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Information on EC 2.7.1.149 - 1-phosphatidylinositol-5-phosphate 4-kinase and Organism(s) Homo sapiens
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2.7.1.149 1-phosphatidylinositol-5-phosphate 4-kinaseSpecify your search results
Word Map
- 2.7.1.149
- 4,5-bisphosphate
- phospholipase
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ptdins4p
-
pi4kiii
-
ptdins4,5p2
- wortmannin
- pip2
-
trans-golgi
-
polyphosphoinositides
-
dfg-out
- phosphatidylinositol-4,5-bisphosphate
- pip5ks
-
phenylarsine
- 3-kinases
-
positive-sense
-
oxysterol-binding
- enteroviruses
- ns5a
- picornaviruses
- medicine
The taxonomic range for the selected organisms is: Homo sapiens
The enzyme appears in selected viruses and cellular organisms
The enzyme appears in selected viruses and cellular organisms
Reaction Schemes
Synonyms
phosphatidylinositol 4-kinase, type ii kinase, pip4k2a, type ii ptdins 4-kinase, pip4k, pip4k2b, pip4k2c, mss4p, type ii phosphatidylinositol 4-kinase, phosphatidylinositol 5-phosphate 4-kinase, 
more
topSYNONYM 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
1-phosphatidylinositol-4-phosphate 5-kinase
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-
-
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1-phosphatidylinositol-4-phosphate kinase
-
-
-
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Diphosphoinositide kinase
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-
-
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phosphatidylinositol 5-phosphate 4-kinase
PI5P4Kalpha
PI5P4Kbeta
PI5P4Kgamma
PIP(4)K
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-
-
-
PIP4K
PIP5KII-alpha
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-
-
-
PIP5KIII
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-
-
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PIPKII
-
-
-
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PtdIns(4)P-5-kinase B isoform
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-
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PtdIns(4)P-5-kinase C isoform
-
-
-
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PtdIns5P 4-kinase
type II PIP kinase
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-
-
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
phospho group transfer
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-
-
-
SYSTEMATIC NAME
IUBMB Comments
ATP:1-phosphatidyl-1D-myo-inositol-5-phosphate 4-phosphotransferase
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CAS REGISTRY NUMBER
COMMENTARY
104645-76-3
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247907-17-1
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SUBSTRATE
PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
ATP + 1-phosphatidyl-1D-myo-inositol 3-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 3,4-bisphosphate
-
poor substrate compared to 1-phosphatidyl-1D-myo-inositol 5-phosphate
-
?
ATP + 1-phosphatidyl-1D-myo-inositol 4-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
ATP + dipalmitoyl-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + dipalmitoyl-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
-
-
-
-
?
ATP + 1-phosphatidyl-1D-myo-inositol 4-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
-
-
-
-
?
ATP + 1-phosphatidyl-1D-myo-inositol 4-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
5' phosphorylation
-
-
r
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
-
-
-
?
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
-
-
-
-
?
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
-
-
-
?
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
-
-
-
ir
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
-
-
-
?
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
-
-
-
?
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
-
phosphorylation at the D-4 position
-
?
additional information
?
-
-
although PIP4K II generates PI-4,5-P2, a substrate for PI3K, expression of this enzyme reduces rather than increases phosphatidylinositol-3,4,5-trisphosphate (PI-3,4,5-P3) levels in cells stimulated with insulin or cells expressing activated PI3K, this reduction in PI-3,4,5-P3 levels results in decreased activation of the downstream protein kinase Akt/PKB, expression of IpgD, a bacterial phosphatase that converts PI-4,5-P2 to PI-5-P, results in Akt activation, and this effect is partially reversed by PIP4K IIbeta, PIP4K IIbeta expression does not impair insulin-dependent association of PI3K with insulin receptor substrate 1 IRS1 but abbreviates Akt activation, indicating that PIP4K II regulates PI-3,4,5-P3 degradation rather than synthesis
-
-
?
additional information
?
-
-
isozyme PIP4Kbeta interacts in vitro and in vivo with the PIP4Kalpha isoform. PIP4Kbeta has 2000fold less activity towards 1-phosphatidyl-1D-myo-inositol 5-phosphate compared with PIP4Kalpha, the majority of enzyme activity associated with PIP4Kbeta comes from its interaction with PIP4Kalpha
-
-
?
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
ATP + 1-phosphatidyl-1D-myo-inositol 4-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
ATP + 1-phosphatidyl-1D-myo-inositol 4-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
-
-
-
-
?
ATP + 1-phosphatidyl-1D-myo-inositol 4-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
5' phosphorylation
-
-
r
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
-
-
-
?
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
-
-
-
-
?
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
-
-
-
?
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
-
-
-
ir
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
-
-
-
?
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
-
-
-
?
additional information
?
-
-
although PIP4K II generates PI-4,5-P2, a substrate for PI3K, expression of this enzyme reduces rather than increases phosphatidylinositol-3,4,5-trisphosphate (PI-3,4,5-P3) levels in cells stimulated with insulin or cells expressing activated PI3K, this reduction in PI-3,4,5-P3 levels results in decreased activation of the downstream protein kinase Akt/PKB, expression of IpgD, a bacterial phosphatase that converts PI-4,5-P2 to PI-5-P, results in Akt activation, and this effect is partially reversed by PIP4K IIbeta, PIP4K IIbeta expression does not impair insulin-dependent association of PI3K with insulin receptor substrate 1 IRS1 but abbreviates Akt activation, indicating that PIP4K II regulates PI-3,4,5-P3 degradation rather than synthesis
-
-
?
additional information
?
-
-
isozyme PIP4Kbeta interacts in vitro and in vivo with the PIP4Kalpha isoform. PIP4Kbeta has 2000fold less activity towards 1-phosphatidyl-1D-myo-inositol 5-phosphate compared with PIP4Kalpha, the majority of enzyme activity associated with PIP4Kbeta comes from its interaction with PIP4Kalpha
-
-
?
COFACTOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
Mg2+
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
(2E)-2-(3,4-dihydroxybenzoyl)-3-(4-hydroxy-3-iodo-5-methoxyphenyl)prop-2-enenitrile
-
-
(2E)-4-(dimethylamino)-N-[1-[(3-[[6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl]amino]phenyl)acetyl]piperidin-4-yl]but-2-enamide
-
-
(3E)-5-amino-3-[(2Z)-1-cyano-2-(3H-indol-3-ylidene)ethylidene]-2,3-dihydro-1H-pyrazole-4-carbonitrile
-
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(E)-N-(4-(5-((2,5-dioxopyrrolidin-3-ylidene)methyl)pyridin-3-yl)phenyl)methanesulfonamide
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(Z)-1-(4-(5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)-3-methylurea
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(Z)-2-imino-5-((5-(4-(methylsulfonyl)phenyl)pyridin-3-yl)methylene)thiazolidin-4-one
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(Z)-2-imino-5-((5-(4-(trifluoromethoxy)phenyl)pyridin-3-yl)methylene)thiazolidin-4-one
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(Z)-2-imino-5-((5-(4-(trifluoromethyl)phenyl)pyridin-3-yl)methylene)thiazolidin-4-one
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(Z)-2-imino-5-((5-(4-methoxynaphthalen-1-yl)pyridin-3-yl)methylene)thiazolidin-4-one
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(Z)-4-(5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)-N-methylbenzenesulfonamide
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-
(Z)-5-((5-(4-(dimethylamino)phenyl)pyridin-3-yl)methylene)-2-iminothiazolidin-4-one
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(Z)-N-(3-(5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)acetamide
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(Z)-N-(4-(2-amino-5-((2-imino-4-oxothiazolidin-5-ylidene)-methyl)pyridin-3-yl)phenyl)methanesulfonamide
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(Z)-N-(4-(5-((2,4-dioxo-oxazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)methanesulfonamide
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(Z)-N-(4-(5-((2,4-dioxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)methanesulfonamide
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-
(Z)-N-(4-(5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)acetamide
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(Z)-N-(4-(5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)methanesulfonamide
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i.e. CVM-05-002, potent and selective inhibitor for isoform PI5P4Kalpha
(Z)-N-(4-(6-amino-5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)methanesulfonamide
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3-(trifluoromethyl)phenyl 4-amino-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)pyrimidine-5-carboxylate
-
3-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl]amino]phenyl)benzamide
-
-
4-amino-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)-N-(3-phenoxyphenyl)pyrimidine-5-carboxamide
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4-amino-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)-N-methyl-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
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4-amino-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)-N-[3-(2,2,2-trifluoroethoxy)phenyl]pyrimidine-5-carboxamide
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4-amino-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
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4-amino-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)-N-[4-methyl-3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
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4-amino-2-(benzylamino)-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
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4-amino-2-(dimethylamino)-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
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4-amino-2-(methylsulfanyl)-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
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4-amino-2-(piperidin-1-yl)-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
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4-amino-2-hydroxy-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
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4-amino-2-methoxy-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
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4-amino-2-[(2,2-dimethylpropyl)amino]-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
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4-amino-2-[(tert-butylcarbamoyl)amino]-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
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4-amino-2-[[(1-methyl-1H-pyrazol-5-yl)methyl]amino]-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
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4-amino-N-(1,3-benzothiazol-5-yl)-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)pyrimidine-5-carboxamide
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4-amino-N-(1-benzothiophen-5-yl)-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)pyrimidine-5-carboxamide
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4-amino-N-[3-(trifluoromethyl)phenyl]-2-(3,4,4-trimethyl-2-oxoimidazolidin-1-yl)pyrimidine-5-carboxamide
-
4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl]amino]phenyl)benzamide
