIC50 8.3 (IC50 5x10-9 M) [28,35]
Description: GSK3α/β complex from pig brain
CHIR-99021 Hs Inhibition 8.2 pIC50 36
pIC50 8.2 (IC50 6.7x10-9 M) [36]
SB 216763 Hs Inhibition ~8.1 pIC50 11
pIC50 ~8.1 (IC50 ~9x10-9 M) [11]
GSK-3 inhibitor X Pig Inhibition 8.0 pIC50 35
pIC50 8.0 (IC50 1x10-8 M) [35]
Description: Measured using GSK3 as a complex of α and β isozymes, isolated from pig brain
GNF4877 Hs Inhibition 7.8 pIC50 39
pIC50 7.8 (IC50 1.6x10-8 M) [39]
compound 2 [PMID: 22560567] Hs Inhibition 7.8 pIC50 10
pIC50 7.8 (IC50 1.72x10-8 M) [10]
1-azakenpaullone Hs Inhibition 7.7 pIC50 24
pIC50 7.7 (IC50 1.8x10-8 M) [24]
indirubin-3'-monoxime Hs Inhibition 7.7 pIC50 25
pIC50 7.7 (IC50 2.2x10-8 M) [25]
kenpaullone Hs Inhibition 7.6 pIC50 25
pIC50 7.6 (IC50 2.3x10-8 M) [25]
compound 52 [PMID: 9677190] Hs Inhibition 7.5 pIC50 17
pIC50 7.5 (IC50 3x10-8 M) [17]
TWS119 Hs Inhibition 7.5 pIC50 13
pIC50 7.5 (IC50 3x10-8 M) [13]
SB-415286 Hs Inhibition ~7.4 pIC50 11
pIC50 ~7.4 (IC50 ~3.8x10-8 M) [11]
IM-12 Hs Inhibition 7.3 pIC50 38
pIC50 7.3 (IC50 5.3x10-8 M) [38]
compound 2f [Jiang et al., 2018] Hs Inhibition 7.2 pIC50 23
pIC50 7.2 (IC50 6.6x10-8 M) [23]
voruciclib Hs Inhibition 7.2 pIC50 33
pIC50 7.2 (IC50 7.1x10-8 M) [33]
compound 89S [PMID: 19115845] Hs Inhibition 6.8 pIC50 29
pIC50 6.8 (IC50 1.46x10-7 M) [29]
compound 4g [PMID: 2680437] Hs Inhibition 6.7 pIC50 41
pIC50 6.7 (IC50 1.9x10-7 M) [41]
Description: Evaluated in a Kinase-Glo assay.
compound 5b [PMID: 24900464] Hs Inhibition 6.6 pIC50 15
pIC50 6.6 (IC50 2.5x10-7 M) [15]
GSK-3beta inhibitor II Hs Inhibition 6.4 pIC50 30
pIC50 6.4 (IC50 3.9x10-7 M) [30]
isogranulatimide Hs Inhibition 6.3 pIC50 17,22
pIC50 6.3 (IC50 5x10-7 M) [17,22]
7-hydroxystaurosporine Hs Inhibition 6.3 pIC50 22
pIC50 6.3 (IC50 5x10-7 M) [22]
BX-795 Hs Inhibition 6.2 pIC50 18
pIC50 6.2 (IC50 6.2x10-7 M) [18]
Cdk/Crk inhibitor Hs Inhibition 6.1 pIC50 17
pIC50 6.1 (IC50 7.54x10-7 M) [17]
Cdk1/5 inhibitor Hs Inhibition 6.0 pIC50 17
pIC50 6.0 (IC50 1x10-6 M) [17]
GSK-3beta inhibitor I Hs Inhibition 5.8 pIC50 45
pIC50 5.8 (IC50 1.4x10-6 M) [45]
GSK2646264 Hs Inhibition 5.3 pIC50 2
pIC50 5.3 (IC50 5.012x10-6 M) [2]
BX-912 Hs Inhibition 5.1 pIC50 18
pIC50 5.1 (IC50 7.4x10-6 M) [18]
Li+ Hs Inhibition 2.6 pIC50 37
pIC50 2.6 (IC50 2.5x10-3 M) Competive with Mg2+ [37]
View species-specific inhibitor tables
Inhibitor Comments
GSK3β may be the primary target of the approved drug lithium, which inhibits GSK3β activity by approximately 80% [43].
DiscoveRx KINOMEscan® screen
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
Reference: 12,44

