Information on EC 2.7.11.26 - tau-protein kinase

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The expected taxonomic range for this enzyme is: Eukaryota

EC NUMBER
COMMENTARY
2.7.11.26
-
RECOMMENDED NAME
GeneOntology No.
tau-protein kinase
REACTION
REACTION DIAGRAM
COMMENTARY
ORGANISM
UNIPROT ACCESSION NO.
LITERATURE
ATP + tau-protein = ADP + O-phospho-tau-protein
show the reaction diagram
-
-
-
-
ATP + [tau-protein] = ADP + O-phospho-[tau-protein]
show the reaction diagram
-
-
-
-
ATP + [tau-protein] = ADP + O-phospho-[tau-protein]
show the reaction diagram
activation loop structure, substrate binding structure, and catalytic site structure and mechanism
-
ATP + [tau-protein] = ADP + O-phospho-[tau-protein]
show the reaction diagram
glycogen synthase kinase-3beta also performs serine/threonine protein kinase reaction, EC 2.7.11.1, with other substrates than tau, e.g. it phosphorylates the glycogen synthase
-
ATP + [tau-protein] = ADP + O-phospho-[tau-protein]
show the reaction diagram
GSK-3 and PKA catalyze tau phosphorylation in the brain, while GSK-3 performs phosphorylation of glycogen synthase, EC 2.7.11.1, and other proteins in different tissues, and PKA performs phosphorylation of other proteins in different tissues
-
REACTION TYPE
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
phospho group transfer
-
-
-
-
SYSTEMATIC NAME
IUBMB Comments
ATP:[tau-protein] O-phosphotransferase
Activated by tubulin. Involved in the formation of paired helical filaments, which are the main fibrous component of all fibrillary lesions in brain and are associated with Alzheimer's disease.
SYNONYMS
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
AtK-1
Q39019
-
brain proteinkinase PK40erk
-
-
cAMP-dependent protein kinase A
-
-
cAMP-dependent protein kinase A
-
-
Cdk5-p25
-
-
Cdk5-p35
-
-
CDK5/p25
-
-
cyclin-dependent kinase 5
-
-
cyclin-dependent kinase 5
-
-
cyclin-dependent kinase 5
-
-
cyclin-dependent kinase 5/p39
-
-
cyclin-dependent kinase-5
-
-
Gasket protein
-
-
-
-
glycogen synthase kinase
-
-
-
-
glycogen synthase kinase 3
-
-
glycogen synthase kinase 3
-
-
glycogen synthase kinase 3 beta
-
-
glycogen synthase kinase 3beta
-
-
glycogen synthase kinase 3beta
P49841
-
glycogen synthase kinase 3beta
-
-
glycogen synthase kinase 3beta
-
-
glycogen synthase kinase-3
P49841
-
glycogen synthase kinase-3
-
-
glycogen synthase kinase-3
Leishmania donovani LG13
-
-
-
glycogen synthase kinase-3
-
-
glycogen synthase kinase-3
-
-
glycogen synthase kinase-3
P18266
-
glycogen synthase kinase-3 alpha
P49841
-
glycogen synthase kinase-3 alpha
P18265
-
glycogen synthase kinase-3 alpha
P18266
-
glycogen synthase kinase-3 homolog
P51136
-
glycogen synthase kinase-3 homolog MsK-1
P51137
-
glycogen synthase kinase-3 homolog MsK-2
P51138
-
glycogen synthase kinase-3 homolog MsK-3
P51139
-
glycogen synthase kinase-3alphabeta
-
-
glycogen synthase kinase-3beta
-
-
glycogen synthase kinase-3beta
-
-
glycogen synthase kinase-3beta
-
-
glycogen synthase kinase-3beta
-
-
glycogen synthase kinase-3beta
-
isoform
glycogen synthase kinase-3beta
-
-
glycogen synthase kinase-3beta
Q9WV60
-
glycogen synthase kinase-3beta
-
-
glycogen synthase kinase-3beta
P18266
-
glycogen synthase kinase-3beta
-
-
GSK 3-beta
-
-
GSK-3
P49841
-
GSK-3
Leishmania donovani LG13
-
-
-
GSK-3
-
-
GSK-3
P18265
-
GSK-3 alpha
-
-
-
-
GSK-3 beta
-
-
-
-
GSK-3 beta
-
-
GSK-3/shaggy-like protein kinase
O04160
-
GSK-3alpha
-
isoform
GSK-3alpha
-
isoform
GSK-3beta
-
-
GSK-3beta
-
-
GSK-3beta
-
-
GSK-3beta
P49841
-
GSK-3beta
-
isoform
GSK-3beta
Leishmania donovani LG13
-
isoform
-
GSK-3beta
-
isoform
GSK-3beta
Q9WV60
-
GSK-3beta
P18266
-
GSK-3beta
-
-
GSK-3beta1
-
isoform
GSK-3beta2
-
neuron-specific isoform
GSK3alpha
-
isoform
GSK3beta
-
isoform
NtK-4
Q40518
-
p-SAPK/JNK
-
-
p25-Cdk5 kinase complex
-
-
protein kinase 1
-
-
protein kinase A
-
-
protein kinase shaggy
P18431
-
protein kinase skp1
Q10452
-
protein kinase-A
-
-
protein tau kinase
-
-
-
-
serine-threonine kinase
-
-
serine/threonine-protein kinase MDS1/RIM11
P38615
-
serine/threonine-protein kinase MRK1
P50873
-
serum- and glucocorticoid-induced protein kinase 1
-
-
SGK1
-
-
SHAGGY-related protein kinase
P43289
-
shaggy-related protein kinase alpha
P43288
-
shaggy-related protein kinase beta
O23145
-
shaggy-related protein kinase delta
Q39010
-
shaggy-related protein kinase eta
Q39011
-
shaggy-related protein kinase gamma
P43289
-
shaggy-related protein kinase iota
Q39012
-
shaggy-related protein kinase kappa
Q39019
-
shaggy-related protein kinase NtK-1
Q40518
-
shaggy-related protein kinase theta
Q96287
-
shaggy-related protein kinase theta
O04160
-
shaggy/zeste white-3
-
-
stress activated kinase/c-jun N-terminal kinase
-
-
Syk
-
common tyrosine kinase of tau and alpha-synuclein
tau factor protein kinase (phosphorylating)
-
-
-
-
tau kinase
-
-
-
-
tau kinase
-
-
tau protein kinase
-
-
-
-
tau protein kinase I
-
-
-
-
tau protein kinase I
-
-
tau protein kinase I/glycogen synthase kinase 3beta
-
-
tau protein kinase I/GSK-3beta/kinaseFA
-
-
tau protein kinase II (cdk5/p20)
-
-
tau protein kinase II system
-
-
tau protein kinase II system
Rattus norvegicus Sprague-Dawley
-
-
-
tau-protein kinase I
-
-
tau-protein kinase I
-
-
tau-protein kinase II
-
-
tau-tubulin kinase
-
-
tau-tubulin kinase
-
-
tau-tubulin kinase
Rattus norvegicus Wistar
-
-
-
Tau-tubulin kinase 1
-
-
Tau-tubulin kinase 1
-
-
tau-tubulin kinase 2
-
-
TPK
-
-
TPK I
-
-
TPKI
-
-
TPKI
Rattus norvegicus Wistar
-
-
-
TPKI/GSK-3beta
-
-
TPKI/GSK-3beta
-
-
TPKI/GSK-3beta/FA
-
-
TPKI/GSK3beta
-
-
TPKI/GSK3beta
Mus musculus C57BL/6Njcl
-
-
-
TPKII
-
-
TTBK2
-
-
TTK
Rattus norvegicus Wistar
-
-
-
zeste-white3
P18431
-
additional information
-
see also EC 2.7.11.1
additional information
-
cf. EC 2.7.11.1
additional information
-
see also EC 2.7.11.1
additional information
-
see also EC 2.7.11.1 and EC 2.7.11.11
additional information
-
see also EC 2.7.11.1 and EC 2.7.11.22
additional information
-
see also EC 2.7.11.22
additional information
-
CDK5 is a unique member of the CDK family, see also EC 2.7.11.22
additional information
-
see also EC 2.7.11.1 and EC 2.7.11.22
additional information
-
see also EC 2.7.11.22
additional information
-
see also EC 2.7.11.1 and EC 2.7.11.11
additional information
-
see also EC 2.7.11.22
CAS REGISTRY NUMBER
COMMENTARY
111694-09-8
-
ORGANISM
COMMENTARY
LITERATURE
SEQUENCE CODE
SEQUENCE DB
SOURCE
strains Guofu x Nongfong and P1
-
-
Manually annotated by BRENDA team
HEK 293 cells; human
-
-
Manually annotated by BRENDA team
isozyme CKIdelta
-
-
Manually annotated by BRENDA team
strain LG13
-
-
Manually annotated by BRENDA team
Leishmania donovani LG13
strain LG13
-
-
Manually annotated by BRENDA team
adult C57/BL6 mice
-
-
Manually annotated by BRENDA team
apolipoprotein E4 transgenic mice
-
-
Manually annotated by BRENDA team
C57BL/6 genetic background
-
-
Manually annotated by BRENDA team
C57BL/6Njcl mice
-
-
Manually annotated by BRENDA team
male C57BL/6Njcl mice
-
-
Manually annotated by BRENDA team
mouse, brain TTK cDNA nucleotide sequence, same accession number in EMBL/DDBJ
SwissProt
Manually annotated by BRENDA team
transgenic APP TG2576 mice
-
-
Manually annotated by BRENDA team
Mus musculus C57BL/6Njcl
C57BL/6Njcl mice
-
-
Manually annotated by BRENDA team
male Wistar rats
-
-
Manually annotated by BRENDA team
pheochromacytoma PC-12 cells
-
-
Manually annotated by BRENDA team
pregnant Wistar rats
-
-
Manually annotated by BRENDA team
Sprague-Dawley
-
-
Manually annotated by BRENDA team
Wistar albino female rats
-
-
Manually annotated by BRENDA team
Rattus norvegicus Sprague-Dawley
Sprague-Dawley
-
-
Manually annotated by BRENDA team
Rattus norvegicus Wistar
Wistar
-
-
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
malfunction
-
inhibition of glycogen synthase kinase-3 increases beta-catenin concentration in the cytoplasm
malfunction
-
chronic inhibition of GSK-3 enhances glycolysis
malfunction
-
inhibition of GSK-3beta mediates Nrf2 activation by the M1 receptor
malfunction
-
inhibition of GSK-3beta abolishes Abeta-induced spine alterations
malfunction
-
inactivation of glycogen synthase kinase-3beta suppresses mitochondrial permeability transition pore opening and protects cardiomyocytes
malfunction
-
GSK-3beta heterozygote mice, which express GSK-3beta at 50% wild type levels, have impaired memory reconsolidation but normal memory consolidation
malfunction
-
inhibition of GSK-3beta abrogates glucocorticoid-induced bone loss by increasing beta-catenin- and Runx2-mediated osteoblast differentiation
physiological function
-
the GSK-3beta-mediated high phosphorylation of protein tau induces synapse loss and neuronal death
physiological function
-
GSK3beta regulates both tau phosphorylation and total tau levels through protein phosphatase-2A
physiological function
-
GSK-3beta is a multifunctional Ser/Thr kinase that plays important roles in necrosis and apoptosis of cardiomyocytes
physiological function
-
increased GSK-3 correlates with increased cell death, GSK-3 plays a very important role in L-DOPA neurotoxicity, as well as in neurodegeneration
physiological function
-
cisplatin-induced cytotoxicity may be associated with modulation of GSK-3 activation
physiological function
-
protein tau phosphorylation plays an essential role in adult hippocampal neurogenesis and GSK-3 facilitates neurogenesis only in the presence of tau proteins, tau hyperphosphorylation induced by activating GSK-3 promotes neurogenesis
physiological function
-
mitochondrial hexokinase II is a promoter of neuronal survival under the regulation of GSK-3
physiological function
-
GSK-3 is necessary and sufficient for cardiomyocyte differentiation in mesenchymal stem cells, GSK-3beta in the cytosol induces cardiomyocyte differentiation of mesenchymal stem cells through down-regulation of beta-catenin. In contrast, GSK-3alpha in the nucleus inhibits cardiomyocyte differentiation through down-regulation of c-Jun
physiological function
-
glycogen synthase kinase-3 regulates the phosphorylation of severe acute respiratory syndrome coronavirus nucleocapsid protein and viral replication
physiological function
-
GSK-3-regulated signal transduction pathways are important for stem cell maintenance and may be involved in events controlling cell differentiation
physiological function
-
GSK3 negatively regulates mycobacteria-induced interleukin-10 production in human monocytes
physiological function
-
the neuron-specific isoform GSK-3beta2 is required for axon growth by phosphorylating microtubule-associated proteins including protein tau
physiological function
-
GSK-3 activity is required for tau filaments to inhibit kinesin-dependent FAT
physiological function
-
GSK-3beta activation is required for memory reconsolidation in the adult brain
physiological function
-
activation of GSK-3beta results in the inhibition of the Wnt signaling pathway
physiological function
-
GSK-3beta is a critical mediator of N-methyl-4-phenyl-1,2,3,6-tetrahydropyridine/1-methyl-4-phenylpyridinium iodide-induced neurotoxicity through its ability to regulate mitochondrial functions
SUBSTRATE
PRODUCT                      
REACTION DIAGRAM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
(Substrate)
LITERATURE
(Substrate)
COMMENTARY
(Product)
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
ATP + alpha-casein
ADP + alpha-casein phosphate
show the reaction diagram
-
-
-
-
?
ATP + alpha-casein
ADP + alpha-casein phosphate
show the reaction diagram
-
isoenzyme TPKI
-
-
?
ATP + alpha-synuclein
ADP + phosphorylated alpha-synuclein
show the reaction diagram
-
-
-
-
?
ATP + amyloid precursor protein
ADP + phosphorylated amyloid precursor protein
show the reaction diagram
-
-
-
-
?
ATP + axin
ADP + phosphorylated axin
show the reaction diagram
Leishmania donovani, Leishmania donovani LG13
-
-
-
-
?
ATP + beta-casein
ADP + beta-casein phosphate
show the reaction diagram
-
isoenzyme TPKII
-
-
?
ATP + beta-catenin
ADP + phosphorylated beta-catenin
show the reaction diagram
-
-
-
-
?
ATP + beta-catenin
ADP + phosphorylated beta-catenin
show the reaction diagram
-
-
-
-
?
ATP + beta-catenin
ADP + phosphorylated beta-catenin
show the reaction diagram
-
-
-
-
?
ATP + beta-catenin
ADP + phosphorylated beta-catenin
show the reaction diagram
-
substrate of isoform GSK-3beta
-
-
?
ATP + beta-catenin
ADP + beta-catenin phosphate
show the reaction diagram
-
-
-
-
?
ATP + beta-catenin
ADP + beta-catenin phosphate
show the reaction diagram
-
-
-
-
?
ATP + beta-tubulin
ADP + beta-tubulin phosphate
show the reaction diagram
-
isoenzyme tau-tubulin kinase
-
-
?
ATP + c-Jun
ADP + phosphorylated c-Jun
show the reaction diagram
-
substrate of isoform GSK-3alpha
-
-
?
ATP + c-Myc
ADP + phosphorylated c-Myc
show the reaction diagram
-
-
-
-
?
ATP + cAMP response element-binding protein
ADP + phosphorylated cAMP response element-binding protein
show the reaction diagram
-
-
-
-
?
ATP + casein
ADP + phosphorylated casein
show the reaction diagram
Leishmania donovani, Leishmania donovani LG13
-
-
-
-
?
ATP + coronavirus nucleocapsid protein
ADP + phosphorylated coronavirus nucleocapsid protein
show the reaction diagram
-
phosphorylation sites are at Ser177, Ser181, Ser184, Ser185, Ser187, Ser189, Ser191, Ser203, and Ser207
-
-
?
ATP + cyclin D
ADP + phosphorylated cyclin D
show the reaction diagram
-
-
-
-
?
ATP + cyclin D1
ADP + phosphorylated cyclin D1
show the reaction diagram
-
-
-
-
?
ATP + cyclin E
ADP + phosphorylated cyclin E
show the reaction diagram
-
-
-
-
?
ATP + DIWKKFELLPTPPLSPSRRSG
ADP + DIWKKFELLP(P)TPPL(P)SPSRRSG
show the reaction diagram
-
c-Myc
-
?
ATP + DIWKKFELVPSPPTSPPWGL
ADP + DIWKKFELVP(P)SPPT(P)SPPWGL
show the reaction diagram
-
L-myc
-
?
ATP + EEPQTVPEMPGETPPLSPIDMESQER
ADP + EEPQTVPEMPGE(P)TPPL(P)SPIDMESQER
show the reaction diagram
-
c-Jun
-
?
ATP + eIF2B peptide
ADP + phosphorylated eIF2B peptide
show the reaction diagram
-
-
-
-
?
ATP + FITC-GSRSRTPSLP
ADP + FITC-GSRSRTP-phosphoserine-LP
show the reaction diagram
-
synthetic fluorescence-labeled peptide substrate derived from residues 207-216 of tau protein, phosphorylation of S214 by SGK1
-
-
?