-
-
4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl]amino]phenyl)cyclohexane-1-carboxamide
-
-
4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[6-(2-methyl-2H-benzimidazol-5-yl)pyrimidin-4-yl]amino]phenyl)benzamide
-
-
4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[6-(4-methylanilino)pyrimidin-4-yl]amino]phenyl)benzamide
-
-
4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[7-(4-methylphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]phenyl)benzamide
-
-
4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(4-methyl-3-[[6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl]amino]phenyl)benzamide
-
-
4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(5-[[6-(1H-indol-3-yl)pyrimidin-4-yl]amino]-2-methylphenyl)benzamide
-
-
4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-[(3-[[6-(1H-indol-3-yl)pyrimidin-4-yl]amino]phenyl)methyl]benzamide
-
-
5-[3-(methylsulfonyl)phenyl]-4-[(1-methyl-1H-tetrazol-5-yl)sulfanyl]thieno[2,3-d]pyrimidine
-
-
AG-538
-
at a concentration of 0.02 mM, AG-538 induces an almost complete inhibition of isoform PI5P4Kalpha and inhibits isoforms PI5P4Ks beta and gamma by 90% and 85%, respectively
N-(3-[[6-([1,1'-biphenyl]-3-yl)pyrimidin-4-yl]amino]phenyl)-4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]benzamide
-
-
N-[3-([6-[([1,1'-biphenyl]-3-yl)amino]pyrimidin-4-yl]amino)phenyl]-4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]benzamide
-
-
N-[3-([6-[([1,1'-biphenyl]-4-yl)amino]pyrimidin-4-yl]amino)phenyl]-4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]benzamide
-
-
tyrphostin
-
ATP-competitive inhibitors, i.e. tyrosine phosphorylation inhibitors, of isozyme PI5P4Kalpha
additional information
-
high-throughput inhibitor screening method, counterscreen assay and ATP competition assay, overview
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.0026 - 0.0101
(2E)-4-(dimethylamino)-N-[1-[(3-[[6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl]amino]phenyl)acetyl]piperidin-4-yl]but-2-enamide
0.0019
(2Z)-2-(1H-indol-3-yl)-3-(isoquinolin-5-yl)prop-2-enenitrile
-
isoform PI5P4Kalpha, at pH 7.5 and 37°C
0.0021 - 0.0089
3-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl]amino]phenyl)benzamide
0.0038
4-amino-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
-
isoform PI5P4Kbeta, at pH 7.5 and 37°C
0.00199 - 0.0356
4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl]amino]phenyl)benzamide
0.002 - 0.0318
4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl]amino]phenyl)cyclohexane-1-carboxamide
0.0035 - 0.0158
4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[6-(2-methyl-2H-benzimidazol-5-yl)pyrimidin-4-yl]amino]phenyl)benzamide
0.0013 - 0.0062
4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[6-(4-methylanilino)pyrimidin-4-yl]amino]phenyl)benzamide
0.00134 - 0.0099
4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[7-(4-methylphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]phenyl)benzamide
0.0065 - 0.0205
4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(4-methyl-3-[[6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl]amino]phenyl)benzamide
0.0053 - 0.0336
4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(5-[[6-(1H-indol-3-yl)pyrimidin-4-yl]amino]-2-methylphenyl)benzamide
0.0052 - 0.0298
4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-[(3-[[6-(1H-indol-3-yl)pyrimidin-4-yl]amino]phenyl)methyl]benzamide
0.0174 - 0.0304
N-(3-[[6-([1,1'-biphenyl]-3-yl)pyrimidin-4-yl]amino]phenyl)-4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]benzamide
0.0193 - 0.0245
N-[3-([6-[([1,1'-biphenyl]-3-yl)amino]pyrimidin-4-yl]amino)phenyl]-4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]benzamide
0.0013 - 0.0063
N-[3-([6-[([1,1'-biphenyl]-4-yl)amino]pyrimidin-4-yl]amino)phenyl]-4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]benzamide
0.0026
(2E)-4-(dimethylamino)-N-[1-[(3-[[6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl]amino]phenyl)acetyl]piperidin-4-yl]but-2-enamide
-
isoform PI5P4Kalpha, at pH 7.5 and 37°C
0.0101
(2E)-4-(dimethylamino)-N-[1-[(3-[[6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl]amino]phenyl)acetyl]piperidin-4-yl]but-2-enamide
-
isoform PI5P4Kbeta, at pH 7.5 and 37°C
0.0021
3-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl]amino]phenyl)benzamide
-
isoform PI5P4Kalpha, at pH 7.5 and 37°C
0.0089
3-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl]amino]phenyl)benzamide
-
isoform PI5P4Kbeta, at pH 7.5 and 37°C
0.00199
4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl]amino]phenyl)benzamide
-
isoform PI5P4Kalpha, at pH 7.5 and 37°C
0.0021
4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl]amino]phenyl)benzamide
-
isoform PI5P4Kalpha, at pH 7.5 and 37°C
0.0109
4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl]amino]phenyl)benzamide
-
isoform PI5P4Kbeta, at pH 7.5 and 37°C
0.0356
4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl]amino]phenyl)benzamide
-
isoform PI5P4Kbeta, at pH 7.5 and 37°C
0.002
4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl]amino]phenyl)cyclohexane-1-carboxamide
-
isoform PI5P4Kalpha, at pH 7.5 and 37°C
0.0318
4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl]amino]phenyl)cyclohexane-1-carboxamide
-
isoform PI5P4Kbeta, at pH 7.5 and 37°C
0.0035
4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[6-(2-methyl-2H-benzimidazol-5-yl)pyrimidin-4-yl]amino]phenyl)benzamide