Key to terms and symbols Click column headers to sort
Target used in screen: GSK3B
Ligand Sp. Type Action Value Parameter
enzastaurin Hs Inhibitor Inhibition 8.1 pKd
AT-7519 Hs Inhibitor Inhibition 8.0 pKd
BMS-387032 Hs Inhibitor Inhibition 7.4 pKd
staurosporine Hs Inhibitor Inhibition 7.2 pKd
GSK690693 Hs Inhibitor Inhibition 7.0 pKd
tamatinib Hs Inhibitor Inhibition 6.9 pKd
R547 Hs Inhibitor Inhibition 6.6 pKd
A-674563 Hs Inhibitor Inhibition 6.5 pKd
dovitinib Hs Inhibitor Inhibition 6.5 pKd
JNJ-28312141 Hs Inhibitor Inhibition 6.1 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.

A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform.

Reference: 1,19

Key to terms and symbols Click column headers to sort
Target used in screen: GSK3β/GSK3b
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
alsterpaullone Hs Inhibitor Inhibition 2.7 -1.0 3.0
alsterpaullone 2-cyanoethyl Hs Inhibitor Inhibition 2.7 -3.0 0.0
GSK-3 inhibitor IX Hs Inhibitor Inhibition 3.8 -1.0 0.0
staurosporine Hs Inhibitor Inhibition 4.4 7.5 4.5
SB 218078 Hs Inhibitor Inhibition 4.6 40.0 23.0
JNK inhibitor V Hs Inhibitor Inhibition 6.2 8.0 1.0
PKR inhibitor Hs Inhibitor Inhibition 6.3 4.0 0.0
GF109203X Hs Inhibitor Inhibition 7.0 24.0 3.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 9.0 4.0 0.0
Ro-32-0432 Hs Inhibitor Inhibition 11.2
Displaying the top 10 most potent ligands  View all ligands in screen »
Immunopharmacology Comments
GSK3β plays an essential function in T cell differentiation and proliferation, and its activity is inhibited following antigen-driven T cell activation [6-7,27,32]. Recent evidence shows that in CD4+ T cells, inactivation of GSK3β is mediated by the GTPase GIMAP5 (GIMAP5; Q96F15), and that GIMAP5 represents an important checkpoint in T cell proliferation [34]. Ablation of Gimap5 activity leads to constitutive GSK3β activation and substantially reduced CD4+ T cell proliferation in vitro and in in vivo rodent models. A loss-of-function mutation in GIMAP5 has been identified in a patient with lymphopenia (see rs72650695; p.Leu204Pro). Treatment of this patient's T cells, ex vivo, with lithium chloride (a GSK3 inhibitor) rescues their proliferative potential.
Immuno Process Associations
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 2 GO processes
GO:0036016 cellular response to interleukin-3 ISS
GO:0036018 cellular response to erythropoietin IEP
Immuno Process:  Immune regulation
GO Annotations:  Associated to 1 GO processes
GO:0045672 positive regulation of osteoclast differentiation IMP
Immuno Process:  Immune system development
GO Annotations:  Associated to 1 GO processes
GO:0045672 positive regulation of osteoclast differentiation IMP


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17. Fedorov O, Marsden B, Pogacic V, Rellos P, Müller S, Bullock AN, Schwaller J, Sundström M, Knapp S. (2007) A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. Proc. Natl. Acad. Sci. U.S.A., 104 (51): 20523-8. [PMID:18077363]

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22. Jiang X, Zhao B, Britton R, Lim LY, Leong D, Sanghera JS, Zhou BB, Piers E, Andersen RJ, Roberge M. (2004) Inhibition of Chk1 by the G2 DNA damage checkpoint inhibitor isogranulatimide. Mol. Cancer Ther., 3 (10): 1221-7. [PMID:15486189]

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How to cite this page

GSK subfamily: glycogen synthase kinase 3 beta. Last modified on 21/02/2020. Accessed on 20/09/2020. IUPHAR/BPS Guide to PHARMACOLOGY,