ATP + FXVEXTPXCFSRXSSLSSLS
ADP + ?
show the reaction diagram
-
-
-
-
?
ATP + glycogen synthase
ADP + phosphorylated glycogen synthase
show the reaction diagram
P51136
-
-
-
-
ATP + glycogen synthase
ADP + glycogen synthase phosphate
show the reaction diagram
-
-
-
-
?
ATP + H-Arg-Arg-Arg-Ala-Ala-Glu-Glu-Leu-Asp-Ser-Arg-Ala-Gly-pSer-Pro-Gln-Leu-OH
ADP + ?
show the reaction diagram
-
-
-
-
?
ATP + heat shock factor-1
ADP + phosphorylated heat shock factor-1
show the reaction diagram
-
-
-
-
?
ATP + histone H1
ADP + histone H1 phosphate
show the reaction diagram
-
isoenzyme TPKII
-
-
?
ATP + histone H1
ADP + histone H1 phosphate
show the reaction diagram
-
isoenzyme TPKII
-
-
?
ATP + histone H1
ADP + histone H1 phosphate
show the reaction diagram
-
Cdk5 substrate
-
-
-
ATP + histone H2a
ADP + histone H2a phosphate
show the reaction diagram
-
isoenzyme TPKII
-
-
?
ATP + histone H2b
ADP + histone H2b phosphate
show the reaction diagram
-
isoenzyme TPKII
-
-
?
ATP + histone H3
ADP + histone H3 phosphate
show the reaction diagram
-
isoenzyme TPKII
-
-
?
ATP + JHMV-N protein
ADP + phosphorylated JHMV-N protein
show the reaction diagram
-
phosphorylation sites are at Ser197, Ser201, Ser-205, and Ser-209
-
-
?
ATP + Jun
ADP + phosphorylated Jun
show the reaction diagram
-
-
-
-
?
ATP + KAUSSPTVSRKTD
ADP + KAUSSPTVSRKTD phosphate
show the reaction diagram
-
synthetic peptide p25/F3
-
-
?
ATP + KRREILSRRPpSYR
ADP + ?
show the reaction diagram
-
KRREILSRRPpSYR is selectively phosphorylated by GSK-3 and therefore acts as a competitive inhibitor of other GSK-3 substrates
-
-
?
ATP + LLNASGSTSTPAPSRTASFSESR
ADP + LLNASGSTS(P)TPAP(P)SRTASFSESR
show the reaction diagram
-
ATP-citrate lyase
-
?
ATP + MADSRPKPANKTPPK
ADP + MADSRPKPANKTPPK phosphate
show the reaction diagram
-
synthetic peptide F5f
-
-
?
ATP + mammalian histone H1
ADP + phosphorylated mammalian histone H1
show the reaction diagram
Leishmania donovani, Leishmania donovani LG13
-
-
-
-
?
ATP + MAP2
ADP + MAP2 phosphate
show the reaction diagram
-
-
-
-
?
ATP + MAP2
ADP + MAP2 phosphate
show the reaction diagram
-
isoenzyme TPKII
-
-
?
ATP + MAP2
ADP + MAP2 phosphate
show the reaction diagram
-
isoenzyme TPKI and TPKII
-
-
?
ATP + MARSRPK
ADP + MARSRPK phosphate
show the reaction diagram
-
synthetic peptide F5h
-
-
?
ATP + Myc
ADP + phosphorylated Myc
show the reaction diagram
-
-
-
-
?
ATP + myelin basic protein
ADP + phosphorylated myelin basic protein
show the reaction diagram
Leishmania donovani, Leishmania donovani LG13
-
-
-
-
?
ATP + nuclear factor-kappaB
ADP + phosphorylated nuclear factor-kappaB
show the reaction diagram
-
-
-
-
?
ATP + p53
ADP + phosphorylated p53
show the reaction diagram
-
-
-
-
?
ATP + p53
ADP + phosphorylated p53
show the reaction diagram
-
-
-
-
?
ATP + p53
ADP + p53 phosphate
show the reaction diagram
-
-
-
-
?
ATP + PANKTPPKSPGEPAKDPAAK
ADP + PANKTPPKSPGEPAKDPAAK phosphate
show the reaction diagram
-
synthetic peptide p25/F5a
-
-
?
ATP + phospho-glycogen synthase peptide-2
ADP + phosphorylated phospho-glycogen synthase peptide-2
show the reaction diagram
-
GSK3 substrate
-
-
-
ATP + protein
ADP + phosphoprotein
show the reaction diagram
-
autophosphorylation at Tyr and Ser
-
-
-
ATP + protein PHF-1
ADP + protein PHF-1 phosphate
show the reaction diagram
-
-
-
-
?
ATP + protein PHF-1 (Ser396/404)
ADP + protein PHF-1 (Ser396/404) phosphate
show the reaction diagram
-
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-, Q3UVR3
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
microtubule-associated protein, enzyme can also phosphorylate human tau
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
enzyme can also phosphorylate bovine tau
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
phosphorylates tau and forms paired helical filament epitopes, tau/K1, K2, K3 and tau/4 repeat
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
phosphorylates tau protein into Alzheimer disease-like forms, resulting in neuronal death
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
when a beta-mediated aggregated tau is used as a substrate for TPKII, an 8fold increase in the rate of TPKII-mediated tau phosphorylation is observed
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
6 isoforms of human tau expressed in adult human brain
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
prior phosphorylation of tau by isoenzyme TPKII strongly enhances the action of TPKI
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
regulates PDH and participates in energy metabolism and acetylcholine synthesis
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
microtubule-associated protein
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
phosphorylates tau on S202, T231, S396, and S400 but not on S262, S235, and S404. Phosphorylates tau directly at S202 but requires the previous phosphorylation on S235 to phosphorylate T231, once a priming kinase phosphorylates S404, GSK3beta sequentially phosphorylates S400 and then S396
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
direct tau phosphorylation by TTBK1 at Ser198, Ser199, Ser202 and Ser422
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
GSK-3beta-mediated hyperphosphorylated forms of tau are degradable by the proteasomal machinery
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
phosphorylation at Ser9
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
role of GSK3 as a key mediator of tau hyperphosphorylation, whereas Cdk5 acts as a modulator of tau hyperphosphorylation via the inhibitory regulation of GSK3
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
T231 is the primary phosphorylation site for GSK3beta, the tau227-237 (AVVRTPPKSPS) derived from tau containing T231P232 motif is the GSK3beta binding site with high affinity (Kd = 0.00082 mmol/L), tau mutant T231A completely abolishes tau phosphorylation by GSK3beta
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
TTBK2 (1-331) phosphorylates residues Ser208 and Ser210
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
Q9WV60
the antagonist of GSK-3beta in protein tau phosphorylation is the phosphatase PP2A
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
in vitro, GSK-3beta phosphorylates protein tau at 14 sites, all tau protein isoforms are phosphorylated by GSK-3beta which changes filament polymerization levels and filament morphology
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
phosphorylation occurs at Ser-396/Ser-404
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
PKA transfers about 2 mol of phosphate per mole of the shortest protein tau isoform and phosphorylates Ser156, 235, 267, 320 and 327 (corresponding to Ser214, 324, 356, 409 and 416 of the longest protein tau isoform)
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
protein tau primed by CK1 functions as an effective phosphate acceptor for GSK-3beta
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
Rattus norvegicus Sprague-Dawley
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
Mus musculus C57BL/6Njcl
-
phosphorylation at Ser9
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
Rattus norvegicus Wistar
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
Rattus norvegicus Wistar
-
-
-
?
ATP + protein tau-1
ADP + protein tau-1 phosphate
show the reaction diagram
-
-
-
-
?
ATP + pyruvate dehydrogenase
ADP + pyruvate dehydrogenase phosphate
show the reaction diagram
-
PDH is phosphorylated and inactivated in vitro and also in betaA-treated hippocampal cultures, resulting in mitochondrial dysfunction which will contribute to neuronal death
-
-
?
ATP + RADSRPK
ADP + RADSRPK phosphate
show the reaction diagram
-
synthetic peptide F5g
-
-
?
ATP + RKRSRAE
ADP + RKRSRAE phosphate
show the reaction diagram
-
synthetic peptide 8659
-
-
?
ATP + RKRSRKE
ADP + RKRSRKE phosphate
show the reaction diagram
-
synthetic peptide 8655
-
-
?
ATP + RRREEETEEE
ADP + RRREEETEEE phosphate
show the reaction diagram
-
synthetic peptide CKII substrate
-
-
?
ATP + RRRPASVPPSPSLSRHSpSHQRR
ADP + ?
show the reaction diagram
-
-
-
-
?
ATP + RSRSRSRSRSRSPPPVSK
ADP + phosphorylated RSRSRSRSRSRSPPPVSK
show the reaction diagram
-
SC35-derived peptide 180-197, recombinant GSK-3beta
-
-
?
ATP + SC35
ADP + phosphorylated SC35
show the reaction diagram
-
substrate prephosphorylated SC35, SC35 is a member of the SR family of serine/arginine-rich splicing factors, substrate prephosphorylated SC35, SC35 is a member of the SR family of serine/arginine-rich splicing factors, recombinant GSK-3beta
-
-
?
ATP + SPPLSPIDMETQER
ADP + (P)SPPLSPIDME(P)TQER
show the reaction diagram
-
JunD
-
?
ATP + SPVVSGDT(P)SPR
ADP + ?
show the reaction diagram
-
-
-
-
-
ATP + tau protein
ADP + phosphorylated tau protein
show the reaction diagram
-
tau in Alzheimer disease brain is highly phosphorylated and aggregates into paired helical filaments comprising characteristic neurofibrillary tangles, overview, determination of several phosphorylation sites, e.g. Ser258, Ser289, Ser262, and Ser356 within the microtubule-binding repeats or at Ser184 and Ser185 of the central region, for casein kinase I, casein kinase 2, and glycogen synthase kinase-3beta in insoluble tau, PHF-tau, extracted from Alzheimer brain and of tau from control healthy brain by mass spectrometry, overview
-
-
?
ATP + TPPKSPSAAK
ADP + TPPK(P)SPSAAK
show the reaction diagram
-
protein tau
-
?
ATP + YRRAAVPPSPSLSRHSSPHQSpEDEEE
ADP + ?
show the reaction diagram
Leishmania donovani, Leishmania donovani LG13
-
-
-
-
?
ATP + [FRAT-2 protein]
ADP + phosphorylated [FRAT-2 protein]
show the reaction diagram
-
i.e. frequently rearranged in advanced T-cell lymphoma protein 2, phosphorylation by GSK3beta
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
-
-
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
-
-
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
-
-
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
-
-, 14-3-3 connects glycogen synthase kinase-3 beta to tau within a brain microtubule-associated tau phosphorylation complex
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
-
abnormal hyperphosphorylation of tau by PKA and GSK-3 is associated with Alzheimer's disease and other tauopaties leading to neuronal degeneration
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
-
activity in organisms with mutated APP and tau, not in wild-type, overview
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
-
cdk5 associated with p25
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
-
cdk5 substrate in brain, cdk5 associated with p39, tau is a microtubule-associated and developmentally regulated protein involved in axonal development in neurons, tau phosphorylation by cyclin-dependent kinase 5/p39 during brain development reduces its affinity for microtubules
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
-
hyperphosphorylation of tau by CDK5 is involved in apoptosis and neurodegeneration in Alzheimer's disease, overview
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
-
phosphorylation of tau, especially at the primed epitope T231 negatively regulates tau-microtubule interactions, different effects of phosphorylation on primed T231 and unprimed S396/S404 epitopes of tau, overview
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
-
protein 14-3-3 mediates phosphorylation of microtubule-associated protein tau by serum- and glucocorticoid-induced protein kinase 1 SGK1, which forms an activated ternary complex with protein 14-3-3theta
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
-
regulation, overview
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
-
tau is microtubule-associated, phopshorylation at T231 by CDK5 causes its release into the cytoplasm
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
-
tau is primarily found in neurons, regulation of tau phosphorylation by GSK3beta via interaction with FRAT-1 and FRAT-2, i.e. frequently rearranged in advanced T-cell lymphoma proteins
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
-
tau phosphorylation by GSK-3beta is involved in development of neurodegenerative Alzheimer's disease, the tau phosphorylation activity by GSK-3beta is further increased by soluble toxic beta-amyloid oligomers, overview
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
-
tau phosphorylation in vivo is stimulated by extracellular signal-regulated kinase Erk phosphorylation and apolipoprotein isozyme E4, to a lesser extent by isozyme apoE3, overview
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
-
cdk5 associated with p25, recombinant bacterially expressed human tau protein as substrate, phosphorylation of the AT8 and AT180 epitopes, and at T231 of the Alzheimer's mitotic epitope TG-3
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
-
phosphorylation at T231, no activity with tau mutant T231A
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
-
phosphorylation at the C-terminus, lower activity with C-terminally truncated tau D421 compared to the wild-type tau, the truncated tau protein forms sarcosyl-insoluble aggregates
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
-
phosphorylation by PKA at Ser214, and by GSK-3 at Ser404, Ser396, Ser198, Ser199, and Ser202
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
-
phosphorylation of primed and unprimed sites by GSK3beta, wild-type and recombinant tau, recombinant GSK3beta S9A
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
-
phosphorylation of S214 by SGK1, recombinant tau S214A is no substrate
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
-
phosphorylation of the PHF-1 epitope at Ser396 and Ser404 by CDK5
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
-
preferred substrate of cdk5 associated with p39, recombinant bacterially expressed human tau protein as substrate, phosphorylation at Ser202 and Thr205
-
-
?
glycogen synthase + ATP
phosphorylated glycogen synthase + ADP
show the reaction diagram
P49841
-
-
-
?
glycogen synthase + ATP
phosphorylated glycogen synthase + ADP
show the reaction diagram
P18266
-
-
-
?
glycogen synthase + ATP
phosphorylated glycogen synthase + ADP
show the reaction diagram
-
-
-
-
?
protein tau + ATP
phosphorylated protein tau + ADP
show the reaction diagram
-
the microtubule-associated protein tau is the principal component of the paired helical filaments - PHFs - found in the brains of patients with Alzheimer disease, and PHF-tau is hyperphosphorylated
-
-
?
glycogen synthase + ATP
phosphorylated glycogen synthase + ADP
show the reaction diagram
-
proline-directed kinase
-
-
?
additional information
?
-
-
-
-
-
-
additional information
?
-
-
TPKI cannot phosphorylate K1, K2 and K3 peptides, histones H1, H2A, H2B and H3 and beta casein
-
-
-
additional information
?
-
-
novel isoenzyme, distinct from TPKI, TPKII CKI and CKII, no activity toward beta-casein and neurofilament, no reaction with synthetic peptides F5a PANKTPPKSPGEPAKDPAAK, F5n MADSRPK, F5d MADSRKPAN, F5e MADSRPAE and 8656 RKRARKE, only weak activity with histones H1, H2a and H2b as substrates
-
-
-
additional information
?
-
P18266
enzyme is involved in the cellular response to insulin, the enzyme is highly phosphorylated on tyrosine and thus active in resting cells
-
-
-
additional information
?
-
-
possible role of the sgg protein in a signal transduction pathway necessary for intercellular communication at different stages of development
-
-
-
additional information
?
-
-
implicated in cell-fate determination and differentiation, phosphorylates several regulatory proteins that are activated by dephosphorylation in response to hormones or growth factors
-
-
-
additional information
?
-
-
enzyme of the lithium-sensitive wnt signaling pathway
-
-
-
additional information
?
-
-
enzyme acts as a repressor of engrailed autoregulation
-
-
-
additional information
?
-
-
enzyme forms part of the wingless signalling pathway. GSK-3beta activity is negatively regulated by phosphorylation on serine 9 and positively regulated by phosphorylation on tyrosine 216. Enzyme may also be regulated at the transcriptional level
-
-
-
additional information
?
-
-
implicated in the hormonal control of several regulatory proteins including glycogen synthase and the transcription factor c-jun
-
-
-
additional information
?
-
-
MDS1 is not essential during normal vegetative growth but appears to be required for meiosis
-
-
-
additional information
?
-
P51136
enzyme regulates cell fate in Dictyostelium
-
-
-
additional information
?
-
P21965
enzyme is involved in the induction of meiosis
-
-
-
additional information
?
-
-
MCK1 encodes a positive regulator of meiosis and spore formation. MCK1 is required in vegetative cells for basal IME1 expression, it is also required for efficient ascus maturation. MCK1 plays a role in governing centromere function during vegetative growth as well as sporulation
-
-
-
additional information
?
-
Q39010, Q39012, Q39019
AtK-1 kinase is involved in reproduction-specific processes
-
-
-
additional information
?
-
-
abnormal phosphorylation of tau in dividing cells leads to its accumulation in the cytosol as microtubule-free form, Cdk5 is involved in neurodegenerative mechanisms
-
-
-
additional information
?
-
-
activation and deregulation of GSK-3, e.g. by wortmannin or GF-109203X, induces Alzheimer-like tau hyperphosphorylation in hippocampus, the hyperphosphorylated tau forms neurofibrillary tangle
-
-
-
additional information
?