-
isoform PI5P4Kalpha, at pH 7.5 and 37°C
0.0158
4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[6-(2-methyl-2H-benzimidazol-5-yl)pyrimidin-4-yl]amino]phenyl)benzamide
-
isoform PI5P4Kbeta, at pH 7.5 and 37°C
0.0013
4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[6-(4-methylanilino)pyrimidin-4-yl]amino]phenyl)benzamide
-
isoform PI5P4Kalpha, at pH 7.5 and 37°C
0.0062
4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[6-(4-methylanilino)pyrimidin-4-yl]amino]phenyl)benzamide
-
isoform PI5P4Kbeta, at pH 7.5 and 37°C
0.00134
4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[7-(4-methylphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]phenyl)benzamide
-
isoform PI5P4Kalpha, at pH 7.5 and 37°C
0.0099
4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[7-(4-methylphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]phenyl)benzamide
-
isoform PI5P4Kbeta, at pH 7.5 and 37°C
0.0065
4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(4-methyl-3-[[6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl]amino]phenyl)benzamide
-
isoform PI5P4Kalpha, at pH 7.5 and 37°C
0.0205
4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(4-methyl-3-[[6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl]amino]phenyl)benzamide
-
isoform PI5P4Kbeta, at pH 7.5 and 37°C
0.0053
4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(5-[[6-(1H-indol-3-yl)pyrimidin-4-yl]amino]-2-methylphenyl)benzamide
-
isoform PI5P4Kalpha, at pH 7.5 and 37°C
0.0336
4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(5-[[6-(1H-indol-3-yl)pyrimidin-4-yl]amino]-2-methylphenyl)benzamide
-
isoform PI5P4Kbeta, at pH 7.5 and 37°C
0.0052
4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-[(3-[[6-(1H-indol-3-yl)pyrimidin-4-yl]amino]phenyl)methyl]benzamide
-
isoform PI5P4Kalpha, at pH 7.5 and 37°C
0.0298
4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-[(3-[[6-(1H-indol-3-yl)pyrimidin-4-yl]amino]phenyl)methyl]benzamide
-
isoform PI5P4Kbeta, at pH 7.5 and 37°C
0.0174
N-(3-[[6-([1,1'-biphenyl]-3-yl)pyrimidin-4-yl]amino]phenyl)-4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]benzamide
-
isoform PI5P4Kalpha, at pH 7.5 and 37°C
0.0304
N-(3-[[6-([1,1'-biphenyl]-3-yl)pyrimidin-4-yl]amino]phenyl)-4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]benzamide
-
isoform PI5P4Kbeta, at pH 7.5 and 37°C
0.0193
N-[3-([6-[([1,1'-biphenyl]-3-yl)amino]pyrimidin-4-yl]amino)phenyl]-4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]benzamide
-
isoform PI5P4Kalpha, at pH 7.5 and 37°C
0.0245
N-[3-([6-[([1,1'-biphenyl]-3-yl)amino]pyrimidin-4-yl]amino)phenyl]-4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]benzamide
-
isoform PI5P4Kbeta, at pH 7.5 and 37°C
0.0013
N-[3-([6-[([1,1'-biphenyl]-4-yl)amino]pyrimidin-4-yl]amino)phenyl]-4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]benzamide
-
isoform PI5P4Kalpha, at pH 7.5 and 37°C
0.0063
N-[3-([6-[([1,1'-biphenyl]-4-yl)amino]pyrimidin-4-yl]amino)phenyl]-4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]benzamide
-
isoform PI5P4Kbeta, at pH 7.5 and 37°C
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.014
(2E)-2-(3,4-dihydroxybenzoyl)-3-(3,4-dihydroxyphenyl)prop-2-enenitrile
Homo sapiens
-
pH 7.4, 22°C, isozyme PI5P4Kalpha
0.002
(2E)-2-(3,4-dihydroxybenzoyl)-3-(4-hydroxy-3-iodo-5-methoxyphenyl)prop-2-enenitrile
Homo sapiens
-
pH 7.4, 22°C, isozyme PI5P4Kalpha
0.013
(3E)-5-amino-3-[(2Z)-1-cyano-2-(3H-indol-3-ylidene)ethylidene]-2,3-dihydro-1H-pyrazole-4-carbonitrile
Homo sapiens
-
pH 7.4, 22°C, isozyme PI5P4Kalpha
0.005
(3Z)-2-amino-4-(3,4,5-trihydroxyphenyl)buta-1,3-diene-1,1,3-tricarbonitrile
Homo sapiens
-
pH 7.4, 22°C, isozyme PI5P4Kalpha
0.0061 - 0.027
(E)-N-(4-(5-((2,5-dioxopyrrolidin-3-ylidene)methyl)pyridin-3-yl)phenyl)methanesulfonamide
0.0018 - 0.0086
(Z)-1-(4-(5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)-3-methylurea
0.035 - 0.05
(Z)-2-imino-5-((5-(4-(methylsulfonyl)phenyl)pyridin-3-yl)methylene)thiazolidin-4-one
0.011 - 0.05
(Z)-2-imino-5-((5-(4-(trifluoromethoxy)phenyl)pyridin-3-yl)methylene)thiazolidin-4-one
0.026 - 0.05
(Z)-2-imino-5-((5-(4-(trifluoromethyl)phenyl)pyridin-3-yl)methylene)thiazolidin-4-one
0.0039 - 0.05
(Z)-2-imino-5-((5-(4-methoxynaphthalen-1-yl)pyridin-3-yl)methylene)thiazolidin-4-one
0.0014 - 0.0043
(Z)-4-(5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)-N-methylbenzenesulfonamide
0.0088 - 0.05
(Z)-5-((5-(4-(dimethylamino)phenyl)pyridin-3-yl)methylene)-2-iminothiazolidin-4-one
0.011 - 0.05
(Z)-N-(3-(5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)acetamide
0.00066 - 0.0027
(Z)-N-(4-(2-amino-5-((2-imino-4-oxothiazolidin-5-ylidene)-methyl)pyridin-3-yl)phenyl)methanesulfonamide
0.021 - 0.05
(Z)-N-(4-(5-((2,4-dioxo-oxazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)methanesulfonamide
0.00013 - 0.0019
(Z)-N-(4-(5-((2,4-dioxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)methanesulfonamide
0.011 - 0.05
(Z)-N-(4-(5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)acetamide
0.00027 - 0.0017
(Z)-N-(4-(5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)methanesulfonamide
0.004 - 0.025
(Z)-N-(4-(6-amino-5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)methanesulfonamide
0.03
2,4-diamino-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
Homo sapiens
IC50 above 0.03 mM, at pH 7.4 and 26°C
0.03
3-(trifluoromethyl)phenyl 4-amino-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)pyrimidine-5-carboxylate
