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Information on EC 2.7.1.149 - 1-phosphatidylinositol-5-phosphate 4-kinase
for references in articles please use BRENDA:EC2.7.1.149
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EC Tree 2 Transferases
2.7 Transferring phosphorus-containing groups
2.7.1 Phosphotransferases with an alcohol group as acceptor
2.7.1.149 1-phosphatidylinositol-5-phosphate 4-kinase
The enzyme appears in viruses and cellular organisms
- 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
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positive-sense
-
oxysterol-binding
- enteroviruses
- ns5a
- picornaviruses
- medicine
Reaction Schemes
showSynonyms
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
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SYNONYM 
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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-
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1-phosphatidylinositol-5-phosphate 4-kinase
Diphosphoinositide kinase
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phosphatidylinositol 5 phosphate 4-kinase
phosphatidylinositol 5-phosphate 4-kinase
phosphatidylinositol 5-phosphate 4-kinase gamma
phosphatidylinositol phosphate kinase II gamma
PI5P4K
PI5P4Kalpha
PI5P4Kbeta
PI5P4Kgamma
PIP(4)K
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-
-
-
PIP4K
Pip4k2a
Pip4k2b
PIP4Kalpha
PIP4Kbeta
PIP4Kgamma
PIP5KII-alpha
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-
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PIP5KIII
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-
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PIPKII
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-
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PIPKIIalpha
PIPkinIIbeta
PtdIns(4)P-5-kinase B isoform
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PtdIns(4)P-5-kinase C isoform
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PtdIns5P 4-kinase
PtdIns5P-4-kinase
type II alpha phosphatidylinositol-5-phosphate 4-kinase
type II PIP kinase
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type IIbeta phosphatidylinositol 5-phosphate 4-kinase
type IIbeta PIPkin
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REACTION
REACTION DIAGRAM
COMMENTARY
ORGANISM
UNIPROT
LITERATURE
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate = ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
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REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
phospho group transfer
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-
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Phosphorylation
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PATHWAY SOURCE
PATHWAYS
MetaCyc
D-myo-inositol (1,4,5)-trisphosphate biosynthesis, D-myo-inositol-5-phosphate metabolism
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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
LITERATURE
COMMENTARY
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
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Substrates: poor substrate compared to 1-phosphatidyl-1D-myo-inositol 5-phosphate
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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
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Substrates: -
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ATP + 1-phosphatidyl-1D-myo-inositol 4-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
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Substrates: 5' phosphorylation
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ATP + 1-phosphatidyl-1D-myo-inositol 4-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
Substrates: 5' phosphorylation
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ATP + 1-phosphatidyl-1D-myo-inositol 4-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
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Substrates: -
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ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
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Substrates: -
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ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
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Substrates: -
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ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
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Substrates: -
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ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
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Substrates: phosphorylation at the D-4 position
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ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
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Substrates: -
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?
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
Substrates: -
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ir
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
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Substrates: -
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?
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
Substrates: -
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?
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
Substrates: -
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?
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
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Substrates: -
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?
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
Substrates: -
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?
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
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Substrates: -
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?
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
-
Substrates: -
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?
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
Substrates: -
Products: -
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ir
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
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Substrates: -
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?
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
-
Substrates: -
Products: -
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?
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
-
Substrates: the enzyme may have an important role in synthesis of phosphatidylinositol bisphosphate in the endoplasmic reticulum
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?
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
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Substrates: -
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?
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
-
Substrates: -
Products: -
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?
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
-
Substrates: type II PIP kinases are physiological targets for protein kinase D phosphorylation. This modification is likely to regulate inositol lipid turnover by inhibition of these lipid kinases
Products: -
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?
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
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Substrates: -
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?
additional information
?
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Substrates: the enzyme phosphorylated His-tagged ANAC078 protein at the C-terminus
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additional information
?
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Substrates: 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
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additional information
?
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Substrates: 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
Products: -
Products: -
?
additional information
?
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Substrates: 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
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NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
LITERATURE
COMMENTARY
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
-
Substrates: 5' phosphorylation
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r
ATP + 1-phosphatidyl-1D-myo-inositol 4-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
Substrates: 5' phosphorylation
Products: -
Products: -
r
ATP + 1-phosphatidyl-1D-myo-inositol 4-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
-
Substrates: -
Products: -
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?
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
-
Substrates: -
Products: -
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?
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
-
Substrates: -
Products: -
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?
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
-
Substrates: -
Products: -
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?
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
-
Substrates: -
Products: -
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?
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
Substrates: -
Products: -
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ir
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
-
Substrates: -
Products: -
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?
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
Substrates: -
Products: -
Products: -
?
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
Substrates: -
Products: -
Products: -
?
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
-
Substrates: -
Products: -
Products: -
?
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
Substrates: -
Products: -
Products: -
?
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
-
Substrates: -
Products: -
Products: -
?