-
-
CDK5-dependent clustering of endoplasmic reticulum ER and mitochondria during ceramide-mediated neuronal death: neurotoxic calcium transfer from ER to mitochondria is regulated by cyclin-dependent kinase 5-dependent phosphorylation of tau, inhibition of the process leads to cell death
-
-
-
additional information
?
-
-
glycogen synthase kinase-3beta also performs serine/threonine protein kinase reaction, EC 2.7.11.1, with other substrates than tau, e.g. it phosphorylates the glycogen synthase
-
-
-
additional information
?
-
-
GSK-3 affects the tau-mRNA splicing of exon 10 via phosphorylation of the splicing factors of the serine/arginine-rich splicing factor SR family, e.g. SC35, leading to priming and dislocation of the splicing factor, aberrant tau splicing contributes to tauopathies including Alzheimer's disease, overview
-
-
-
additional information
?
-
-
GSK3beta and PKA work coordinatedly on tau phosphorylation
-
-
-
additional information
?
-
-
naturally occurring V717I mutation of the amyloid precursor protein APP in a CT100 fragment of mutants leads to augmented age-dependent tau phosphorylation, followed by increased activation status of mitogen-activated protein kinase family members, e.g. ERK1/2, p38, and c-Jun NH2-terminal kinase, compared to the wild-type organism, naturally occurring V337M mutation of tau protein of mutants leads to age-dependent memory deficits
-
-
-
additional information
?
-
-
naturally occurring V717I mutation of the amyloid precursor protein APP in a CT100 fragment of organisms with Alzheimer's disease leads to augmented age-dependent tau phosphorylation, followed by increased activation status of mitogen-activated protein kinase family members, e.g. ERK1/2, p38, and c-Jun NH2-terminal kinase, compared to the wild-type organism, naturally occurring V337M mutation of tau protein of patients suffering from Alzheimer's disease leads to age-dependent memory deficits
-
-
-
additional information
?
-
-
phosphorylated tau is important in cytoskeleton assembly
-
-
-
additional information
?
-
-
protein 14-3-3 facilitates tau phosphorylation by SGK1 and regulates its subcellular localization in the nucleus or cytoplasm, overview
-
-
-
additional information
?
-
-
rapid, reversible cold-water stress-induced hyperphosphorylation of tau S199, S202, T205, T231, and S235 in hippocampal and cerebral region of the brain, hyperphosphorylation of tau is associated to the Alzheimer's disease
-
-
-
additional information
?
-
-
tau becomes a more favorable substrate for GSK-3 when it is prephosphorylated by PKA in rat brain, inhibition of tau hyperphosphorylation inhibits an associated loss in spatial memory
-
-
-
additional information
?
-
-
the enzyme participates in Alzheimer's disease
-
-
-
additional information
?
-
-
cdk5 also performs the kinase reaction of EC 2.7.11.22
-
-
-
additional information
?
-
-
GSK3beta catalyzes tau phosphorylation in brain, but phosphorylation of glycogen synthase and other proteins, EC 2.7.11.1, in different tissues
-
-
-
additional information
?
-
-
GSK3beta, EC 2.7.11.1, and PKA, EC 2.7.11.11, catalyze tau phosphorylation in brain, but phosphorylation of glycogen synthase and other proteins in different tissues
-
-
-
additional information
?
-
-
substrate specificity of GSK3beta
-
-
-
additional information
?
-
-
does not phosphorylate tau at epitope Ser 262
-
-
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
(Substrate)
LITERATURE
(Substrate)
COMMENTARY
(Product)
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
ATP + amyloid precursor protein
ADP + phosphorylated amyloid precursor protein
show the reaction diagram
-
-
-
-
?
ATP + beta-catenin
ADP + phosphorylated beta-catenin
show the reaction diagram
-
-
-
-
?
ATP + c-Myc
ADP + phosphorylated c-Myc
show the reaction diagram
-
-
-
-
?
ATP + cyclin D
ADP + phosphorylated cyclin D
show the reaction diagram
-
-
-
-
?
ATP + cyclin E
ADP + phosphorylated cyclin E
show the reaction diagram
-
-
-
-
?
ATP + glycogen synthase
ADP + glycogen synthase phosphate
show the reaction diagram
-
-
-
-
?
ATP + nuclear factor-kappaB
ADP + phosphorylated nuclear factor-kappaB
show the reaction diagram
-
-
-
-
?
ATP + p53
ADP + phosphorylated p53
show the reaction diagram
-
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-, Q3UVR3
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
prior phosphorylation of tau by isoenzyme TPKII strongly enhances the action of TPKI
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
regulates PDH and participates in energy metabolism and acetylcholine synthesis
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
microtubule-associated protein
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
phosphorylates tau on S202, T231, S396, and S400 but not on S262, S235, and S404. Phosphorylates tau directly at S202 but requires the previous phosphorylation on S235 to phosphorylate T231, once a priming kinase phosphorylates S404, GSK3beta sequentially phosphorylates S400 and then S396
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
Rattus norvegicus Sprague-Dawley
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
Rattus norvegicus Wistar
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
Rattus norvegicus Wistar
-
-
-
?
ATP + SC35
ADP + phosphorylated SC35
show the reaction diagram
-
substrate prephosphorylated SC35, SC35 is a member of the SR family of serine/arginine-rich splicing factors
-
-
?
ATP + tau protein
ADP + phosphorylated tau protein
show the reaction diagram
-
tau in Alzheimer disease brain is highly phosphorylated and aggregates into paired helical filaments comprising characteristic neurofibrillary tangles, overview
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
-
-
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
-
-
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
-
14-3-3 connects glycogen synthase kinase-3 beta to tau within a brain microtubule-associated tau phosphorylation complex
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
-
abnormal hyperphosphorylation of tau by PKA and GSK-3 is associated with Alzheimer's disease and other tauopaties leading to neuronal degeneration
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
-
activity in organisms with mutated APP and tau, not in wild-type, overview
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
-
cdk5 associated with p25
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
-
cdk5 substrate in brain, cdk5 associated with p39, tau is a microtubule-associated and developmentally regulated protein involved in axonal development in neurons, tau phosphorylation by cyclin-dependent kinase 5/p39 during brain development reduces its affinity for microtubules
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
-
hyperphosphorylation of tau by CDK5 is involved in apoptosis and neurodegeneration in Alzheimer's disease, overview
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
-
phosphorylation of tau, especially at the primed epitope T231 negatively regulates tau-microtubule interactions, different effects of phosphorylation on primed T231 and unprimed S396/S404 epitopes of tau, overview
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
-
protein 14-3-3 mediates phosphorylation of microtubule-associated protein tau by serum- and glucocorticoid-induced protein kinase 1 SGK1, which forms an activated ternary complex with protein 14-3-3theta
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
-
regulation, overview
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
-
tau is microtubule-associated, phopshorylation at T231 by CDK5 causes its release into the cytoplasm
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
-
tau is primarily found in neurons, regulation of tau phosphorylation by GSK3beta via interaction with FRAT-1 and FRAT-2, i.e. frequently rearranged in advanced T-cell lymphoma proteins
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
-
tau phosphorylation by GSK-3beta is involved in development of neurodegenerative Alzheimer's disease, the tau phosphorylation activity by GSK-3beta is further increased by soluble toxic beta-amyloid oligomers, overview
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
-
tau phosphorylation in vivo is stimulated by extracellular signal-regulated kinase Erk phosphorylation and apolipoprotein isozyme E4, to a lesser extent by isozyme apoE3, overview
-
-
?
additional information
?
-
-
-
-
-
-
additional information
?
-
P18266
enzyme is involved in the cellular response to insulin, the enzyme is highly phosphorylated on tyrosine and thus active in resting cells
-
-
-
additional information
?
-
-
possible role of the sgg protein in a signal transduction pathway necessary for intercellular communication at different stages of development
-
-
-
additional information
?
-
-
implicated in cell-fate determination and differentiation, phosphorylates several regulatory proteins that are activated by dephosphorylation in response to hormones or growth factors
-
-
-
additional information
?
-
-
enzyme of the lithium-sensitive wnt signaling pathway
-
-
-
additional information
?
-
-
enzyme acts as a repressor of engrailed autoregulation
-
-
-
additional information
?
-
-
enzyme forms part of the wingless signalling pathway. GSK-3beta activity is negatively regulated by phosphorylation on serine 9 and positively regulated by phosphorylation on tyrosine 216. Enzyme may also be regulated at the transcriptional level
-
-
-
additional information
?
-
-
implicated in the hormonal control of several regulatory proteins including glycogen synthase and the transcription factor c-jun
-
-
-
additional information
?
-
-
MDS1 is not essential during normal vegetative growth but appears to be required for meiosis
-
-
-
additional information
?
-
P51136
enzyme regulates cell fate in Dictyostelium
-
-
-
additional information
?
-
P21965
enzyme is involved in the induction of meiosis
-
-
-
additional information
?
-
-
MCK1 encodes a positive regulator of meiosis and spore formation. MCK1 is required in vegetative cells for basal IME1 expression, it is also required for efficient ascus maturation. MCK1 plays a role in governing centromere function during vegetative growth as well as sporulation
-
-
-
additional information
?
-
Q39010, Q39012, Q39019
AtK-1 kinase is involved in reproduction-specific processes
-
-
-
additional information
?
-
-
abnormal phosphorylation of tau in dividing cells leads to its accumulation in the cytosol as microtubule-free form, Cdk5 is involved in neurodegenerative mechanisms
-
-
-
additional information
?
-
-
activation and deregulation of GSK-3, e.g. by wortmannin or GF-109203X, induces Alzheimer-like tau hyperphosphorylation in hippocampus, the hyperphosphorylated tau forms neurofibrillary tangle
-
-
-
additional information
?
-
-
CDK5-dependent clustering of endoplasmic reticulum ER and mitochondria during ceramide-mediated neuronal death: neurotoxic calcium transfer from ER to mitochondria is regulated by cyclin-dependent kinase 5-dependent phosphorylation of tau, inhibition of the process leads to cell death
-
-
-
additional information
?
-
-
glycogen synthase kinase-3beta also performs serine/threonine protein kinase reaction, EC 2.7.11.1, with other substrates than tau, e.g. it phosphorylates the glycogen synthase
-
-
-
additional information
?
-
-
GSK-3 affects the tau-mRNA splicing of exon 10 via phosphorylation of the splicing factors of the serine/arginine-rich splicing factor SR family, e.g. SC35, leading to priming and dislocation of the splicing factor, aberrant tau splicing contributes to tauopathies including Alzheimer's disease, overview
-
-
-
additional information
?
-
-
GSK3beta and PKA work coordinatedly on tau phosphorylation
-
-
-
additional information
?
-
-
naturally occurring V717I mutation of the amyloid precursor protein APP in a CT100 fragment of mutants leads to augmented age-dependent tau phosphorylation, followed by increased activation status of mitogen-activated protein kinase family members, e.g. ERK1/2, p38, and c-Jun NH2-terminal kinase, compared to the wild-type organism, naturally occurring V337M mutation of tau protein of mutants leads to age-dependent memory deficits
-
-
-
additional information
?
-
-
naturally occurring V717I mutation of the amyloid precursor protein APP in a CT100 fragment of organisms with Alzheimer's disease leads to augmented age-dependent tau phosphorylation, followed by increased activation status of mitogen-activated protein kinase family members, e.g. ERK1/2, p38, and c-Jun NH2-terminal kinase, compared to the wild-type organism, naturally occurring V337M mutation of tau protein of patients suffering from Alzheimer's disease leads to age-dependent memory deficits
-
-
-
additional information
?
-
-
phosphorylated tau is important in cytoskeleton assembly
-
-
-
additional information
?
-
-
protein 14-3-3 facilitates tau phosphorylation by SGK1 and regulates its subcellular localization in the nucleus or cytoplasm, overview
-
-
-
additional information
?
-
-
rapid, reversible cold-water stress-induced hyperphosphorylation of tau S199, S202, T205, T231, and S235 in hippocampal and cerebral region of the brain, hyperphosphorylation of tau is associated to the Alzheimer's disease
-
-
-
additional information
?
-
-
tau becomes a more favorable substrate for GSK-3 when it is prephosphorylated by PKA in rat brain, inhibition of tau hyperphosphorylation inhibits an associated loss in spatial memory
-
-
-
additional information
?