Homo sapiens
IC50 above 0.03 mM, at pH 7.4 and 26°C
0.0054
4-amino-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)-N-(3-phenoxyphenyl)pyrimidine-5-carboxamide
Homo sapiens
at pH 7.4 and 26°C
0.03
4-amino-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)-N-methyl-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
Homo sapiens
IC50 above 0.03 mM, at pH 7.4 and 26°C
0.0081
4-amino-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)-N-[3-(2,2,2-trifluoroethoxy)phenyl]pyrimidine-5-carboxamide
Homo sapiens
at pH 7.4 and 26°C
0.013
4-amino-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)-N-[4-methyl-3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
Homo sapiens
at pH 7.4 and 26°C
0.025
4-amino-2-(benzylamino)-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
Homo sapiens
at pH 7.4 and 26°C
0.03
4-amino-2-(dimethylamino)-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
Homo sapiens
IC50 above 0.03 mM, at pH 7.4 and 26°C
0.03
4-amino-2-(methylsulfanyl)-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
Homo sapiens
IC50 above 0.03 mM, at pH 7.4 and 26°C
0.03
4-amino-2-(piperidin-1-yl)-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
Homo sapiens
IC50 above 0.03 mM, at pH 7.4 and 26°C
0.03
4-amino-2-hydroxy-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
Homo sapiens
IC50 above 0.03 mM, at pH 7.4 and 26°C
0.03
4-amino-2-methoxy-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
Homo sapiens
IC50 above 0.03 mM, at pH 7.4 and 26°C
0.008
4-amino-2-[(2,2-dimethylpropyl)amino]-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
Homo sapiens
at pH 7.4 and 26°C
0.03
4-amino-2-[(tert-butylcarbamoyl)amino]-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
Homo sapiens
IC50 above 0.03 mM, at pH 7.4 and 26°C
0.0041
4-amino-2-[[(1-methyl-1H-pyrazol-5-yl)methyl]amino]-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
Homo sapiens
at pH 7.4 and 26°C
0.025
4-amino-N-(1,3-benzothiazol-5-yl)-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)pyrimidine-5-carboxamide
Homo sapiens
at pH 7.4 and 26°C
0.013
4-amino-N-(1-benzothiophen-5-yl)-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)pyrimidine-5-carboxamide
Homo sapiens
at pH 7.4 and 26°C
0.03
4-amino-N-[3-(trifluoromethyl)phenyl]-2-(3,4,4-trimethyl-2-oxoimidazolidin-1-yl)pyrimidine-5-carboxamide
Homo sapiens
IC50 above 0.03 mM, at pH 7.4 and 26°C
0.03
4-amino-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
Homo sapiens
IC50 above 0.03 mM, at pH 7.4 and 26°C
0.0061
(E)-N-(4-(5-((2,5-dioxopyrrolidin-3-ylidene)methyl)pyridin-3-yl)phenyl)methanesulfonamide
Homo sapiens
-
isoform PI5P4Kalpha, at pH 7.4 and 25°C
0.027
(E)-N-(4-(5-((2,5-dioxopyrrolidin-3-ylidene)methyl)pyridin-3-yl)phenyl)methanesulfonamide
Homo sapiens
-
isoform PI5P4Kbeta, at pH 7.4 and 25°C
0.0018
(Z)-1-(4-(5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)-3-methylurea
Homo sapiens
-
isoform PI5P4Kalpha, at pH 7.4 and 25°C
0.0086
(Z)-1-(4-(5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)-3-methylurea
Homo sapiens
-
isoform PI5P4Kbeta, at pH 7.4 and 25°C
0.035
(Z)-2-imino-5-((5-(4-(methylsulfonyl)phenyl)pyridin-3-yl)methylene)thiazolidin-4-one
Homo sapiens
-
isoform PI5P4Kalpha, at pH 7.4 and 25°C
0.05
(Z)-2-imino-5-((5-(4-(methylsulfonyl)phenyl)pyridin-3-yl)methylene)thiazolidin-4-one
Homo sapiens
-
IC50 above 0.05 mM, isoform PI5P4Kbeta, at pH 7.4 and 25°C
0.011
(Z)-2-imino-5-((5-(4-(trifluoromethoxy)phenyl)pyridin-3-yl)methylene)thiazolidin-4-one
Homo sapiens
-
isoform PI5P4Kalpha, at pH 7.4 and 25°C
0.05
(Z)-2-imino-5-((5-(4-(trifluoromethoxy)phenyl)pyridin-3-yl)methylene)thiazolidin-4-one
Homo sapiens
-
IC50 above 0.05 mM, isoform PI5P4Kbeta, at pH 7.4 and 25°C
0.026
(Z)-2-imino-5-((5-(4-(trifluoromethyl)phenyl)pyridin-3-yl)methylene)thiazolidin-4-one
Homo sapiens
-
isoform PI5P4Kbeta, at pH 7.4 and 25°C
0.05
(Z)-2-imino-5-((5-(4-(trifluoromethyl)phenyl)pyridin-3-yl)methylene)thiazolidin-4-one
Homo sapiens
-
IC50 above 0.05 mM, isoform PI5P4Kalpha, at pH 7.4 and 25°C
0.0039
(Z)-2-imino-5-((5-(4-methoxynaphthalen-1-yl)pyridin-3-yl)methylene)thiazolidin-4-one
Homo sapiens
-
isoform PI5P4Kalpha, at pH 7.4 and 25°C
0.05
(Z)-2-imino-5-((5-(4-methoxynaphthalen-1-yl)pyridin-3-yl)methylene)thiazolidin-4-one
Homo sapiens
-
IC50 above 0.05 mM, isoform PI5P4Kbeta, at pH 7.4 and 25°C
0.0014
(Z)-4-(5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)-N-methylbenzenesulfonamide
Homo sapiens
-
isoform PI5P4Kalpha, at pH 7.4 and 25°C
0.0043
(Z)-4-(5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)-N-methylbenzenesulfonamide
Homo sapiens
-
isoform PI5P4Kbeta, at pH 7.4 and 25°C
0.0088
(Z)-5-((5-(4-(dimethylamino)phenyl)pyridin-3-yl)methylene)-2-iminothiazolidin-4-one
Homo sapiens
-
isoform PI5P4Kalpha, at pH 7.4 and 25°C
0.05
(Z)-5-((5-(4-(dimethylamino)phenyl)pyridin-3-yl)methylene)-2-iminothiazolidin-4-one
Homo sapiens
-
IC50 above 0.05 mM, isoform PI5P4Kbeta, at pH 7.4 and 25°C
0.028
(Z)-5-((5-(4-fluorophenyl)pyridin-3-yl)methylene)-2-iminothiazolidin-4-one
Homo sapiens
-
isoform PI5P4Kbeta, at pH 7.4 and 25°C
0.05
(Z)-5-((5-(4-fluorophenyl)pyridin-3-yl)methylene)-2-iminothiazolidin-4-one
Homo sapiens
-
IC50 above 0.05 mM, isoform PI5P4Kalpha, at pH 7.4 and 25°C
0.011
(Z)-N-(3-(5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)acetamide
Homo sapiens
-
isoform PI5P4Kalpha, at pH 7.4 and 25°C
0.05