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
-
Substrates: -
Products: -
Products: -
?
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
Substrates: -
Products: -
Products: -
ir
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
-
Substrates: -
Products: -
Products: -
?
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
-
Substrates: the enzyme may have an important role in synthesis of phosphatidylinositol bisphosphate in the endoplasmic reticulum
Products: -
Products: -
?
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
-
Substrates: -
Products: -
Products: -
?
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
-
Substrates: -
Products: -
Products: -
?
ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
-
Substrates: type II PIP kinases are physiological targets for protein kinase D phosphorylation. This modification is likely to regulate inositol lipid turnover by inhibition of these lipid kinases
Products: -
Products: -
?
additional information
?
-
-
Substrates: 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
Products: -
Products: -
?
additional information
?
-
-
Substrates: 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
Products: -
Products: -
?
additional information
?
-
-
Substrates: 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
Products: -
Products: -
?
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COFACTOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
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METALS and IONS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
Mg2+
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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
-
-
(E)-N-(4-(5-((2,5-dioxopyrrolidin-3-ylidene)methyl)pyridin-3-yl)phenyl)methanesulfonamide
-
-
(Z)-1-(4-(5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)-3-methylurea
-
-
(Z)-2-imino-5-((5-(4-(methylsulfonyl)phenyl)pyridin-3-yl)methylene)thiazolidin-4-one
-
-
(Z)-2-imino-5-((5-(4-(trifluoromethoxy)phenyl)pyridin-3-yl)methylene)thiazolidin-4-one
-
-
(Z)-2-imino-5-((5-(4-(trifluoromethyl)phenyl)pyridin-3-yl)methylene)thiazolidin-4-one
-
-
(Z)-2-imino-5-((5-(4-methoxynaphthalen-1-yl)pyridin-3-yl)methylene)thiazolidin-4-one
-
-
(Z)-4-(5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)-N-methylbenzenesulfonamide
-
-
(Z)-5-((5-(4-(dimethylamino)phenyl)pyridin-3-yl)methylene)-2-iminothiazolidin-4-one
-
-
(Z)-N-(3-(5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)acetamide
-
-
(Z)-N-(4-(2-amino-5-((2-imino-4-oxothiazolidin-5-ylidene)-methyl)pyridin-3-yl)phenyl)methanesulfonamide
-
-
(Z)-N-(4-(5-((2,4-dioxo-oxazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)methanesulfonamide
-
-
(Z)-N-(4-(5-((2,4-dioxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)methanesulfonamide
-
-
(Z)-N-(4-(5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)acetamide
-
-
(Z)-N-(4-(5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)methanesulfonamide
-
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
-
-
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
-
4-amino-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)-N-methyl-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
-
4-amino-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)-N-[3-(2,2,2-trifluoroethoxy)phenyl]pyrimidine-5-carboxamide
-
4-amino-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
-
-
4-amino-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)-N-[4-methyl-3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
-
4-amino-2-(benzylamino)-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
-
4-amino-2-(dimethylamino)-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
-
4-amino-2-(methylsulfanyl)-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
-
4-amino-2-(piperidin-1-yl)-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
-
4-amino-2-hydroxy-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
-
4-amino-2-methoxy-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
-
4-amino-2-[(2,2-dimethylpropyl)amino]-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
-
4-amino-2-[(tert-butylcarbamoyl)amino]-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
-
4-amino-2-[[(1-methyl-1H-pyrazol-5-yl)methyl]amino]-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
-
4-amino-N-(1,3-benzothiazol-5-yl)-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)pyrimidine-5-carboxamide
-
4-amino-N-(1-benzothiophen-5-yl)-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)pyrimidine-5-carboxamide
-
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
-
NIH-12848
-
full designation NCGC00012848-02, specific inhibitor of isoform PI5P4Kgamma, does not inhibit the alpha and beta PI5P4K isoforms at concentrations up to 0.1 mM; inhibitor of isoform PI5P4Kgamma only
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KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
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TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
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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
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
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
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SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
additional information
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
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
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pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
7.4
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TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
30
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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
-
-
brenda
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
brenda
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SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
SOURCE
-
isoform PI5P4Kbeta is expressed in neuronal populations, especially hippocampus and cortex
brenda
-
isoform PI5P4Kalpha localizes to white matter tracts, especially the corpus callosum
brenda
restricted expression in the thick ascending limb of the loop of Henle and in the intercalated cells of the collecting duct
brenda
-
isoform PI5P4Kbeta is expressed in neuronal populations, especially hippocampus and cortex
brenda
-
both isoforms PI5P4Kalpha and PI5P4Kbeta are contained in axon terminals and dendritic spines adjacent to the synaptic membrane
brenda
-
quantitative real-time PCR enzyme expression analysis
brenda
additional information
-
isoform PI5P4Kalpha is expressed in adulthood, whereas isoform PI5P4Kbeta is expressed early in development
brenda
-
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.