-
-
the enzyme participates in Alzheimer's disease
-
-
-
METALS and IONS
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
Mg2+
-
binding site structure
Mg2+
-
-
Zn2+
-
high zinc concentrations (0.1-0.5 mM) increase glycogen synthase kinase-3beta phosphorylation on tyrosine 216, a phosphorylation associated with increased activity of this tau kinase, whereas the phosphorylation of GSK-3alpha at Y279 and the level of total GSK-3beta are not affected
additional information
-
not activated by K+, Ca2+ or Zn2+
INHIBITORS
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
(2'Z, 3'E)-6-bromoindirubin-3'-oxime
-
-
-
(2'Z,3'E)-6-bromoindirubin-3'-oxime
-
-
(Rp)-adenosine 3',5'-cyclic monophosphorothionate triethyl ammonium salt
-
inhibitor of PKA
1-(4-methoxyphenyl)-6-(5-[[3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)-1H-benzimidazole
-
-
1-(4-methoxyphenyl)-6-(5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)-1H-benzimidazole
-
-
1-(cyclopropylmethyl)-3-[4-(5,6-difluoro-1-benzofuran-3-yl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]-1H-indole-5-carbonitrile
-
-
1-ethyl-3-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)urea
-
-
-
1-methyl-5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-amine
-
-
1-methyl-6-(5-[[3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)-1H-benzimidazole
-
-
2-(1,3-benzodioxol-5-yl)-5-[(3-fluoro-4-methoxybenzyl)sulfanyl]-1,3,4-oxadiazole
-
-
2-(1-benzofuran-5-yl)-5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazole
-
-
2-(2,3-dihydro-1-benzofuran-5-yl)-5-[(3-fluoro-4-methoxybenzyl)sulfanyl]-1,3,4-oxadiazole
-
-
2-(2,3-dihydro-1-benzofuran-5-yl)-5-[(3-fluorobenzyl)sulfanyl]-1,3,4-oxadiazole
-
-
2-(2,3-dihydro-1-benzofuran-5-yl)-5-[(4-methoxybenzyl)sulfanyl]-1,3,4-oxadiazole
-
-
2-(2,3-dihydro-1-benzofuran-5-yl)-5-[2-(3-fluorophenyl)ethyl]-1,3,4-oxadiazole
-
-
2-(2,3-dihydro-1-benzofuran-5-yl)-5-[[(3-fluorophenyl)sulfanyl]methyl]-1,3,4-oxadiazole
-
-
2-(2,3-dihydro-1-benzofuran-5-yl)-5-[[3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazole
-
-
2-(2,3-dihydro-1-benzofuran-5-yl)-5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazole
-
-
2-(3-ethylpiperazin-1-yl)-N-[6-(3-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]acetamide
-
-
-
2-(benzylsulfanyl)-5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazole
-
-
2-amino-N-(2'-(cyclohex-2''-enyl)acetyl)acetimide
-
-
2-amino-N-(2'-(phenyl)acetyl)propanimide
-
-
2-chloro-5-[(2,5-dioxo-4-phenyl-2,5-dihydro-1H-pyrrol-3-yl)amino]benzoic acid
-
-
-
2-chloro-5-[[4-(2-chlorophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
-
-
-
2-chloro-5-[[4-(2-nitrophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
-
-
-
2-chloro-5-[[4-(3-chlorophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
-
-
-
2-chloro-5-[[4-(3-methoxyphenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
-
-
-
2-chloro-5-[[4-(3-nitrophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
-
-
-
2-chloro-5-[[4-(4-chlorophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
-
-
-
2-cyanoethyl alsterpaullone
-
-
-
2-methyl-N-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)propanamide
-
-
-
2-[(2-chlorobenzyl)sulfanyl]-5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazole
-
-
2-[(3-chloro-4-methoxybenzyl)sulfanyl]-5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazole
-
-
2-[(3-chlorobenzyl)sulfanyl]-5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazole
-
-
2-[(4-chlorobenzyl)sulfanyl]-5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazole
-
-
2-[3-(4-methoxyphenyl)-1-benzofuran-5-yl]-5-[[3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazole
-
-
2-[3-(4-methoxyphenyl)-1-benzofuran-5-yl]-5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazole
-
-
3-(1-(2-(1H-imidazol-1-yl)ethyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-1-phenyl-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1-methyl-1H-pyrrolo[3,2-b]pyridin-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-(3-(dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-(3-(piperidin-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-(3-hydroxypropyl)-1H-indol-3-yl)-4-(1-methyl-1H-pyrrolo[3,2-b]pyridin-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-(4-(1H-imidazol-1-yl)butyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-benzofuran-3-yl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-benzofuran-3-yl)-4-(1-methyl-7-phenoxy-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-benzofuran-3-yl)-4-(5-bromo-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-benzofuran-3-yl)-4-(5-cyclopropyl-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-benzofuran-3-yl)-4-(5-fluoro-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-benzofuran-3-yl)-4-(5-fluoro-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-benzofuran-3-yl)-4-(5-hydroxy-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-benzofuran-3-yl)-4-(5-iodo-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-benzofuran-3-yl)-4-(6-chloro-5-fluoro-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-benzofuran-3-yl)-4-(6-chloro-5-methoxy-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-benzofuran-3-yl)-4-(6-hydroxy-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-benzofuran-3-yl)-4-(6-iodo-5-methoxy-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-benzofuran-3-yl)-4-(7-hydroxy-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-benzofuran-3-yl)-4-[1-(3-hydroxypropyl)-5-phenoxy-1H-indol-3-yl]-1H-pyrrole-2,5-dione
-
-
3-(1-benzofuran-3-yl)-4-[1-methyl-5-(morpholin-4-yl)-1H-indol-3-yl]-1H-pyrrole-2,5-dione
-
-
3-(1-benzofuran-3-yl)-4-[5-(benzyloxy)-1H-indol-3-yl]-1H-pyrrole-2,5-dione
-
-
3-(1-benzofuran-3-yl)-4-[5-bromo-1-(3-hydroxypropyl)-1H-indol-3-yl]-1H-pyrrole-2,5-dione
-
-
3-(1-benzofuran-3-yl)-4-[6-(benzyloxy)-1-methyl-1H-indol-3-yl]-1H-pyrrole-2,5-dione
-
-
3-(1-benzofuran-3-yl)-4-[7-(hydroxymethyl)-1-methyl-1H-indol-3-yl]-1H-pyrrole-2,5-dione
-
-
3-(1-benzofuran-3-yl)-4-[7-(methoxymethyl)-1-methyl-1H-indol-3-yl]-1H-pyrrole-2,5-dione
-
-
3-(1-methyl-1H-pyrrolo[3,2-b]pyridin-3-yl)-4-(1-(2-morpholinoethyl)-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-methyl-1H-pyrrolo[3,2-b]pyridin-3-yl)-4-(1-(3-morpholinopropyl)-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(2,3-dihydro-1H-indol-1-yl)-4-(2-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
-
3-(2,3-dihydro-1H-indol-1-yl)-4-(2-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
-
3-(2,3-dihydro-1H-indol-1-yl)-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
-
3-(2,3-dihydro-1H-indol-1-yl)-4-(4-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
-
3-(2-chlorophenyl)-4-(2,3-dihydro-1H-indol-1-yl)-1H-pyrrole-2,5-dione
-
-
-
3-(2-chlorophenyl)-4-(phenylamino)-1H-pyrrole-2,5-dione
-
-
-
3-(2-chlorophenyl)-4-[(3,5-dichloro-4-hydroxyphenyl)amino]-1H-pyrrole-2,5-dione
-
-
-
3-(2-chlorophenyl)-4-[(3-chlorophenyl)amino]-1H-pyrrole-2,5-dione
-
-
-
3-(2-chlorophenyl)-4-[(3-hydroxyphenyl)amino]-1H-pyrrole-2,5-dione
-
-
-
3-(2-chlorophenyl)-4-[[4-(methylsulfanyl)phenyl]amino]-1H-pyrrole-2,5-dione
-
-
-
3-(2-methoxyphenyl)-4-(phenylamino)-1H-pyrrole-2,5-dione
-
-
-
3-(2-methoxyphenyl)-4-[[4-(methylsulfanyl)phenyl]amino]-1H-pyrrole-2,5-dione
-
-
-
3-(3-chlorophenyl)-4-(2,3-dihydro-1H-indol-1-yl)-1H-pyrrole-2,5-dione
-
-
-
3-(3-chlorophenyl)-4-[(3,5-dichloro-4-hydroxyphenyl)amino]-1H-pyrrole-2,5-dione
-
-
-
3-(3-chlorophenyl)-4-[(3-hydroxyphenyl)amino]-1H-pyrrole-2,5-dione
-
-
-
3-(3-chlorophenyl)-4-[[4-(methylsulfanyl)phenyl]amino]-1H-pyrrole-2,5-dione
-
-
-
3-(3-methoxyphenyl)-4-[[4-(methylsulfanyl)phenyl]amino]-1H-pyrrole-2,5-dione
-
-
-
3-(3-nitrophenyl)-4-(phenylamino)-1H-pyrrole-2,5-dione
-
-
-
3-(4-chlorophenyl)-4-(2,3-dihydro-1H-indol-1-yl)-1H-pyrrole-2,5-dione
-
-
-
3-(4-chlorophenyl)-4-(phenylamino)-1H-pyrrole-2,5-dione
-
-
-
3-(4-chlorophenyl)-4-[(3,5-dichloro-4-hydroxyphenyl)amino]-1H-pyrrole-2,5-dione
-
-
-
3-(4-chlorophenyl)-4-[(3-chlorophenyl)amino]-1H-pyrrole-2,5-dione
-
-
-
3-(4-chlorophenyl)-4-[(3-hydroxyphenyl)amino]-1H-pyrrole-2,5-dione
-
-
-
3-(4-chlorophenyl)-4-[(4-hydroxyphenyl)amino]-1H-pyrrole-2,5-dione
-
-
-
3-(4-chlorophenyl)-4-[methyl(phenyl)amino]-1H-pyrrole-2,5-dione
-
-
-
3-(4-chlorophenyl)-4-[[4-(methylsulfanyl)phenyl]amino]-1H-pyrrole-2,5-dione
-
-
-
3-(4-methoxyphenyl)-4-(phenylamino)-1H-pyrrole-2,5-dione
-
-
-
3-(4-methoxyphenyl)-4-[[4-(methylsulfanyl)phenyl]amino]-1H-pyrrole-2,5-dione
-
-
-
3-(5,6-difluoro-1-benzofuran-3-yl)-4-(1-methyl-1H-benzo[g]indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(5,7-dibromo-1-methyl-1H-indol-3-yl)-4-(7-methoxy-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(5-bromo-1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(5-bromo-1-benzofuran-3-yl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(5-bromo-1-methyl-1H-indol-3-yl)-4-(7-methoxy-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(5-bromo-1-methyl-1H-indol-3-yl)-4-[6-(4-methoxyphenoxy)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
-
-
3-(5-bromo-1-methyl-1H-indol-3-yl)-4-[6-(hydroxymethyl)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
-
-
3-(5-bromo-1-methyl-1H-indol-3-yl)-4-[6-(prop-2-en-1-yloxy)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
-
-
3-(5-bromo-1-methyl-1H-indol-3-yl)-4-[6-(prop-2-yn-1-yloxy)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
-
-
3-(5-chloro-1-methyl-1H-indol-3-yl)-4-(5-fluoro-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(5-fluoro-1-benzofuran-3-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(5-fluoro-1-benzofuran-3-yl)-4-(5-iodo-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(5-fluoro-1-benzofuran-3-yl)-4-(6-hydroxy-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(5-fluoro-1-methyl-1H-indol-3-yl)-4-(6-hydroxy-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(5-fluoro-1-methyl-1H-indol-3-yl)-4-[6-(hydroxymethyl)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
-
-
3-(5-fluoro-1-methyl-1H-indol-3-yl)-4-[6-(methoxymethyl)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
-
-
3-(5-fluoro-6-iodo-1-methyl-1H-indol-3-yl)-4-(7-methoxy-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(5-methoxy-1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(5-methoxy-1-(3-(dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(5H-[1,3]dioxolo[4,5-f]indol-7-yl)-4-(5-fluoro-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(6-bromo-1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(6-bromo-1-(3-(dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(6-chloro-5-fluoro-1-methyl-1H-indol-3-yl)-4-(6-methoxy-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(6-chloro-5-fluoro-1-methyl-1H-indol-3-yl)-4-(7-methoxy-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(6-chloro-5-fluoro-1-methyl-1H-indol-3-yl)-4-[6-(cyclobutylmethoxy)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
-
-
3-(6-chloro-5-fluoro-1-methyl-1H-indol-3-yl)-4-[6-(cyclopropylmethoxy)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
-
-
3-(6-chloro-5-fluoro-1-methyl-1H-indol-3-yl)-4-[6-(hydroxymethyl)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
-
-
3-(6-fluoro-1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(6-fluoro-1-(3-(dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(7-methoxy-1-benzofuran-3-yl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(7-methoxy-1-benzofuran-3-yl)-4-[1-methyl-6-(trifluoromethyl)-1H-indol-3-yl]-1H-pyrrole-2,5-dione
-
-
3-([[5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazol-2-yl]sulfanyl]methyl)benzo-nitrile
-
-
3-benzyl-N-[5-bromo-6-(furan-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrrolidine-1-carboxamide
-
-
-
3-phenyl-4-(phenylamino)-1H-pyrrole-2,5-dione
-
-
-
3-[(2,5-dioxo-4-phenyl-2,5-dihydro-1H-pyrrol-3-yl)amino]benzoic acid
-
-
-
3-[(3,5-dichloro-4-hydroxyphenyl)amino]-4-(2-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
-
3-[(3,5-dichloro-4-hydroxyphenyl)amino]-4-(2-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
-
3-[(3,5-dichloro-4-hydroxyphenyl)amino]-4-(3-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
-
3-[(3,5-dichloro-4-hydroxyphenyl)amino]-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
-
3-[(3,5-dichloro-4-hydroxyphenyl)amino]-4-(4-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
-
3-[(3,5-dichloro-4-hydroxyphenyl)amino]-4-(4-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
-
3-[(3,5-dichloro-4-hydroxyphenyl)amino]-4-phenyl-1H-pyrrole-2,5-dione
-
-
-
3-[(3-chloro-4-hydroxyphenyl)amino]-4-(2-chlorophenyl)-1H-pyrrole-2,5-dione
-
-
-
3-[(3-chloro-4-hydroxyphenyl)amino]-4-(2-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
-
3-[(3-chloro-4-hydroxyphenyl)amino]-4-(2-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
-
3-[(3-chloro-4-hydroxyphenyl)amino]-4-(3-chlorophenyl)-1H-pyrrole-2,5-dione
-
-
-
3-[(3-chloro-4-hydroxyphenyl)amino]-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
-
3-[(3-chloro-4-hydroxyphenyl)amino]-4-(4-chlorophenyl)-1H-pyrrole-2,5-dione
-
-
-
3-[(3-chlorophenyl)amino]-4-(2-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
-
3-[(3-chlorophenyl)amino]-4-(2-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
-
3-[(3-chlorophenyl)amino]-4-(3-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
-
3-[(3-chlorophenyl)amino]-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
-
3-[(3-chlorophenyl)amino]-4-(4-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
-
3-[(3-chlorophenyl)amino]-4-phenyl-1H-pyrrole-2,5-dione
-
-
-
3-[(3-hydroxyphenyl)amino]-4-(2-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
-
3-[(3-hydroxyphenyl)amino]-4-(2-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
-
3-[(3-hydroxyphenyl)amino]-4-(3-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
-
3-[(3-hydroxyphenyl)amino]-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
-
3-[(3-hydroxyphenyl)amino]-4-(4-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
-
3-[(3-hydroxyphenyl)amino]-4-phenyl-1H-pyrrole-2,5-dione
-
-
-
3-[(4-hydroxyphenyl)amino]-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
-
3-[(5E)-5-methyl-4-oxo-2-hydroxy-5-octenyl]glutarimide
-
-
3-[([5-[1-(4-methoxyphenyl)-1H-benzimidazol-6-yl]-1,3,4-oxadiazol-2-yl]sulfanyl)methyl]benzonitrile
-
-
3-[([5-[3-(4-methoxyphenyl)-1-benzofuran-5-yl]-1,3,4-oxadiazol-2-yl]sulfanyl)methyl]benzonitrile
-
-
3-[4-(6-ethyl-1-benzofuran-3-yl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]-1-methyl-1H-indole-5-carbonitrile
-
-
3-[5-(cyclopropylethynyl)-1-methyl-1H-indol-3-yl]-4-(5-fluoro-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
-
3-[6-(4-chlorophenyl)-5-fluoro-1-methyl-1H-indol-3-yl]-4-(7-methoxy-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
-
3-[6-(benzyloxy)-1-methyl-1H-indol-3-yl]-4-(5-fluoro-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
-
3-[6-(hydroxymethyl)-1-benzofuran-3-yl]-4-[7-(hydroxymethyl)-1-methyl-1H-indol-3-yl]-1H-pyrrole-2,5-dione
-
-
3-[methyl(phenyl)amino]-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
-
3-[methyl(phenyl)amino]-4-phenyl-1H-pyrrole-2,5-dione
-
-
-
3-[[4-(2-chlorophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
-
-
-
3-[[4-(3-chlorophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
-
-
-
3-[[4-(3-methoxyphenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
-
-
-
3-[[4-(3-nitrophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
-
-
-
3-[[4-(4-chlorophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
-
-
-
3-[[4-(4-methoxyphenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
-
-
-
3-[[4-(methylsulfanyl)phenyl]amino]-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
-
3-[[4-(methylsulfanyl)phenyl]amino]-4-(4-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
-
3-[[4-(methylsulfanyl)phenyl]amino]-4-phenyl-1H-pyrrole-2,5-dione
-
-
-
3alpha,5alpha-tetrahydroprogesterone
-
decreases only expression of GSK-3 beta in the cerebellum but not in the hypothalamus
4,5-diphenyl-1H-pyrazolo[3,4-c]pyridazin-3-amine
-
-
4-benzyl-2-methyl-1, 2, 4-thiadiazolidine-3,5-dione
-
TDZD-8
-
4-benzyl-2-methyl-1,2,4-thiadiazolidine-3,5-dione
-
-
4-benzyl-2-methyl-1,2,4-thiadiazolidine-3,5-dione
-
-
4-phenyl-1H-pyrazolo[3,4-b]pyridin-3-amine
-
-
4-{(2R)-2-[(1R,3R,5S)-3,5-dimethyl-2-oxocyclohexyl]-2-hydroxyethyl}piperidine-2,6-dione
-
-
5-(2,3-dihydro-1-benzofuran-5-yl)-N-(3-fluorobenzyl)-1,3,4-oxadiazol-2-amine
-
-
5-(5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)-1H-indazole
-
-
5-([ [5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazol-2-yl]sulfanyl]methyl)-2-methoxybenzonitrile
-
-
5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-amine
-
-
5-phenyl-1H-pyrazolo[3,4-c]pyridazin-3-amine
-
-
5-phenyl-1H-pyrazolo[3,4-c]pyridin-3-amine
-
-
5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-amine
-
-
5-phenyl[1,2]oxazolo[5,4-b]pyridin-3-amine
-
-
5alpha-dihydroprogesterone
-
decreases only expression of GSK-3 beta in the cerebellum but not in the hypothalamus