(Z)-N-(3-(5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)acetamide
Homo sapiens
-
IC50 above 0.05 mM, isoform PI5P4Kbeta, at pH 7.4 and 25°C
0.00066
(Z)-N-(4-(2-amino-5-((2-imino-4-oxothiazolidin-5-ylidene)-methyl)pyridin-3-yl)phenyl)methanesulfonamide
Homo sapiens
-
isoform PI5P4Kalpha, at pH 7.4 and 25°C
0.0027
(Z)-N-(4-(2-amino-5-((2-imino-4-oxothiazolidin-5-ylidene)-methyl)pyridin-3-yl)phenyl)methanesulfonamide
Homo sapiens
-
isoform PI5P4Kbeta, at pH 7.4 and 25°C
0.021
(Z)-N-(4-(5-((2,4-dioxo-oxazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)methanesulfonamide
Homo sapiens
-
isoform PI5P4Kalpha, at pH 7.4 and 25°C
0.05
(Z)-N-(4-(5-((2,4-dioxo-oxazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)methanesulfonamide
Homo sapiens
-
IC50 above 0.05 mM, isoform PI5P4Kbeta, at pH 7.4 and 25°C
0.00013
(Z)-N-(4-(5-((2,4-dioxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)methanesulfonamide
Homo sapiens
-
isoform PI5P4Kalpha, at pH 7.4 and 25°C
0.0019
(Z)-N-(4-(5-((2,4-dioxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)methanesulfonamide
Homo sapiens
-
isoform PI5P4Kbeta, at pH 7.4 and 25°C
0.011
(Z)-N-(4-(5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)acetamide
Homo sapiens
-
isoform PI5P4Kalpha, at pH 7.4 and 25°C
0.05
(Z)-N-(4-(5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)acetamide
Homo sapiens
-
IC50 above 0.05 mM, isoform PI5P4Kbeta, at pH 7.4 and 25°C
0.00027
(Z)-N-(4-(5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)methanesulfonamide
Homo sapiens
-
isoform PI5P4Kalpha, at pH 7.4 and 25°C
0.0017
(Z)-N-(4-(5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)methanesulfonamide
Homo sapiens
-
isoform PI5P4Kbeta, at pH 7.4 and 25°C
0.004
(Z)-N-(4-(6-amino-5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)methanesulfonamide
Homo sapiens
-
isoform PI5P4Kalpha, at pH 7.4 and 25°C
0.025
(Z)-N-(4-(6-amino-5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)methanesulfonamide
Homo sapiens
-
isoform PI5P4Kbeta, at pH 7.4 and 25°C
0.014
N-(3-((5-(4-(methylsulfonamido)phenyl)pyridin-3-yl)amino)phenyl)acetamide
Homo sapiens
-
isoform PI5P4Kalpha, at pH 7.4 and 25°C
0.045
N-(3-((5-(4-(methylsulfonamido)phenyl)pyridin-3-yl)amino)phenyl)acetamide
Homo sapiens
-
isoform PI5P4Kbeta, at pH 7.4 and 25°C
0.009
N-(3-((5-(4-(Mmthylsulfonamido)phenyl)pyridin-3-yl)oxy)phenyl)acetamide
Homo sapiens
-
isoform PI5P4Kalpha, at pH 7.4 and 25°C
0.025
N-(3-((5-(4-(Mmthylsulfonamido)phenyl)pyridin-3-yl)oxy)phenyl)acetamide
Homo sapiens
-
isoform PI5P4Kbeta, at pH 7.4 and 25°C
0.0053
N-(3-(5-(4-(methylsulfonamido)phenyl)pyridin-3-yl)phenyl)acetamide
Homo sapiens
-
isoform PI5P4Kalpha, at pH 7.4 and 25°C
0.036
N-(3-(5-(4-(methylsulfonamido)phenyl)pyridin-3-yl)phenyl)acetamide
Homo sapiens
-
isoform PI5P4Kbeta, at pH 7.4 and 25°C
0.002
N-(4-(5-(1H-indol-4-yl)pyridin-3-yl)phenyl)methanesulfonamide
Homo sapiens
-
isoform PI5P4Kalpha, at pH 7.4 and 25°C
0.0094
N-(4-(5-(1H-indol-4-yl)pyridin-3-yl)phenyl)methanesulfonamide
Homo sapiens
-
isoform PI5P4Kbeta, at pH 7.4 and 25°C
0.0089
N-(4-(5-(2-oxoindolin-4yl)pyridin-3-yl)phenyl)methanesulfonamide
Homo sapiens
-
isoform PI5P4Kalpha, at pH 7.4 and 25°C
0.015
N-(4-(5-(2-oxoindolin-4yl)pyridin-3-yl)phenyl)methanesulfonamide
Homo sapiens
-
isoform PI5P4Kbeta, at pH 7.4 and 25°C
0.0037
N-(4-(5-(4-(3-methylureido)phenyl)pyridin-3-yl)phenyl)methanesulfonamide
Homo sapiens
-
isoform PI5P4Kalpha, at pH 7.4 and 25°C
0.043
N-(4-(5-(4-(3-methylureido)phenyl)pyridin-3-yl)phenyl)methanesulfonamide
Homo sapiens
-
isoform PI5P4Kbeta, at pH 7.4 and 25°C
0.0021
N-(5-(5-(1H-indol-4-yl)pyridin-3-yl)phenyl)methanesulfonamide
Homo sapiens
-
isoform PI5P4Kalpha, at pH 7.4 and 25°C
0.022
N-(5-(5-(1H-indol-4-yl)pyridin-3-yl)phenyl)methanesulfonamide
Homo sapiens
-
isoform PI5P4Kbeta, at pH 7.4 and 25°C
0.0032
N-(6-(5-(1H-indol-4-yl)pyridin-3-yl)phenyl)methanesulfonamide
Homo sapiens
-
isoform PI5P4Kalpha, at pH 7.4 and 25°C
0.029
N-(6-(5-(1H-indol-4-yl)pyridin-3-yl)phenyl)methanesulfonamide
Homo sapiens
-
isoform PI5P4Kbeta, at pH 7.4 and 25°C
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
additional information
additional information
Bacterially-expressed recombinant PIP4Kgamma is completely inactive, but does have the ability to associate with active PIP4Kalpha in vitro.
additional information
In three independent experiments, the ratio (tagged cells to wild-type) of immunoprecipitated enzyme activity, quantified by densitometry or by scintillation counting, is 2.37 +/-0.27
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
7.4
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
Site-directed mutagenesis is performed on the human type IIbeta PIPkin cloned into pEGFP-C1 using QuikChange mutagenesis method, to introduce an Glu300Asp amino acid substitution into the human nuclear localisation sequence producing the equivalent chicken sequence 289-DRAEQEEMEVE(E300D)RAEDEE-306
UniProt
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
SOURCE
DT40 cell from chicken, that expresses active PIPkin IIbetA tagged at the C-terminus of Hef, a protein component of the Fanconi anemia-related tumor-suppressor complex.
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY
GeneOntology No.
LITERATURE
SOURCE
small amount, it is unclear how much of PIPkin II in the cytoplasmic fraction can be accounted for by nuclear disintegration or by leakage of PIPkinIIbeta during the fractionation.