6-(5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)-1,3-benzothiazole
-
-
6-(5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)imidazo[1,2-a]pyridine
-
-
6-(5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)quinoline
-
-
6-bromo-5-methylindirubin-3'-oxime
-
potent inhibitor
-
6-bromo-indirubin-3'-acetoxime
-
potent inhibitor
-
6-bromo-indirubin-3'-oxime
-
selective and potent GSK3beta inhibitor
-
6-bromo-indirubin-3'-oxime
-
potent inhibitor
-
6-bromo-indirubin-3'-oxime
-
-
-
6-bromoindirubin-3'-oxim
-
-
6-bromoindirubin-3'-oxime
-
-
6-O-methyl-7-O-alpha-L-rhamnopyranosyldaidzein
-
-
7-O-alpha-L-rhamnopyranosyldaidzein
-
-
A-582941
-
attenuates beta-amyloid peptide 1-42-induced activation of GSK-3beta
alpha-bungarotoxin
-
attenuates beta-amyloid peptide 1-42-induced activation of GSK-3beta
alsterpaullone
-
-
AMP-PNP
-
ATP analogue adenosine 5'-(beta,gamma-imino)triphosphate
AR-A014418
-
selective ATP-competitive inhibitor of GSK3
ATP
-
strongly inhibited by elevated concentrations of ATP uncomplexed with magnesium
ATP
-
strongly inhibited by elevated concentrations of ATP uncomplexed with magnesium
Butyrolactone
-
cdk5 inhibitor, isoenzyme TPKII
caffeic acid
-
0.02 mg/ml caffeic acid decreases the activating phosphorylation of GSK-3beta
carteriosulfonic acid A
-
low micromolar inhibitor of GSK-3beta
carteriosulfonic acid B
-
low micromolar inhibitor of GSK-3beta
carteriosulfonic acid C
-
low micromolar inhibitor of GSK-3beta
CHIR98023
-
attenuates beta-amyloid peptide 1-42-induced activation of GSK-3beta
CT99021
-
-
-
cycloheximide
-
-
dantrolene
-
in the presence of dantrolene, GSK-3beta activation and tau phosphorylation are decreased
disheveled protein
-
-
-
DMSO
-
complete inhibition at 0.4% (v/v)
enzastaurin
-
activation-related phosphorylation of Y216/Y276 is dramatically decreased following exposure to enzastaurin whereas the inhibitory phosphorylation of S21 is significantly up-regulated in glioma cells. GSK3 inhibition results in glioma cell death and reduced tumorigenicity
GF 109203X
-
-
GSK-3 inhibitor IX
-
-
-
GSK3betaI
-
0.0001 mM
-
GTPgamma-S
-
-
Insulin
-
insulin induces phosphorylation of the Ser9 residue, thereby inactivating GSK-3beta
-
insulin-like growth factor-I
-
-
-
kenpaullone
-
-
KRM-189
-
74% inhibition at 0.01 mM, competes with ATP for GSK-3beta, leading to decreased Vmax and constant Km with increasing concentrations of ATP
KRM-191
-
84% inhibition at 0.01 mM, competes with ATP for GSK-3beta, leading to decreased Vmax and constant Km with increasing concentrations of ATP
KRM-192
-
75% inhibition at 0.01 mM
KRM-195
-
80% inhibition at 0.01 mM
KRM-296
-
65% inhibition at 0.01 mM
KRM-7777
-
65% inhibition at 0.01 mM
leptin
-
-
-
LiCl
-
slight inhibition of T231 phosphorylation by p25-Cdk5 kinase complex
LiCl
-
pharmacological inhibition of GSK3 in old transgenic mice by chronic treatment with lithium, leads to a reduction of the age-dependent increase in tau hyperphosphorylation
LiCl
-
71% inhibition at 0.01 mM
LiCl
-
lithium is a weak inhibitor of GSK3beta, lithium dose-dependently inhibits GSK3beta through the phosphorylation of serine 9 residue
LiCl
-
GSK-3-specific inhibitor
LiCl
-
complete inhibition at 2 mM
LiCl
-
a dose-dependent increase in phosphorylation of GSK-3beta occurs after treatment with LiCl (5-20 mM)
lithium
-
after inhibition of GSK-3 in cortical neurons, the splicing factor SC35 is nuclearly redistributed and enriched in nuclear speckles and colocalizes with the kinase
lithium chloride
Q9WV60
15 mM
lithium chloride
-
-
methyl 3-([[5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazol-2-yl]sulfanyl]methyl)benzoate
-
-
N-(1H-pyrazolo[3,4-b]pyridin-3-yl)butanamide
-
-
-
N-(4,5-diphenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl)butanamide
-
-
-
N-(5,6-diphenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)cyclopropanecarboxamide
-
-
-
N-(5-bromo-6-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)-4-methylpiperidine-1-carboxamide
-
-
-
N-(5-bromo-6-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)cyclopropanecarboxamide
-
-
-
N-(5-chloro-6-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)cyclopropanecarboxamide
-
-
-
N-(5-cyano-6-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)cyclopropanecarboxamide
-
-
-
N-(5-phenyl-1H-indazol-3-yl)butanamide
-
-
-
N-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)acetamide
-
-
-
N-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)butanamide
-
-
-
N-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)cyclopentanecarboxamide
-
-
-
N-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)methanesulfonamide
-
-
N-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)propanamide
-
-
-
N-(5-phenyl-1H-pyrazolo[3,4-c]pyridin-3-yl)butanamide
-
-
-
N-(5-phenyl-1H-pyrazolo[4,3-d]pyrimidin-3-yl)butanamide
-
-
-
N-(6-phenyl-1H-indazol-3-yl)cyclopropanecarboxamide
-
-
-
N-(6-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)cyclopropanecarboxamide
-
-
-
N-[4-[3-(4-ethylpiperazin-1-yl)propyl]-5-phenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl]butanamide
-
-
-
N-[4-[3-(dimethylamino)propyl]-5-phenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl]butanamide
-
-
-
N-[4-[3-(morpholin-4-yl)propyl]-5-phenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl]butanamide
-
-
-
N-[4-[ethyl(piperidin-1-ylmethyl)amino]-5-phenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl]butanamide
-
-
-
N-[4-[methyl(piperidin-1-yl)amino]-5-phenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl]butanamide
-
-
-
N-[5-(2,3-difluorophenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
-
-
-
N-[5-(2-chlorophenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
-
-
-
N-[5-(2-fluorophenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
-
-
-
N-[5-(3-fluorophenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
-
-
-
N-[5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
-
-
-
N-[5-(6,6-difluorocyclohexa-1,3-dien-1-yl)-4-[3-(dimethylamino)propyl]-1H-pyrazolo[3,4-c]pyridazin-3-yl]butanamide
-
-
-
N-[5-(biphenyl-4-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
-
-
-
N-[5-(naphthalen-1-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
-
-
-
N-[5-(naphthalen-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
-
-
-
N-[5-(pyridin-3-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
-
-
-
N-[5-(pyridin-4-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
-
-
-
N-[5-bromo-6-(4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-4-(4-ethylpiperazin-1-yl)butanamide
-
-
-
N-[5-bromo-6-(4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-4-methylpiperidine-1-carboxamide
-
-
-
N-[5-bromo-6-(4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
-
N-[5-bromo-6-(furan-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
-
N-[5-bromo-6-(tetrahydrothiophen-3-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
-
N-[5-bromo-6-(thiophen-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-2-(4-methylpiperidin-1-yl)acetamide
-
-
-
N-[5-bromo-6-(thiophen-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
-
N-[5-chloro-6-(4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
-
N-[5-phenyl-4-[3-(pyrrolidin-1-yl)propyl]-1H-pyrazolo[3,4-c]pyridazin-3-yl]butanamide
-
-
-
N-[6-(1H-indol-5-yl)-1H-indazol-3-yl]cyclopropanecarboxamide
-
-
-
N-[6-(2,5-difluorophenyl)-1H-indazol-3-yl]cyclopropanecarboxamide
-
-
-
N-[6-(2-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
-
N-[6-(2-methoxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
-
N-[6-(2H-pyrrol-2-yl)-1H-indazol-3-yl]cyclopropanecarboxamide
-
-
-
N-[6-(3,4-dihydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
-
N-[6-(3-bromo-4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
-
N-[6-(3-chloro-4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
-
N-[6-(3-fluorophenyl)-1H-indazol-3-yl]cyclopropanecarboxamide
-
-
-
N-[6-(3-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
-
N-[6-(3-methoxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
-
N-[6-(3-sulfamoylphenyl)-1H-indazol-3-yl]cyclopropanecarboxamide
-
-
-
N-[6-(4-hydroxyphenyl)-1H-indazol-3-yl]cyclopropanecarboxamide
-
-
-
N-[6-(4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-4-methylpiperidine-1-carboxamide
-
-
-
N-[6-(4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
-
N-[6-(4-hydroxyphenyl)-5-methyl-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
-
N-[6-(4-hydroxyphenyl)-5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
-
N-[6-(4-methoxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
-
N-[6-(furan-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
-
N-[6-(furan-3-yl)-1H-indazol-3-yl]cyclopropanecarboxamide
-
-
-
N-[6-(tetrahydrothiophen-3-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
-
N-[6-(thiophen-2-yl)-1H-indazol-3-yl]cyclopropanecarboxamide
-
-
-
N-[6-(thiophen-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
-
N-[6-(thiophen-3-yl)-1H-indazol-3-yl]cyclopropanecarboxamide
-
-
-
naramycin B
-
-
Nicotine
-
attenuates beta-amyloid peptide 1-42-induced activation of GSK-3beta
p25
-
p25 overexpressing mice have reduced GSK3beta activity
-
progesterone
-
decreases expression and phosphorylation of GSK-3 beta in the cerebellum but not in the hypothalamus, regulation of tau expression and phosphorylation by progesterone may contribute to the hormonal regulation of cerebellar function by the modification of neuronal cytoskeleton
Protein kinase C
-
protein kinase C inhibits GSK-3beta by phosphorylating its auto-inhibitory domain at Ser9
-
Ro 31-8220
-
-
roscovitine
-
complete inhibition of T231 phosphorylation by 25-Cdk5 kinase complex
roscovitine
-
inhibition of CDK5
roscovitine
-
Cdk5 inhibitor
SB 216743
-
-
-
SB 216763
-
GSK-3-specific inhibitor
-
SB-216763
-
specific inhibitor of GSK-3beta
SB-216763
-
selective ATP-competitive inhibitor of GSK3
SB-415286
-
-
-
SB-415286
-
complete inhibition at 0.005 mM
-
SB216763
-
specific GSK-3 inhibitor
-
SB216763
-
potent and selective cell permeable ATP-competitive inhibitor of GSK3
-
SRN-003-556
-
-
staurosporine
-
-
TDZD-8
-
selective GSK-3beta inhibitor, induces phosphorylation of the Ser9 residue, thereby inactivating GSK-3beta
trans-activating transcriptor-eIF2B
-
acts as a competitive inhibitor of GSK-3
-
ZM336372
-
inhibits GSK-3beta through phosphorylation at Ser9, a dose-dependent increase in phosphorylation of GSK-3beta occurs after treatment with ZM336372 (0.025-0.1 mM)
methyllycaconitine
-
attenuates beta-amyloid peptide 1-42-induced activation of GSK-3beta
additional information
-
no inhibition of the p25-Cdk5 kinase complex by PD98059 and SB203580
-
additional information
-
phosphorylation of GSK3beta at S9 inhibits the enzyme
-
additional information
-
phosphorylation of GSK3beta at S9 inhibits the enzyme, the phosphorylation at Ser9 is inhibited by wortmannin or GF-109203X, this inhibition is eliminated by inhibition of GSK-3 by a different inhibitor
-
additional information
-
inactivating phosphorylation of Ser9 of TPKI/GSK3beta in close correspondence with tau phosphorylation
-
additional information
-
Cdk5 over-activation leads to inhibition of GSK3 in young transgenic mice, in old transgenic animals the inhibition of GSK3 is lost
-
additional information
-
N-terminus negatively regulates tau phosphorlyation by blocking GSK3beta access, local conformational change induced by T231 phosphorylation is required for the phosphorylation of the C-terminus and hyperphosphorylation of tau
-
additional information
-
inhibition of GSK3 activity results in c-MYC activation, leading to the induction of Bax, Bim, DR4/DR5, and tumor necrosis factor-related apoptosis-inducing ligand expression and subsequent cytotoxicity. inhibition of GSK3 activity causes a dramatic decrease in intracellular nuclear factor-kappaB activity. Inhibition of GSK3 activity results in c-MYC-dependent glioma cell death through multiple mechanisms, all of which converge on the apoptotic pathways
-
additional information
-
cdk5 can negatively regulate GSK3beta activity through neuregulin/ErbB signaling, phosphorylation at the inhibitory GSK3beta-Ser9 site activates GSK3beta
-
additional information
-
Galphaq protein inhibits GSK-3beta via activation of protein kinase C
-
additional information
-
protein tau-associated novel protein kinase Cepsilon suppresses the GSK-3beta-mediated phosphorylation of protein tau through the phosphorylation of GSK-3beta by the kinase in vitro
-
additional information
-
not inhibited by 2-(2,3-dihydro-1-benzofuran-5-yl)-5-[(3-fluorobenzyl)oxy]-1,3,4-oxadiazole
-
additional information
-
galectin-3 regulates GSK-3beta activity/phosphorylation via the PI3K/AKT pathway
-
additional information
-
the 3-nitropropionic acid treatment induces GSK-3beta truncation, calpeptin prevents GSK-3beta cleavage and cell death induced by 3-nitropropionic acid
-
additional information
-
not inhibited by indirubin, indirubin-3'-oxime, 5-bromo-indirubin, 5-aminoindirubin-3'-oxime, 6-bromo-indirubin, 6-bromo-N-methyl-indirubin-3'-oxime, 6-bromo-N-methyl-indirubin-3'-acetoxime, 6-bromo-indirubin-3'diethyl phosphatoxime, indirubin-3'-methoxime, 6-bromo-5-nitroindirubin, 6-bromo-5-nitroindirubin-3'-oxime, and 6-bromo-5-methylindirubin
-
additional information
-
treatment with 1 CFU/cell bacillus Calmette-Guerin increases the phosphorylation of GSK3beta at serine 9 and therefore inhibits the activity to about 40% 1 h after stimulation
-
additional information
-
the crude organic extract of fermentation cultures of Streptomyces sp. strain H7667 inhibits growth of a yeast transformant (with cloned human GSK-3beta) at 37C, but shows no inhibition at 25C
-
additional information
-
desacyl-carteriosulfonic acid shows no GSK-3beta inhibitory activity at concentrations up to 0.05 mM
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
amyloid-beta 1-42 peptide
-
0.005 mM
-
AT7519
-
0.0005 mM AT7519 inhibits glycogen synthase kinase 3beta phosphorylation, AT7519 dephosphorylates GSK-3beta independent of inhibition of transcription
beta-amyloid peptide
-
-
-
beta-amyloid peptide 1-42
-
0.01 mM, induces phosphorylation at Tyr216 activating GSK-3beta
-
cAMP
-
required for PKA activity
cAMP
-
required for PKA activation
carbonyl cyanide p-trifluoromethoxyphenylhydrazone
-
-
cholesterol 3-sulfate
-
potent stimulator for the GSK-3beta-mediated phosphorylation of tau protein (about 10fold stimulation in the presence of 0.003 mM)
cisplatin
-
GSK-3 is activated by cisplatin treatment of HEI-OC1 cells, 0.02 mM cisplatin induces phosphorylation of Tyr216 GSK-3beta in HEI-OC1 cells but reduces the phosphorylation of Ser9 GSK-3beta, the activity of GSK-3beta is regulated negatively by the phosphorylation of Ser9 and positively by the phosphorylation of Tyr216
CP-681301
-
CP-681301 treatment reverses the inhibition of GSK3beta activity
D-galactosylceramide-3-O-sulfate
-
potent stimulator for the GSK-3beta-mediated phosphorylation of tau protein (about 11fold stimulation in the presence of 0.003 mM)
Dickkopf-1
-
100 ng/ml
-
ether
-
dramatic increase in the phosphorylation level of Ser9 of TPKI/GSK3beta immediately and 10 min after ether administration, followed by rapid virtual reversion to baseline by 20 min, no significant changes in the protein level or Tyr216 phosphorylation level of the enzyme
forskolin
-
activates PKA
forskolin
-
forskolin specifically induces tau hyperphosphorylation by PKA at Ser214 resulting in increased phosphorylation at Ser199, Ser22, Ser396, and Ser404 in N2a/tau441 cells, forskolin has no effect on GSK-3
FRAT-2
-
i.e. frequently rearranged in advanced T-cell lymphoma protein 2, activates phosphorylation of primed sites of tau protein about 8fold, no effect on unprimed site phosphorylation
-
Frizzled-8
-
100 ng/ml
-
GF-109203X
-
-
p25
-
inducible cytotoxic expression factor required for Cdk5 activity, formation of a complex with Cdk5, p25 overexpression increases tau phosphorylation rate
-
p25
-
activator required for CDK5 activity, activation of CDK5 by p25 which is activated by cleavage of p35 to p25
-
p25
-
cyclin activator, dependent on, over 10fold increase in activity of CDK5
-
p35
-
tightly bound neuronal activator of cdk5, required for activity with regulatory function, p39 activates to a greater extent compared to p35 in vitro
-
p39
-
tightly bound neuronal activator of cdk5, required for activity with regulatory function, p39 activates to a greater extent compared to p35 in vitro, p39 is the activator activator in vivo
-
protein 14-3-3
-
a dimeric scaffold protein, protein is absolutely required for connection by simultaneous binding of glycogen synthase kinase-3 beta to tau within a brain microtubule-associated tau phosphorylation complex
-
protein 14-3-3
-
protein 14-3-3 facilitates tau phosphorylation by SGK1 and regulates its subcellular localization
-
soluble beta-amyloid oligomers
-
activate GSK-3beta mediated tau phosphorylation and increase toxicity, reduced content of soluble, not insoluble, amyloid oligomers reduces the tau phosphorylation activity, specific antibodies can inhibit the activation, overview
-
syndapin 1
-
highly stimulates the GSK-3beta-mediated phosphorylation of protein tau (about 4.3fold stimulation in the presence of 0.003 mM)
-
tubulin
-
stimulates phosphorylation of tau under the condition of microtubile formation
-
tubulin
-
-
-
Wortmannin
-
-
Wortmannin
-
100 ng/ml
L-Dopa
-
activates GSK-3beta at high dose
additional information
-
not activated by cyclic nucleotides cAMP and cGMP, calmodulin or phospholipide
-
additional information
-
activation loop structure
-
additional information
-
starvation- and cold-water stress-induced reversible hyperphosphorylation of tau at S199, S202, T205, T231, and S235 in the brain
-
additional information
-
tau phosphorylation in vivo is stimulated by extracellular signal-regulated kinase Erk phosphorylation and apolipoprotein E4, Erk phosphorylation is stinulated by Zn2+ and inhibited by MEK-inhibitor U0126
-
additional information
-
tau becomes a more favorable substrate for GSK-3 when it is prephosphorylated by PKA in rat brain
-
additional information
-
treatment of the hippocampus cells with phosphoinositol 3-kinase inhibitor wortmannin or protein kinase C inhibitor GF-109203X leads to tau hyperphosphorylation both at Ser396/404 and at Ser199/202, with both inhibitors acting synergistically to each other, resulting in Alzheimer's disease-like tau accumulation, overview, wortmannin or GF-109203X decrease the phosphorylation of GSK-3 at Ser9, inhibition of the GSK-3 eliminates the effects of wortmannin and GF-109203X leads to tau hyperphosphorylation both at Ser396/404 and at Ser199/202, with both inhibitors acting synergistically with each other, resulting in Alzheimer's disease-like tau accumulation, overview, wortmannin or GF-109203X
-
additional information
-
mechanism transitory activation of tau phosphorylation by PKA in Alzheimer's disease, effects of durative incubation with activators, overview
-
additional information
-
cold water stress dramatically and transiently increases TPKI/GSK3beta phosphorylation at Ser9 accompanied by Akt phosphorylation
-
additional information
-
age-dependent increase in tau hyperphosphorylated at the AT-8 site and PHF-1 site, Cdk5 activity does not account for the age-dependent hyperphosphorylation of tau at the disease-related sites, it is mediated by GSK3 activity
-
additional information
-
tau phosphorylation by TPKI/GSK3beta occurs rapidly in the hippocampus and its neighboring regions under a physiological learning situation of fear conditioning paradigm
-
additional information
Q9WV60
the inhibition of PP2A increases the phosphorylation of GSK-3beta at Ser9
-
additional information
-
17beta-estradiol attenuates glycogen synthase kinase-3beta activation
-
additional information
-
dephosphorylation at the inhibitory GSK3beta-Ser9 site activates the enzyme, GSK3beta activity increases with aging
-
additional information
-
GSK-3beta is activated by inhibition of both Wnt and PI3K/Akt signaling
-
additional information
-
glycogen synthase kinase-3beta is activated by matrix metalloproteinase-2-mediated proteolysis (dephosphorylation of Ser-9) in cardiomyoblasts MMP-2, GSK-3beta may be a target of matrix metalloproteinase-2 and its cleavage by matrix metalloproteinase-2 enhances its kinase activity, matrix metalloproteinase-2-mediated augmentation of GSK-3beta kinase activity may contribute to cardiac injury resulting from enhanced oxidative stress
-
additional information
-
activation of GSK-3beta is absolutely dependent on the presence of alpha-synuclein
-
IC50 VALUE [mM]
IC50 VALUE [mM] Maximum
INHIBITOR
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
2.5e-06
-
1-(4-methoxyphenyl)-6-(5-[[3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)-1H-benzimidazole
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
8.6e-06
-
1-(4-methoxyphenyl)-6-(5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)-1H-benzimidazole
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.000125
-
1-(cyclopropylmethyl)-3-[4-(5,6-difluoro-1-benzofuran-3-yl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]-1H-indole-5-carbonitrile
-
-
0.000131
-
1-(cyclopropylmethyl)-3-[4-(5,6-difluoro-1-benzofuran-3-yl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]-1H-indole-5-carbonitrile
-
-
0.00281
-
1-ethyl-3-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)urea
-
-
-
0.023
-
1-methyl-5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-amine
-
-
9.4e-06
-
1-methyl-6-(5-[[3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)-1H-benzimidazole
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
6.5e-05
-
2-(1,3-benzodioxol-5-yl)-5-[(3-fluoro-4-methoxybenzyl)sulfanyl]-1,3,4-oxadiazole
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
4.9e-06
-
2-(1-benzofuran-5-yl)-5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazole
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
4.4e-05
-
2-(2,3-dihydro-1-benzofuran-5-yl)-5-[(3-fluoro-4-methoxybenzyl)sulfanyl]-1,3,4-oxadiazole
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
5.4e-05
-
2-(2,3-dihydro-1-benzofuran-5-yl)-5-[(3-fluorobenzyl)sulfanyl]-1,3,4-oxadiazole
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.00022
-
2-(2,3-dihydro-1-benzofuran-5-yl)-5-[(4-methoxybenzyl)sulfanyl]-1,3,4-oxadiazole
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.00034
-
2-(2,3-dihydro-1-benzofuran-5-yl)-5-[2-(3-fluorophenyl)ethyl]-1,3,4-oxadiazole
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.00068
-
2-(2,3-dihydro-1-benzofuran-5-yl)-5-[[(3-fluorophenyl)sulfanyl]methyl]-1,3,4-oxadiazole
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
6.8e-05
-
2-(2,3-dihydro-1-benzofuran-5-yl)-5-[[3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazole
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
5.7e-06
-
2-(2,3-dihydro-1-benzofuran-5-yl)-5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazole
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
2.1e-05
-
2-(3-ethylpiperazin-1-yl)-N-[6-(3-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]acetamide
-
-
-
0.00021
-
2-(benzylsulfanyl)-5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazole
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.000143
-
2-chloro-5-[(2,5-dioxo-4-phenyl-2,5-dihydro-1H-pyrrol-3-yl)amino]benzoic acid
-
-
-
7.4e-05
-
2-chloro-5-[[4-(2-chlorophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
-
-
-
2.8e-05
-
2-chloro-5-[[4-(2-nitrophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
-
-
-
7.6e-05
-
2-chloro-5-[[4-(3-chlorophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
-
-
-
8.5e-05
-
2-chloro-5-[[4-(3-methoxyphenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
-
-
-
2.6e-05
-
2-chloro-5-[[4-(3-nitrophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
-
-
-
0.000109
-
2-chloro-5-[[4-(4-chlorophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
-
-
-
1.9e-05
-
2-methyl-N-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)propanamide
-
-
-
9.4e-05
-
2-[(2-chlorobenzyl)sulfanyl]-5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazole
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
1.3e-05
-
2-[(3-chloro-4-methoxybenzyl)sulfanyl]-5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazole
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.0002
-
2-[(3-chlorobenzyl)sulfanyl]-5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazole
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.00028
-
2-[(4-chlorobenzyl)sulfanyl]-5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazole
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
8.4e-05
-
2-[3-(4-methoxyphenyl)-1-benzofuran-5-yl]-5-[[3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazole
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
2.5e-05
-
2-[3-(4-methoxyphenyl)-1-benzofuran-5-yl]-5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazole
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.00026
-
3-(1-(2-(1H-imidazol-1-yl)ethyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
0.07334
-
3-(1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-1-phenyl-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
0.00066
-
3-(1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1-methyl-1H-pyrrolo[3,2-b]pyridin-3-yl)-1H-pyrrole-2,5-dione
-
-
0.00055
-
3-(1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
0.01358
-
3-(1-(3-(dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
0.01245
-
3-(1-(3-(piperidin-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
0.00114
-
3-(1-(3-hydroxypropyl)-1H-indol-3-yl)-4-(1-methyl-1H-pyrrolo[3,2-b]pyridin-3-yl)-1H-pyrrole-2,5-dione
-
-
0.00179
-
3-(1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
0.00085
-
3-(1-(4-(1H-imidazol-1-yl)butyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
3.5e-05
-
3-(1-benzofuran-3-yl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
0.00022
-
3-(1-benzofuran-3-yl)-4-(1-methyl-7-phenoxy-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
7e-06
-
3-(1-benzofuran-3-yl)-4-(5-bromo-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
0.000235
-
3-(1-benzofuran-3-yl)-4-(5-cyclopropyl-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
2.6e-05
-
3-(1-benzofuran-3-yl)-4-(5-fluoro-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
0.00036
-
3-(1-benzofuran-3-yl)-4-(5-fluoro-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
0.00069
-
3-(1-benzofuran-3-yl)-4-(5-hydroxy-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3.45e-05
-
3-(1-benzofuran-3-yl)-4-(5-iodo-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
0.000184
-
3-(1-benzofuran-3-yl)-4-(6-chloro-5-fluoro-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
0.00044
-
3-(1-benzofuran-3-yl)-4-(6-chloro-5-methoxy-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
1.5e-05
-
3-(1-benzofuran-3-yl)-4-(6-hydroxy-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
0.000223
-
3-(1-benzofuran-3-yl)-4-(6-iodo-5-methoxy-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
5.5e-05
-
3-(1-benzofuran-3-yl)-4-(7-hydroxy-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
0.00022
-
3-(1-benzofuran-3-yl)-4-[1-(3-hydroxypropyl)-5-phenoxy-1H-indol-3-yl]-1H-pyrrole-2,5-dione
-
-
0.001304
-
3-(1-benzofuran-3-yl)-4-[1-methyl-5-(morpholin-4-yl)-1H-indol-3-yl]-1H-pyrrole-2,5-dione
-
-
0.00165
-
3-(1-benzofuran-3-yl)-4-[5-(benzyloxy)-1H-indol-3-yl]-1H-pyrrole-2,5-dione
-
-
1.6e-06
-
3-(1-benzofuran-3-yl)-4-[5-bromo-1-(3-hydroxypropyl)-1H-indol-3-yl]-1H-pyrrole-2,5-dione
-
-
0.0009
-
3-(1-benzofuran-3-yl)-4-[6-(benzyloxy)-1-methyl-1H-indol-3-yl]-1H-pyrrole-2,5-dione
-
-
5.4e-06
-
3-(1-benzofuran-3-yl)-4-[7-(hydroxymethyl)-1-methyl-1H-indol-3-yl]-1H-pyrrole-2,5-dione
-
-
1.2e-07
-
3-(1-benzofuran-3-yl)-4-[7-(methoxymethyl)-1-methyl-1H-indol-3-yl]-1H-pyrrole-2,5-dione
-
-
0.0009
-
3-(1-methyl-1H-pyrrolo[3,2-b]pyridin-3-yl)-4-(1-(2-morpholinoethyl)-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
0.00076
-
3-(1-methyl-1H-pyrrolo[3,2-b]pyridin-3-yl)-4-(1-(3-morpholinopropyl)-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
0.0306
-
3-(1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
0.000187
-
3-(2,3-dihydro-1H-indol-1-yl)-4-(2-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
-
0.000131
-
3-(2,3-dihydro-1H-indol-1-yl)-4-(2-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
-
0.000161
-
3-(2,3-dihydro-1H-indol-1-yl)-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
-
0.000694
-
3-(2,3-dihydro-1H-indol-1-yl)-4-(4-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
-
0.000337
-
3-(2-chlorophenyl)-4-(2,3-dihydro-1H-indol-1-yl)-1H-pyrrole-2,5-dione
-
-
-
0.000216
-
3-(2-chlorophenyl)-4-(phenylamino)-1H-pyrrole-2,5-dione
-
-
-
9.3e-05
-
3-(2-chlorophenyl)-4-[(3,5-dichloro-4-hydroxyphenyl)amino]-1H-pyrrole-2,5-dione
-
-
-
0.000195
-
3-(2-chlorophenyl)-4-[(3-chlorophenyl)amino]-1H-pyrrole-2,5-dione
-
-
-
0.000374
-
3-(2-chlorophenyl)-4-[(3-hydroxyphenyl)amino]-1H-pyrrole-2,5-dione
-
-
-
0.000161
-
3-(2-chlorophenyl)-4-[[4-(methylsulfanyl)phenyl]amino]-1H-pyrrole-2,5-dione
-
-
-
0.000216
-
3-(2-methoxyphenyl)-4-(phenylamino)-1H-pyrrole-2,5-dione
-
-
-
0.00011
-
3-(2-methoxyphenyl)-4-[[4-(methylsulfanyl)phenyl]amino]-1H-pyrrole-2,5-dione
-
-
-
0.00046
-
3-(3-chlorophenyl)-4-(2,3-dihydro-1H-indol-1-yl)-1H-pyrrole-2,5-dione
-
-
-
5.8e-05
-
3-(3-chlorophenyl)-4-[(3,5-dichloro-4-hydroxyphenyl)amino]-1H-pyrrole-2,5-dione
-
-
-
0.001478
-
3-(3-chlorophenyl)-4-[(3-hydroxyphenyl)amino]-1H-pyrrole-2,5-dione
-
-
-
0.000532
-
3-(3-chlorophenyl)-4-[[4-(methylsulfanyl)phenyl]amino]-1H-pyrrole-2,5-dione
-
-
-
0.000203
-
3-(3-methoxyphenyl)-4-[[4-(methylsulfanyl)phenyl]amino]-1H-pyrrole-2,5-dione
-
-
-
0.000141
-
3-(3-nitrophenyl)-4-(phenylamino)-1H-pyrrole-2,5-dione
-
-
-
0.001412
-
3-(4-chlorophenyl)-4-(2,3-dihydro-1H-indol-1-yl)-1H-pyrrole-2,5-dione
-
-
-
0.000514
-
3-(4-chlorophenyl)-4-(phenylamino)-1H-pyrrole-2,5-dione
-
-
-
9.1e-05
-
3-(4-chlorophenyl)-4-[(3,5-dichloro-4-hydroxyphenyl)amino]-1H-pyrrole-2,5-dione
-
-
-
0.000447
-
3-(4-chlorophenyl)-4-[(3-chlorophenyl)amino]-1H-pyrrole-2,5-dione
-
-
-
0.000407
-
3-(4-chlorophenyl)-4-[(3-hydroxyphenyl)amino]-1H-pyrrole-2,5-dione
-
-
-
0.000317
-
3-(4-chlorophenyl)-4-[(4-hydroxyphenyl)amino]-1H-pyrrole-2,5-dione
-
-
-
0.002285
-
3-(4-chlorophenyl)-4-[methyl(phenyl)amino]-1H-pyrrole-2,5-dione
-
-
-
0.000529
-
3-(4-chlorophenyl)-4-[[4-(methylsulfanyl)phenyl]amino]-1H-pyrrole-2,5-dione
-
-
-
0.00039
-
3-(4-methoxyphenyl)-4-(phenylamino)-1H-pyrrole-2,5-dione
-
-
-
0.000243
-
3-(4-methoxyphenyl)-4-[[4-(methylsulfanyl)phenyl]amino]-1H-pyrrole-2,5-dione
-
-
-
0.000314
-
3-(5,6-difluoro-1-benzofuran-3-yl)-4-(1-methyl-1H-benzo[g]indol-3-yl)-1H-pyrrole-2,5-dione
-
-
8.87e-05
-
3-(5,7-dibromo-1-methyl-1H-indol-3-yl)-4-(7-methoxy-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
-
0.00014
-
3-(5-bromo-1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
0.00055
-
3-(5-bromo-1-benzofuran-3-yl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
7.5e-06
-
3-(5-bromo-1-methyl-1H-indol-3-yl)-4-(7-methoxy-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
-
0.000335
-
3-(5-bromo-1-methyl-1H-indol-3-yl)-4-[6-(4-methoxyphenoxy)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
-
-
5.1e-07
-
3-(5-bromo-1-methyl-1H-indol-3-yl)-4-[6-(hydroxymethyl)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
-
-
4.83e-05
-
3-(5-bromo-1-methyl-1H-indol-3-yl)-4-[6-(prop-2-en-1-yloxy)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
-
-
2.53e-05
-
3-(5-bromo-1-methyl-1H-indol-3-yl)-4-[6-(prop-2-yn-1-yloxy)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
-
-
4.2e-05
-
3-(5-chloro-1-methyl-1H-indol-3-yl)-4-(5-fluoro-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
-
0.00067
-
3-(5-fluoro-1-benzofuran-3-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
0.00018
-
3-(5-fluoro-1-benzofuran-3-yl)-4-(5-iodo-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
1.4e-05
-
3-(5-fluoro-1-benzofuran-3-yl)-4-(6-hydroxy-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3.5e-06
-
3-(5-fluoro-1-methyl-1H-indol-3-yl)-4-(6-hydroxy-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
-
3.5e-07
-
3-(5-fluoro-1-methyl-1H-indol-3-yl)-4-[6-(hydroxymethyl)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
-
-
2.38e-05
-
3-(5-fluoro-1-methyl-1H-indol-3-yl)-4-[6-(methoxymethyl)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
-
-
0.000247
-
3-(5-fluoro-6-iodo-1-methyl-1H-indol-3-yl)-4-(7-methoxy-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
-
0.00048
-
3-(5-methoxy-1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
0.02246
-
3-(5-methoxy-1-(3-(dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
0.000708
-
3-(5H-[1,3]dioxolo[4,5-f]indol-7-yl)-4-(5-fluoro-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
-
0.00095
-
3-(6-bromo-1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
0.00226
-
3-(6-bromo-1-(3-(dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
0.000866
-
3-(6-chloro-5-fluoro-1-methyl-1H-indol-3-yl)-4-(6-methoxy-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
-
0.000114
-
3-(6-chloro-5-fluoro-1-methyl-1H-indol-3-yl)-4-(7-methoxy-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
-
0.004092
-
3-(6-chloro-5-fluoro-1-methyl-1H-indol-3-yl)-4-[6-(cyclobutylmethoxy)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
-
-
0.00104
-
3-(6-chloro-5-fluoro-1-methyl-1H-indol-3-yl)-4-[6-(cyclopropylmethoxy)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
-
-
9.5e-07
-
3-(6-chloro-5-fluoro-1-methyl-1H-indol-3-yl)-4-[6-(hydroxymethyl)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
-
-
0.00031
-
3-(6-fluoro-1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
0.01244
-
3-(6-fluoro-1-(3-(dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
0.00018
-
3-(7-methoxy-1-benzofuran-3-yl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