-
isozyme PIP4Kbeta can modulate the nuclear localization of isozyme PIP4Kalpha
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
malfunction
physiological function
malfunction
-
phosphatidylinositol-5-phosphate 4-kinase type II beta knockdown inhibits E-cadherin upregulation induced by the vitamin D3 metabolite 1alpha,25(OH)2D3, while phosphatidylinositol-5-phosphate 4-kinase type II alpha does not
malfunction
-
enzyme depletion enhances the spindle pole accumulation of mitotic centromere-associated kinesin, a microtubule-depolymerizing kinesin, and results in a less stable spindle pole-associated microtubule
physiological function
-
isozyme PIP4Kalpha affects the ubiquitination of isozyme PIP4Kbeta by the SPOP-CUL3 complex. Isozyme PIP4Kbeta can modulate the nuclear localization of isozyme PIP4Kalpha, and isozyme PIP4Kalpha has a role in regulating isozyme PIP4Kbeta functions
physiological function
-
the enzyme is required for vitamin D receptor-mediated E-cadherin induction in SW480-ADH cells expressing the vitamin D receptor. The enzyme is also involved in the suppression of the cell motility induced by 1alpha,25-dihydroxyvitamin D3, PIPKIIbeta inhibits the migratory activity of SW480-ADH cells. PIPKIIbeta-mediated phosphatidylinositol-4,5-bisphosphate signaling is important for E-cadherin upregulation and inhibition of cellular motility induced by vitamin D receptor activation. PIPKIIbeta but not PIPKIIalpha promotes E-cadherin upregulation in the presence of 1alpha,25(OH)2D3, overview
physiological function
-
the enzyme is part of piperine-mediated anti-inflammatory signaling mechanisms
physiological function
the enzyme isoform PIP5K2B is linked to the pathogenesis of obesity, insulin resistance and diabetes
physiological function
-
the enzyme plays a role in CD3 receptor signal transduction and is is a key component in early T cell activation signaling cascades
physiological function
-
human enzyme isoforms are able to rescue salivary gland cell size defects in the Drosophila enzyme-deficient mutant
physiological function
-
the enzyme is required for the assembly of bipolar spindles. The enzyme and phosphatidylinositol 4,5-bisphosphate may negatively regulate the microtubule depolymerization activity of mitotic centromere-associated kinesin by reducing polo-like kinase 1-mediated phosphorylation of mitotic centromere-associated kinesin
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION
The reliability class of the localization prediction ranges from 1 (very reliable) to 5 (not reliable).
The reliability class of the localization prediction ranges from 1 (very reliable) to 5 (not reliable). PI42A_HUMAN
406
0
46225
Swiss-Prot
other Location (Reliability: 4)
PI42B_HUMAN
416
0
47378
Swiss-Prot
other Location (Reliability: 5)
PI42C_HUMAN
421
0
47300
Swiss-Prot
other Location (Reliability: 3)
PDB
SCOP
CATH
UNIPROT
ORGANISM
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
47000
49000
-
2 * 49000, recombinant isozyme PIP4Kbeta, SDS-PAGE, and crystal structure of isozyme PIP4Kbeta
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
homodimer
-
2 * 49000, recombinant isozyme PIP4Kbeta, SDS-PAGE, and crystal structure of isozyme PIP4Kbeta
CRYSTALLIZATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
isoform PI5P4Kalpha in complex with inhibitor CVM-05-002, sitting drop vapor diffusion method, using 2 M NH4 (pH 6.5)
-
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
E300D
Site-directed mutagenesis is performed on the human Type IIbeta PIPkin cloned into pEGFP-C1 using the QuikChange mutagenesis method, to introduce an Glu300Asp amino acid substitution into the human nuclear localisation sequence producing the equivalent chicken sequence.
N165I
-
the mutation in isoform PI5P4Kgamma leads to resistance to inhibitor NIH-12848
additional information
additional information
-
isozymes PIPKalpha and PIP4Kbeta inactivation by specific RNAi. Overexpression of PIP4Kalpha leads to a dramatic increase in PIP4K activity, that is not present when wild-type PIP4Kbeta kinase is expressed
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
recombinant GST-tagged isozymes by glutathione affinity chromatography, recombinant HA-tagged isozymes by affinity chromatography from HEK-293 cells
-
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
expression of EGFP-tagged isozymes PIPKIIbeta and PIPKIIalpha in SW480-ADH cells cytosol and nucleus or cytosol, respectively
-
PIP5K2 genes are amplified from a whole human brain marathon-ready cDNA library using gene-specific primers. Recombinant protein is expressed from Escherichia coli harbouring PIP5K2s in pET-32a. PCR products are cloned, via incorporated HindIII and BamHI restriction sites, into appropriate plasmid vectors. HeLa, HEK 293, COS-7 and NRK cells are transiently transfected with plasmid constructs.
recombinant expression of GST-tagged isozymes and of HA-tagged isozymes in HEK-293 cells
-
The last 2.6 kbp of the human PIPkin IIbeta gene and the following 3.6 kbp are cloned and inserted into a plasmid which placed a FLAG-(His6)2 double-tag, followed by a puromycin selection cassette between them. Transfection of this into DT40 cells followed by puromycin selection produces cells which have the tag attached to the C-terminus of the protein when expressed by one of the two alleles. Experiments are conducted on one clonal line derived from this procedure calling JPR3. Successful integration of the tag at the correct genomic location was confirmed by PCR analysis.
APPLICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
medicine
-
phosphatidylinositol-5-phosphate 4-kinase type II beta might be an effective therapeutic target for preventing of colon cancer progression
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Rameh, L.E.; Tolias, K.F.; Duckworth, B.C.; Cantley, L.C.
A new pathway for synthesis of phosphatidylinositol-4,5-bisphosphate
Nature
390
192-196
1997
Homo sapiens
Carricaburu, V.; Lamia, K.A.; Lo, E.; Favereaux, L.; Payrastre, B.; Cantley, L.C.; Rameh, L.E.