0.000831
-
3-(7-methoxy-1-benzofuran-3-yl)-4-[1-methyl-6-(trifluoromethyl)-1H-indol-3-yl]-1H-pyrrole-2,5-dione
-
-
9.1e-05
-
3-([[5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazol-2-yl]sulfanyl]methyl)benzo-nitrile
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
1.4e-05
-
3-benzyl-N-[5-bromo-6-(furan-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrrolidine-1-carboxamide
-
-
-
0.00059
-
3-phenyl-4-(phenylamino)-1H-pyrrole-2,5-dione
-
-
-
0.000291
-
3-[(2,5-dioxo-4-phenyl-2,5-dihydro-1H-pyrrol-3-yl)amino]benzoic acid
-
-
-
8.2e-05
-
3-[(3,5-dichloro-4-hydroxyphenyl)amino]-4-(2-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
-
5.2e-05
-
3-[(3,5-dichloro-4-hydroxyphenyl)amino]-4-(2-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
-
0.000142
-
3-[(3,5-dichloro-4-hydroxyphenyl)amino]-4-(3-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
-
2e-05
-
3-[(3,5-dichloro-4-hydroxyphenyl)amino]-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
-
8.3e-05
-
3-[(3,5-dichloro-4-hydroxyphenyl)amino]-4-(4-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
-
7.1e-05
-
3-[(3,5-dichloro-4-hydroxyphenyl)amino]-4-(4-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
-
0.000149
-
3-[(3,5-dichloro-4-hydroxyphenyl)amino]-4-phenyl-1H-pyrrole-2,5-dione
-
-
-
0.000152
-
3-[(3-chloro-4-hydroxyphenyl)amino]-4-(2-chlorophenyl)-1H-pyrrole-2,5-dione
-
-
-
0.000139
-
3-[(3-chloro-4-hydroxyphenyl)amino]-4-(2-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
-
0.000104
-
3-[(3-chloro-4-hydroxyphenyl)amino]-4-(2-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
-
9.4e-05
-
3-[(3-chloro-4-hydroxyphenyl)amino]-4-(3-chlorophenyl)-1H-pyrrole-2,5-dione
-
-
-
5.9e-05
-
3-[(3-chloro-4-hydroxyphenyl)amino]-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
-
0.000173
-
3-[(3-chloro-4-hydroxyphenyl)amino]-4-(4-chlorophenyl)-1H-pyrrole-2,5-dione
-
-
-
0.000114
-
3-[(3-chlorophenyl)amino]-4-(2-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
-
0.000104
-
3-[(3-chlorophenyl)amino]-4-(2-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
-
0.000257
-
3-[(3-chlorophenyl)amino]-4-(3-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
-
7e-05
-
3-[(3-chlorophenyl)amino]-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
-
0.000156
-
3-[(3-chlorophenyl)amino]-4-(4-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
-
0.000301
-
3-[(3-chlorophenyl)amino]-4-phenyl-1H-pyrrole-2,5-dione
-
-
-
0.000259
-
3-[(3-hydroxyphenyl)amino]-4-(2-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
-
0.000251
-
3-[(3-hydroxyphenyl)amino]-4-(2-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
-
0.000472
-
3-[(3-hydroxyphenyl)amino]-4-(3-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
-
0.000236
-
3-[(3-hydroxyphenyl)amino]-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
-
0.000481
-
3-[(3-hydroxyphenyl)amino]-4-(4-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
-
0.000704
-
3-[(3-hydroxyphenyl)amino]-4-phenyl-1H-pyrrole-2,5-dione
-
-
-
0.000123
-
3-[(4-hydroxyphenyl)amino]-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
-
2.3e-06
-
3-[([5-[1-(4-methoxyphenyl)-1H-benzimidazol-6-yl]-1,3,4-oxadiazol-2-yl]sulfanyl)methyl]benzonitrile
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
3.5e-06
-
3-[([5-[3-(4-methoxyphenyl)-1-benzofuran-5-yl]-1,3,4-oxadiazol-2-yl]sulfanyl)methyl]benzonitrile
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
1.32e-05
-
3-[4-(6-ethyl-1-benzofuran-3-yl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]-1-methyl-1H-indole-5-carbonitrile
-
-
2.26e-05
-
3-[5-(cyclopropylethynyl)-1-methyl-1H-indol-3-yl]-4-(5-fluoro-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
-
0.007
-
3-[6-(4-chlorophenyl)-5-fluoro-1-methyl-1H-indol-3-yl]-4-(7-methoxy-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
-
0.00016
-
3-[6-(benzyloxy)-1-methyl-1H-indol-3-yl]-4-(5-fluoro-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
-
5.1e-06
-
3-[6-(hydroxymethyl)-1-benzofuran-3-yl]-4-[7-(hydroxymethyl)-1-methyl-1H-indol-3-yl]-1H-pyrrole-2,5-dione
-
-
0.001398
-
3-[methyl(phenyl)amino]-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
-
0.002613
-
3-[methyl(phenyl)amino]-4-phenyl-1H-pyrrole-2,5-dione
-
-
-
0.000136
-
3-[[4-(2-chlorophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
-
-
-
0.000134
-
3-[[4-(3-chlorophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
-
-
-
0.000195
-
3-[[4-(3-methoxyphenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
-
-
-
7.9e-05
-
3-[[4-(3-nitrophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
-
-
-
0.000186
-
3-[[4-(4-chlorophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
-
-
-
0.000214
-
3-[[4-(4-methoxyphenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
-
-
-
0.000152
-
3-[[4-(methylsulfanyl)phenyl]amino]-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
-
0.000392
-
3-[[4-(methylsulfanyl)phenyl]amino]-4-(4-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
-
0.000404
-
3-[[4-(methylsulfanyl)phenyl]amino]-4-phenyl-1H-pyrrole-2,5-dione
-
-
-
0.00025
-
4,5-diphenyl-1H-pyrazolo[3,4-c]pyridazin-3-amine
-
-
0.023
-
4-phenyl-1H-pyrazolo[3,4-b]pyridin-3-amine
-
-
0.00033
-
5-(2,3-dihydro-1-benzofuran-5-yl)-N-(3-fluorobenzyl)-1,3,4-oxadiazol-2-amine
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
1.6e-05
-
5-(5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)-1H-indazole
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
2.8e-05
-
5-([ [5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazol-2-yl]sulfanyl]methyl)-2-methoxybenzonitrile
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.00043
-
5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-amine
-
-
0.00053
-
5-phenyl-1H-pyrazolo[3,4-c]pyridazin-3-amine
-
-
0.00126
-
5-phenyl-1H-pyrazolo[3,4-c]pyridin-3-amine
-
-
0.023
-
5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-amine
-
-
0.023
-
5-phenyl[1,2]oxazolo[5,4-b]pyridin-3-amine
-
-
3.1e-06
-
6-(5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)-1,3-benzothiazole
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
6.5e-06
-
6-(5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)imidazo[1,2-a]pyridine
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
1.8e-05
-
6-(5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)quinoline
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.0125
-
carteriosulfonic acid A
-
at 37C
0.0068
-
carteriosulfonic acid B
-
at 37C
0.0068
-
carteriosulfonic acid C
-
at 37C
0.000548
-
KRM-189
-
-
0.000467
-
KRM-191
-
-
0.001012
-
KRM-192
-
-
0.001863
-
KRM-195
-
-
0.000539
-
KRM-296
-
-
0.007149
-
KRM-7777
-
-
7.1e-05
-
LiCl
-
-
0.00063
-
methyl 3-([[5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazol-2-yl]sulfanyl]methyl)benzoate
-
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.002343
-
N-(1H-pyrazolo[3,4-b]pyridin-3-yl)butanamide
-
-
-
0.000691
-
N-(4,5-diphenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl)butanamide
-
-
-
0.000415
-
N-(5,6-diphenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)cyclopropanecarboxamide
-
-
-
0.000383
-
N-(5-bromo-6-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)-4-methylpiperidine-1-carboxamide
-
-
-
7.5e-05
-
N-(5-bromo-6-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)cyclopropanecarboxamide
-
-
-
0.000234
-
N-(5-chloro-6-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)cyclopropanecarboxamide
-
-
-
8.7e-05
-
N-(5-cyano-6-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)cyclopropanecarboxamide
-
-
-
9.9e-05
-
N-(5-phenyl-1H-indazol-3-yl)butanamide
-
-
-
0.000291
-
N-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)acetamide
-
-
-
5.6e-05
-
N-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)butanamide
-
-
-
5e-06
-
N-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)cyclopentanecarboxamide
-
-
-
0.003572
-
N-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)methanesulfonamide
-
-
4.3e-05
-
N-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)propanamide
-
-
-
7e-06
-
N-(5-phenyl-1H-pyrazolo[3,4-c]pyridin-3-yl)butanamide
-
-
-
0.002697
-
N-(5-phenyl-1H-pyrazolo[4,3-d]pyrimidin-3-yl)butanamide
-
-
-
0.000498
-
N-(6-phenyl-1H-indazol-3-yl)cyclopropanecarboxamide
-
-
-
0.000425
-
N-(6-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)cyclopropanecarboxamide
-
-
-
7e-06
-
N-[4-[3-(4-ethylpiperazin-1-yl)propyl]-5-phenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl]butanamide
-
-
-
2.2e-05
-
N-[4-[3-(dimethylamino)propyl]-5-phenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl]butanamide
-
-
-
5e-06
-
N-[4-[3-(morpholin-4-yl)propyl]-5-phenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl]butanamide, N-[4-[ethyl(piperidin-1-ylmethyl)amino]-5-phenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl]butanamide
-
-
-
9e-06
-
N-[4-[methyl(piperidin-1-yl)amino]-5-phenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl]butanamide
-
-
-
7e-06
-
N-[5-(2,3-difluorophenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
-
-
-
2.7e-05
-
N-[5-(2-chlorophenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
-
-
-
1.8e-05
-
N-[5-(2-fluorophenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
-
-
-
2e-05
-
N-[5-(3-fluorophenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
-
-
-
0.000356
-
N-[5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
-
-
-
5e-06
-
N-[5-(6,6-difluorocyclohexa-1,3-dien-1-yl)-4-[3-(dimethylamino)propyl]-1H-pyrazolo[3,4-c]pyridazin-3-yl]butanamide
-
-
-
0.000851
-
N-[5-(biphenyl-4-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
-
-
-
0.000241
-
N-[5-(naphthalen-1-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
-
-
-
0.000169
-
N-[5-(naphthalen-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
-
-
-
1.1e-05
-
N-[5-(pyridin-3-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
-
-
-
0.000443
-
N-[5-(pyridin-4-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
-
-
-
4e-06
-
N-[5-bromo-6-(4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-4-(4-ethylpiperazin-1-yl)butanamide
-
-
-
1e-06
-
N-[5-bromo-6-(4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-4-methylpiperidine-1-carboxamide
-
-
-
8e-07
-
N-[5-bromo-6-(4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
-
7e-06
-
N-[5-bromo-6-(furan-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
-
1.6e-05
-
N-[5-bromo-6-(tetrahydrothiophen-3-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
-
1.8e-05
-
N-[5-bromo-6-(thiophen-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-2-(4-methylpiperidin-1-yl)acetamide
-
-
-
7e-06
-
N-[5-bromo-6-(thiophen-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
-
1e-06
-
N-[5-chloro-6-(4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
-
1.1e-05
-
N-[5-phenyl-4-[3-(pyrrolidin-1-yl)propyl]-1H-pyrazolo[3,4-c]pyridazin-3-yl]butanamide
-
-
-
4.2e-05
-
N-[6-(1H-indol-5-yl)-1H-indazol-3-yl]cyclopropanecarboxamide
-
-
-
0.001
-
N-[6-(2,5-difluorophenyl)-1H-indazol-3-yl]cyclopropanecarboxamide
-
-
-
3.6e-05
-
N-[6-(2-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
-
0.001593
-
N-[6-(2-methoxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
-
0.00032
-
N-[6-(2H-pyrrol-2-yl)-1H-indazol-3-yl]cyclopropanecarboxamide
-
-
-
8e-06
-
N-[6-(3,4-dihydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
-
5e-06
-
N-[6-(3-bromo-4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
-
7e-06
-
N-[6-(3-chloro-4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
-
0.000828
-
N-[6-(3-fluorophenyl)-1H-indazol-3-yl]cyclopropanecarboxamide
-
-
-
1.2e-05
-
N-[6-(3-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
-
0.000125
-
N-[6-(3-methoxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
-
0.000481
-
N-[6-(3-sulfamoylphenyl)-1H-indazol-3-yl]cyclopropanecarboxamide
-
-
-
1.5e-05
-
N-[6-(4-hydroxyphenyl)-1H-indazol-3-yl]cyclopropanecarboxamide
-
-
-
1.2e-05
-
N-[6-(4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-4-methylpiperidine-1-carboxamide
-
-
-
8e-06
-
N-[6-(4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
-
6e-06
-
N-[6-(4-hydroxyphenyl)-5-methyl-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
-
2.4e-05
-
N-[6-(4-hydroxyphenyl)-5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
-
0.023
-
N-[6-(4-methoxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
-
0.000141
-
N-[6-(furan-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
-
3.5e-05
-
N-[6-(furan-3-yl)-1H-indazol-3-yl]cyclopropanecarboxamide
-
-
-
9.9e-05
-
N-[6-(tetrahydrothiophen-3-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
-
0.000215
-
N-[6-(thiophen-2-yl)-1H-indazol-3-yl]cyclopropanecarboxamide
-
-
-
3.9e-05
-
N-[6-(thiophen-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
-
0.000329
-
N-[6-(thiophen-3-yl)-1H-indazol-3-yl]cyclopropanecarboxamide
-
-
-
3.4e-05
-
SB216763
-
-
-
0.0002
-
staurosporine
-
-
SPECIFIC ACTIVITY [µmol/min/mg]
SPECIFIC ACTIVITY MAXIMUM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
0.001
-
-
isoenzyme TPKI, optimum conditions
0.01325
-
-
activity towards tubulin
0.01665
-
-
activity towards tau
0.056
-
-
isoenzyme TPKI
0.26
-
-
in the presence of Mg2+
0.57
-
-
in the presence of Mn2+
additional information
-
-
-
pH OPTIMUM
pH MAXIMUM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
7.2
-
-
assay at
7.2
-
-
assay at
7.2
-
-
assay at
7.4
-
-
assay at
7.4
-
-
assay at
7.4
-
-
assay at
7.4
-
-
assay at
7.5
-
-
assay at
7.5
-
-
assay at
7.5
-
-
assay at
TEMPERATURE OPTIMUM
TEMPERATURE OPTIMUM MAXIMUM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
30
-
-
assay at
30
-
-
assay at
30
-
-
assay at
30
-
-
assay at
30
-
-
assay at
30
-
-
assay at
30
-
-
assay at
30
-
-
assay at
30
-
-
assay at
37
-
-
assay at
pI VALUE
pI VALUE MAXIMUM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
9.4
-
-
isoenzyme TPKI, ?
SOURCE TISSUE
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
SOURCE
Leishmania donovani LG13
-
-
-
Manually annotated by BRENDA team
-
entire amygdala or ventroposterior quadrant of cerebral hemisphere
Manually annotated by BRENDA team
Mus musculus C57BL/6Njcl
-
entire amygdala or ventroposterior quadrant of cerebral hemisphere
-
Manually annotated by BRENDA team
-
hyperphosphorylation in hippocampal and cerebral regions, weak in the cerebellum
Manually annotated by BRENDA team
-
developing postnatal and embryonic
Manually annotated by BRENDA team
-
distribution in brain regions, overview
Manually annotated by BRENDA team
-
from Alzheimer patients, isozyme CKIdelta
Manually annotated by BRENDA team
-
interaction of GSK3beta and tau
Manually annotated by BRENDA team
-
adult brain cortex and fetal brain tissue
Manually annotated by BRENDA team
-
cortical layers
Manually annotated by BRENDA team
Mus musculus C57BL/6Njcl
-
-
-
Manually annotated by BRENDA team
Rattus norvegicus Wistar
-
;
-
Manually annotated by BRENDA team
-
primary midbrain mesencephalonic cells
Manually annotated by BRENDA team
-
granular layer
Manually annotated by BRENDA team
-
cold-water stress-induced tau phosphorylation pattern
Manually annotated by BRENDA team
-
immortilized embryonic brain cortex cell line
Manually annotated by BRENDA team
-
purified recombinant GSK-3beta
Manually annotated by BRENDA team
Rattus norvegicus Sprague-Dawley, Rattus norvegicus Wistar
-
-
-
Manually annotated by BRENDA team
-
U251, T98, U87, U373, U118, A172
Manually annotated by BRENDA team
-
tau phosphorylation pattern
Manually annotated by BRENDA team
-
hippocampal neuron
Manually annotated by BRENDA team
Mus musculus C57BL/6Njcl
-
-
-
Manually annotated by BRENDA team
-
immortilized embryonic brain cortex cell line overexpressing the human tau protein
Manually annotated by BRENDA team
-
bone marrow-derived mesenchymal stem cell
Manually annotated by BRENDA team
-
cell line stably expressing human apolipoprotein apoE4
Manually annotated by BRENDA team
-
neurofibrillary tangles
Manually annotated by BRENDA team
-
CA1 pyramidal neurons and cerebellum granular neurons
Manually annotated by BRENDA team
-
present in an active form in postmitotic neurons
Manually annotated by BRENDA team
Rattus norvegicus Sprague-Dawley
-
-
-
Manually annotated by BRENDA team
Leishmania donovani LG13
-
-
-
Manually annotated by BRENDA team
-
neuroblastoma cell line
Manually annotated by BRENDA team
-
weak expression
Manually annotated by BRENDA team
-
weak expression
Manually annotated by BRENDA team
additional information
-
expression pattern during brain development
Manually annotated by BRENDA team
additional information
-
hippothalamus
Manually annotated by BRENDA team
additional information
-
N18 cell, hyperphosphorylation reduces taus ability to promote tubulin assembly and to form bundles
Manually annotated by BRENDA team
additional information
-
perinuclear and cytoplasmic regions of the large cortical pyramidal cells in the temporal cortex
Manually annotated by BRENDA team
LOCALIZATION
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
GeneOntology No.
LITERATURE
SOURCE
-
inactive GSK-3beta
Manually annotated by BRENDA team
-
GSK-3beta phosphorylated at Tyr216 is mainly localized in cytoplasm
Manually annotated by BRENDA team
-
isoform GSK-3beta
Manually annotated by BRENDA team
-
1-methyl-4-phenylpyridinium iodide treatment induces a significant decrease of the specific phospho-Tyr216-GSK-3beta labeling in mitochondria concomitantly with an increase into the cytosol
Manually annotated by BRENDA team
-
GSK-3 after cell treatment with lithium
Manually annotated by BRENDA team
-
isoform GSK-3alpha
Manually annotated by BRENDA team
-
activated GSK-3beta
Manually annotated by BRENDA team
-
when amyloid precursor protein is overexpressed, the GSK-3beta phosphorylated at Tyr216 level significantly increases in the nuclear fraction
Manually annotated by BRENDA team
-
GSK-3beta partially localizes within mitochondria
Manually annotated by BRENDA team
additional information
-
CDK5-dependent clustering of endoplasmic reticulum ER and mitochondria and translocation to the centrosome during ceramide-mediated neuronal death
-
Manually annotated by BRENDA team
additional information
-
perinuclear region
-
Manually annotated by BRENDA team
MOLECULAR WEIGHT
MOLECULAR WEIGHT MAXIMUM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
30000
-
-
isoenzyme TPKII, SDS-PAGE
30000
-
-
gel filtration
30000
-
-
recombinant TPKII, SDS-PAGE
32000
-
-
gel filtration, SDS-PAGE
35000
-
-
gel filtration
36000
-
Q3UVR3
calculated from cDNA sequence
38620
-
-
calculated
45000
-
-
isoenzyme TPKI, SDS-PAGE
45000
-
-
SDS-PAGE
45000
-
-
isoenzyme TPKI, SDS-PAGE
47000
-
-
SDS-PAGE
47000
-
-
SDS-PAGE
47000
-
-
SDS-PAGE
47000
-
-
SDS-PAGE
47000
-
-
SDS-PAGE
72000
-
-
SDS-PAGE
100000
-
-
immunoprecipitation, lysosomal degradation product of full-length TTBK1
142700
-
-
predicted
230000
-
-
immunoprecipitation, full-length TTBK1 migrates to 230 kDa because of the negative charge of the polyglutamate sequence and the protein modification
additional information
-
-
absence of a 230-kDa protein in the mouse cortex, suggests a very small quantity of full-length TTBK1
SUBUNITS
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
heterodimer
-
1 * 30000 + 1 * 23000, catalytic and regulatory subunit, SDS-PAGE
monomer
-
1 * 39000, SDS-PAGE
additional information
-
14-3-3 connects glycogen synthase kinase-3 beta to tau within a brain microtubule-associated tau phosphorylation complex
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
phosphoprotein
-
in diapause eggs, an abrupt decrease in phosphorylation of GSK-3beta is found with the onset of diapause, and phosphorylation level of GSK-3beta reaches a minimum level within 1 week after oviposition. Extracellular signal-regulated kinase phosphorylation is not involved in upstream signaling for GSK-3beta phosphorylation. Phosphorylated GSK-3beta is observed in yolk cells but not in embryos of eggs which are maintained at 5C for 60 days
phosphoprotein
-
phosphorylated in vitro at Ser9 by p70 S6 kinase and p90rsk-1, resulting in its inhibition
phosphoprotein
-
phosphorylation of GSK3beta at S9 inhibits the enzyme
phosphoprotein
-
0.001 mg/ml chaperonin 10 stimulates the phosphorylation of GSK-3beta
phosphoprotein
-
the activity of GSK-3beta is decreased by the phosphorylation of Ser9 by Akt
phosphoprotein
-
GSK-3beta is activated via phosphorylation at Ser9
phosphoprotein
-
Akt phosphorylates GSK-3beta at serine residue 9 thereby inhibiting the activity of GSK-3beta, furthermore GSK-3beta is controlled by tyrosine phosphorylation, which increases its activity
phosphoprotein
-
-
phosphoprotein
-
phosphorylation on serine-21 of GSK3alpha and serine-9 of GSK3beta greatly inhibits the activity of GSK3
phosphoprotein
-
GSK-3beta is activated by phosphorylation of the tyrosine 216 residue located in the kinase domain and inactivated by phosphorylation of the amino-terminal serine 9 residue
phosphoprotein
-
phosphorylation of GSK3beta by a different protein kinase, e.g. phosphoinositol 3-kinase or protein kinase C, at Ser9 inhibits the enzyme
phosphoprotein
-
phosphorylation of GSK-3beta at Ser9 reduces activity of this kinase
phosphoprotein
-
the serine-9 phosphorylated GSK-3beta form is inactive
phosphoprotein
-
activity of GSK3beta is regulated through phosphorylation on serine-9 (inhibitory) and tyrosine-216 residues (stimulatory)
phosphoprotein
-
-
phosphoprotein
-
phosphorylation at Tyr216
phosphoprotein
-
regulation of Rim11 by Tyr phosphorylation during sporulation. Rim11 is phosphorylated on Tyr199, and the Tyr phosphorylation is essential for its in vivo function
phosphoprotein
-
autophosphorylation, phosphorylation on a conserved tyrosine residue is required for efficient activity. Phosphorylated at a Ser225 is likely to inhibit its function
Crystallization/COMMENTARY
ORGANISM
UNIPROT ACCESSION NO.
LITERATURE
by hanging-drop vapour-diffusion method, crystals belong to space group P212121, with unit-cell parameters a = 55.6, b = 113.7, c = 117.3 A, alpha = beta = gamma = 90.0, to 2.9 A resolution
-
hanging drop vapour-diffusion method, prismatic crystals, orthorhombic space group P2(1)2(1)2(1), unit cell parameters a = 82.9, b = 86.1, c = 178.1 A
-
purified recombinant Leu-Glu-His6-tagged GSK3beta in complex with ATP or ATP analogue AMP-PNP, 10 mg/ml protein, 2 mM ATP or AMP-PNP, 12-14% w/v PEG 6000, 100 mM NaCl, 5 mM MgCl2, 10% v/v glycerol, in 100 mM HEPES-NaOH, pH 7.5, hanging drop vapor diffusion method, 4C, several day, soaking in 0.1 mM ethylmercuric thiosalicylate at pH 7.5 for 1 h, cryoprotection by 30% w/v D-sorbitol, X-ray diffraction structure determination and analysis at 1.7-2.6 A resolution
-
TEMPERATURE STABILITY
TEMPERATURE STABILITY MAXIMUM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
95
-
-
10 min, inactivation
Purification/COMMENTARY
ORGANISM
UNIPROT ACCESSION NO.
LITERATURE
2 isoenzymes, TPKI and TPKII
-
3 isoenzymes, tau protein kinase I and II and tau-tubulin kinase
-
centrifugation, sonication, gel filtration, metal affinity chromatography, to homogeneity
-
GSTrap affinity chromatography
-
Ni-NTA resin and by gel filtration
-
recombinant isoenzyme TPHII
-
recombinant Leu-Glu-His6-tagged GSK3beta from Escherichia coli
-
Cloned/COMMENTARY
ORGANISM
UNIPROT ACCESSION NO.
LITERATURE
expression in Escherichia coli; expression in Escherichia coli
-
isolation of cDNA
-
co-expression of glycogen synthase kinase-3 beta, tau, and 14-3-3 in COS-7 cells and in HEK-293 cells
-
Flag-tagged wild-type or various mutant tau and HA-tagged GSK3beta cotransfected in HEK-293 cells
-
isolation of cDNA
-, O04160
coexpression of human tau with a constitutively active form or a dominant-negative form of Sgg
-
after cloning and cDNA analysis TPKI is found to be identical with glycogen synthase kinase 3beta, the catalytic subunit of TPKII is identical with cdc2-related kinase, PSSALRE/Cdk5
-
cDNA cloned and expressed in Escherichia coli BL21(DE3)
-
expressed in CHO cells
-
expressed in Escherichia coli BL21-CodonPlus (DE3) cells
-
expressed in Neuro2a cells
-
expressed in Saccharomyces cerevisiae
-
expression of GSK3beta in Escherichia coli in fusion with a Leu-Glu-His6-tag at the C-terminus
-
expression of GST-fusion SGK1 in COS-1 cells in the cytoplasm, coexpression with protein 14-3-3 or addition of serum leads to relocation of the enzyme in the nucleus
-
HA- and myc-tagged full-length TTBK1 expressed in COS-7 cells, HA-TTBK1 expressed in HEK293 cells and in mock-transfected cells, recombinant full length TTBK1 expressed in Escherichia coli or baculovirus-infected Sf-9 insect cells
-
recombinant TPKII cdk5/p20
-
tau protein kinase II, full length human cdk5 gene inserted into baculovirus genome
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TPKI/GSK-3beta-interacting proteins from a human brain cDNA library in a yeast two-hybrid system
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transient co-expression of human tau long isoform, HA-tagged GSK3beta, and GST-tagged GFP-fusion FRAT-2 protein in HEK-293 cells
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transient expression of HA-tagged wild-type and mutant enzymes in CHO cells
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TTBK2 kinase domain (residues 1-331) of TTBK2 subcloned into pBiEx-3 vector, expressed in insect cells with a baculovirus overexpression system
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using a baculovirus expression system
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; mouse TTK cDNA isolated using amino acid sequences of purified bovine brain TTK
Q3UVR3
alternative splicing isoform of tau protein kinase I/glycogen synthase kinase 3beta, by RT-PCR also found in rat and human brains, transient expression in COS-7 cells
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His-tagged GSK3beta expressed in Escherichia coli BL21, into pEGFP vector and N18 cells transiently transfected
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p25-induced Cdk5 over-activation of Cdk5 in young and old transgenic mice
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; expression of alpha and beta protein in COS cells
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co-expression of dominant negative EGFP-tagged CDK5 and p25 in PC12 cells
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expressed in Sf9 cells
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EXPRESSION
ORGANISM
UNIPROT ACCESSION NO.
LITERATURE
the reduction of tau phosphorylation by treatment with 100 nM leptin is mimicked by the downregulation of GSK-3beta
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LiCl and BIO also reduce the expression of GSK3beta
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treatment of hippocampal cells with 3-nitropropionic acid (0.5 mM) modifies GSK-3beta levels shown by an increase in proteolysis and a decrease of Ser-9 phosphorylation
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5-azacytidine treatment (0.005 mM for 24 h) causes significant up-regulation of GSK-3beta whereas it stimulates GSK-3alpha expression only modestly
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GSK-3beta levels are elevated by about 80% in APP transgenic neuronal cultures
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after lactacystin treatment, the total level of GSK-3beta does not change while the Ser-9-phosphorylated GSK-3beta (inactive form) decreases, especially at 72 h
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administration of insulin or TDZD-8 to diabetic rats does not modify the total GSK-3beta mRNA levels
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ENGINEERING
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
A81T
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kinase-null, dominant negative form of Shaggy, leads to the accumulation of hypophosphorylated high-molecular-weight human tau proteins in old transgenic flies. In young transgenic flies expression results in disappearance of monomeric hyperphosphorylated forms of human tau, concomitantly with the accumulation of monomeric hypophosphorylated forms of human tau
S9A
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constitutively active form of Shaggy, drastic upward mobility shift of all monomeric human tau proteins
R96A
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site-directed mutagenesis of GSK3beta, the mutant shows reduced phosphorylation activity at primed epitopes and increased activity at unprimed epitopes of tau protein substrate compared to the wild-type GSK3beta
Y216F
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inactive
K85R
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dead-kinase mutant of GSK-3beta
additional information
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naturally occurring V717I mutation of the amyloid precursor protein APP in a CT100 fragment of organisms with Alzheimer's disease leads to augmented age-dependent tau phosphorylation, followed by increased activation status of mitogen-activated protein kinase family members, e.g. ERK1/2, p38, and c-Jun NH2-terminal kinase, compared to the wild-type organism, naturally occurring V337M mutation of tau protein of patients suffering from Alzheimer's disease leads to age-dependent memory deficits
additional information
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down-regulation of GSK3 activity results in alteration of intracellular glucose metabolism resulting in dissociation of hexokinase II from the outer mitochondrial membrane with subsequent mitochondrial destabilization
S9A
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site-directed mutagenesis, mutant cannot be inhibited by phosphorylation at position 9 and is thus constitutively active
additional information
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a cdk-deficient mouse mutant lacks tau phosphorylation activity
APPLICATION
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
medicine
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brain pathology in investigation of Alzheimers's disease, human tau phosphorylated by the kinase carries an epitope of the paired helical filaments that accumulate in the brain
medicine
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brain pathology in investigation of Alzheimers's disease, human tau phosphorylated by the kinase carries an epitope of the paired helical filaments that accumulate in the brain
medicine
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TPKI/GSK-3beta plays a key role in the pathogenesis of Alzheimer disease, tau protein kinases I and II are candidate enzymes responsible for hyperphosphorylation of tau to induce formation of paired helical filaments
medicine
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TTBK1 is located on human chromosome 6p21.1. It is a neuron-specific dual kinase involved in tau phosphorylation at Alzheimers disease-related sites and is also associated with tau aggregation
medicine
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GSK3 is an important therapeutic target for gliomas
medicine
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a significant inverse correlation is observed between level of phospho-GSK-3beta at the time of reperfusion and the extent of myocardium infarction in heart, phospho-GSK-3beta is a determinant of myocardial tolerance against reperfusion-induced necrosis. Thus, GSK-3beta is a target of therapy for cardioprotection upon reperfusion. Inactivation of GSK-3beta by phosphorylation at Ser9 elevates the threshold for mitochondrial permeability transition pore opening, which reduces myocyte necrosis.
medicine
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GSK-3beta is a therapeutic target in cancer treatment
pharmacology
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anti-bodies highly specific for toxic amyloid oligomer subspecies may reduce toxicity via reduction of GSK-3beta amount in Alzheimer's disease therapeutic strategy
medicine
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disruption of regulation of GSK3 activity underlies tau hyperphosphorylation in neurodegenerative tauopathies. GSK3 may be a prime target for therapeutic intervention in tauopathies including Alzheimer disease
medicine
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involvement of tau and TPKI/GSK3beta phosphorylation in an early phase of memory formation in the hippocampus and amygdala, possibility that a dysregulation of tau phosphorylation may underlie memory impairment in incipient Alzheimer's disease
medicine
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controlling GSK-3beta signaling in bone cells is a strategy for preventing glucocorticoid-induced osteopenia
medicine
Mus musculus C57BL/6Njcl
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involvement of tau and TPKI/GSK3beta phosphorylation in an early phase of memory formation in the hippocampus and amygdala, possibility that a dysregulation of tau phosphorylation may underlie memory impairment in incipient Alzheimer's disease
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medicine
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brain pathology in investigation of Alzheimers's disease, human tau phosphorylated by the kinase carries an epitope of the paired helical filaments that accumulate in the brain
medicine
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PKA and GSK-3 are targets for the therpeutical treatement of Alzheimer's disease and other tauopathies
medicine
Rattus norvegicus Sprague-Dawley
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-
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medicine
Rattus norvegicus Wistar
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; brain pathology in investigation of Alzheimers's disease, human tau phosphorylated by the kinase carries an epitope of the paired helical filaments that accumulate in the brain
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medicine
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additional information
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model of tauopathy in which, depending on toxic challenges (e.g., oxidative stress, exposure to amyloid peptide, etc.), abnormal phosphorylation of tau by kinases distinct from GSK-3beta leads to progressive accumulation of hyperphosphorylated tau oligomers that are resistant to degradation. Sgg activity is required to prevent the accumulation of high-molecular-weight forms of human tau
medicine
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GSK3 is a fundamental and central component of Fragile X syndrome pathology
additional information
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phosphorylation of T231 by GSK3beta may play an important role in taus hyperphosphorylation and functional regulation