The phosphatidylinositol (PI)-5-phosphate 4-kinase type II enzyme controls insulin signaling by regulating PI-3,4,5-trisphosphate degradation
Proc. Natl. Acad. Sci. USA
100
9867-9872
2003
Homo sapiens
Clarke, J.H.; Emson, P.C.; Irvine, R.F.
Localization of Phosphatidylinositol phosphate Kinase II gamma in kidney to a membrane trafficking compartment within specialized cells of the nephron
Am. J. Physiol. Renal Physiol.
295
F1422-1430
2008
Homo sapiens (Q8TBX8), Mus musculus (Q91XU3)
Richardson, J.P.; Wang, M.; Clarke, J.H.; Patel, K.J.; Irvine, R.F.
Genomic tagging of endogenous type IIbeta phosphatidylinositol 5-phosphate 4-kinase in DT40 cells reveals a nuclear localization
Cell. Signal.
19
1309-1314
2007
Gallus gallus, Homo sapiens (P78356)
Kouchi, Z.; Fujiwara, Y.; Yamaguchi, H.; Nakamura, Y.; Fukami, K.
Phosphatidylinositol 5-phosphate 4-kinase type II beta is required for vitamin D receptor-dependent E-cadherin expression in SW480 cells
Biochem. Biophys. Res. Commun.
408
523-529
2011
Homo sapiens
Bultsma, Y.; Keune, W.J.; Divecha, N.
PIP4Kbeta interacts with and modulates nuclear localization of the high-activity PtdIns5P-4-kinase isoform PIP4Kalpha
Biochem. J.
430
223-235
2010
Homo sapiens, Rattus norvegicus
Davis, M.I.; Sasaki, A.T.; Shen, M.; Emerling, B.M.; Thorne, N.; Michael, S.; Pragani, R.; Boxer, M.; Sumita, K.; Takeuchi, K.; Auld, D.S.; Li, Z.; Cantley, L.C.; Simeonov, A.
A homogeneous, high-throughput assay for phosphatidylinositol 5-phosphate 4-kinase with a novel, rapid substrate preparation
PLoS ONE
8
e54127
2013
Homo sapiens
Bulley, S.J.; Clarke, J.H.; Droubi, A.; Giudici, M.L.; Irvine, R.F.
Exploring phosphatidylinositol 5-phosphate 4-kinase function
Adv. Biol. Regul.
57
193-202
2015
Homo sapiens
Voss, M.D.; Czechtizky, W.; Li, Z.; Rudolph, C.; Petry, S.; Brummerhop, H.; Langer, T.; Schiffer, A.; Schaefer, H.L.
Discovery and pharmacological characterization of a novel small molecule inhibitor of phosphatidylinositol-5-phosphate 4-kinase, type II, beta
Biochem. Biophys. Res. Commun.
449
327-331
2014
Homo sapiens (P78356)
Clarke, J.H.; Irvine, R.F.
Evolutionarily conserved structural changes in phosphatidylinositol 5-phosphate 4-kinase (PI5P4K) isoforms are responsible for differences in enzyme activity and localization
Biochem. J.
454
49-57
2013
Homo sapiens (P48426), Homo sapiens (P78356), Homo sapiens (Q8TBX8), Homo sapiens
Sinha, R.K.; Bojjireddy, N.; Kulkarni, D.; Ratheesh, A.; Chiplunkar, S.V.; Gude, R.; Subrahmanyam, G.
Type II phosphatidylinositol 4-kinase beta is an integral signaling component of early T cell activation mechanisms
Biochimie
95
1560-1566
2013
Homo sapiens
Boura, E.; Nencka, R.
Phosphatidylinositol 4-kinases: Function, structure, and inhibition
Exp. Cell Res.
337
136-145
2015
Homo sapiens
Bojjireddy, N.; Sinha, R.K.; Subrahmanyam, G.
Type II phosphatidylinositol 4-kinases interact with FcepsilonRIgamma subunit in RBL-2H3 cells
Mol. Cell. Biochem.
390
197-203
2014
Homo sapiens
Manz, T.D.; Sivakumaren, S.C.; Yasgar, A.; Hall, M.D.; Davis, M.I.; Seo, H.S.; Card, J.D.; Ficarro, S.B.; Shim, H.; Marto, J.A.; Dhe-Paganon, S.; Sasaki, A.T.; Boxer, M.B.; Simeonov, A.; Cantley, L.C.; Shen, M.; Zhang, T.; Ferguson, F.M.; Gray, N.S.
Structure-activity relationship study of covalent pan-phosphatidylinositol 5-phosphate 4-kinase inhibitors
ACS Med. Chem. Lett.
11
346-352
2020
Homo sapiens
Giudici, M.; Clarke, J.; Irvine, R.
Phosphatidylinositol 5-phosphate 4-kinase gamma (PI5P4Kgamma), a lipid signalling enigma
Adv. Biol. Regul.
61
47-50
2016
Homo sapiens
Mathre, S.; Reddy, K.B.; Ramya, V.; Krishnan, H.; Ghosh, A.; Raghu, P.
Functional analysis of the biochemical activity of mammalian phosphatidylinositol 5 phosphate 4-kinase enzymes
Biosci. Rep.
39
BSR20182210
2019
Homo sapiens
Lin, T.C.; Kuo, H.H.; Wu, Y.C.; Pan, T.S.; Yih, L.H.
Phosphatidylinositol-5-phosphate 4-kinase gamma accumulates at the spindle pole and prevents microtubule depolymerization
Cell Div.
14
9-9
2019
Homo sapiens
Manz, T.D.; Sivakumaren, S.C.; Ferguson, F.M.; Zhang, T.; Yasgar, A.; Seo, H.S.; Ficarro, S.B.; Card, J.D.; Shim, H.; Miduturu, C.V.; Simeonov, A.; Shen, M.; Marto, J.A.; Dhe-Paganon, S.; Hall, M.D.; Cantley, L.C.; Gray, N.S.
Discovery and structure-activity relationship study of (Z)-5-methylenethiazolidin-4-one derivatives as potent and selective pan-phosphatidylinositol 5-phosphate 4-kinase inhibitors
J. Med. Chem.
63
4880-4895
2020
Homo sapiens
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