brenda
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.
brenda
PIP4Kgamma in heart run predominantly as a 40 kDa band, suggesting that processing of this isoform occurs.
brenda
cortex and outer medulla, regulation of vesicular transport in specialized kidney epithelial cells
brenda
additional information
-
light-driven translocation of PIPKIIalpha from the rod inner segment to rod outer segment, and subsequent binding to the ROS membrane
brenda
additional information
-
light-driven translocation of PIPKIIalpha from the rod inner segment to rod outer segment, and subsequent binding to the ROS membrane
brenda
additional information
-
light-driven translocation of PIPKIIalpha from the rod inner segment to rod outer segment, and subsequent binding to the ROS membrane
-
brenda
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LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY
GeneOntology No.
LITERATURE
SOURCE
partial Golgi localization, primarily the matrix of the cis-Golgi
brenda
-
PI5P4Kalpha is membrane-bound in DT40 cells with a significant amount of endogenous PI5P4Kalpha in the nucleus
brenda
additional information
-
analysis of subcellular localization of native and recombinant isozyme PI5P4Kalpha, overview
-
brenda
-
small amount, it is unclear how much of PIPkin IIbeta in the cytoplasmic fraction can be accounted for by nuclear disintegration or by leakage of PIPkinIIbeta during the fractionation.
brenda
-
isoform PI5P4Kalpha is predominantly (possible entirely) cytoplasmic when isoform PI5P4Kbeta is stably deleted from cells. In contrast, when PI5P4Kbeta is inducibly removed within 1 h PI5P4Kalpha retains its wild-type distribution of approximately 50:50 between cytoplasm and nucleus
brenda
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.
brenda
-
isoform PI5P4Kalpha is chromatin-associated. In the exponential phase of growth PI5P4Kbeta is primarily cytoplasmic but translocates to the nucleus upon growth into the stationary phase or upon serum starvation
brenda
-
isozyme PIP4Kbeta can modulate the nuclear localization of isozyme PIP4Kalpha
brenda
-
PI5P4Kalpha is membrane-bound in DT40 cells with a significant amount of endogenous PI5P4Kalpha in the nucleus
brenda
-
isozyme PIP4Kbeta can modulate the nuclear localization of isozyme PIP4Kalpha
brenda
Highest Expressing Human Cell Lines
Cell Line LinksPlease wait a moment until the data is sorted. This message will disappear when the data is sorted.
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
evolution
malfunction
metabolism
-
the enzyme regulates plasma-membrane phosphatidylinositol 3,4,5-trisphosphate turnover and insulin signalling. The enzyme is required to limit phosphatidylinositol 3,4,5-trisphosphate levels during insulin receptor activation
physiological function
evolution
-
two subfamilies of phosphatidylinositol 5-phosphate 4-kinase kinases produce 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate from independent pools of substrates. In addition, type I and II subfamilies of PIPK can localize in different subcellular compartments and are involved in the synthesis of 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate in distinct sites within cell
evolution
-
two subfamilies of phosphatidylinositol 5-phosphate 4-kinases produce 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate from independent pools of substrates. In addition, type I and II subfamilies of PIPK can localize in different subcellular compartments and are involved in the synthesis of 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate in distinct sites within cell
evolution
-
PI5P4Kalpha is present in all vertebrates, and a few organisms are missing either beta or gamma. Several key structural differences between the three mammalian PI5P4Ks largely account for their different activities, e.g. a glycine-rich loop supposed to be involved with substrate interaction
evolution
-
two subfamilies of phosphatidylinositol 5-phosphate 4-kinases produce 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate from independent pools of substrates. In addition, type I and II subfamilies of PIPK can localize in different subcellular compartments and are involved in the synthesis of 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate in distinct sites within cell
-
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
-
isoform PI4Kgamma5 deficiency results in the serrated leaves and accelerated cell division at leaf margin due to the increased auxin level
malfunction
-
loss-of-function mutants in PIP4K show reduced body weight and prolonged larval development
malfunction
-
enzyme knockdown leads to severe morphological abnormalities, including midbody winding defects at 48 h post-fertilization
malfunction
-
flies lacking the enzyme show mislocalization of rhodopsin 1 on expanded endomembranes within the cell body. Enzyme loss is associated with increased clathrin-mediated endocytosis and an enlarged Rab5-positive compartment in cultured Drosophila cells
malfunction
-
mice lacking both enzyme isoforms in the liver have a defect in the ability to catabolize lipid droplets following a period of fasting. Enzyme loss of both isoforms results in lipid droplets accumulation and autophagy defects in MEF cells. Enzyme loss modifies expression of lysosomal and mTORC1 genes and alters metabolism as well as increases transcription factor EB nuclear translocation and activity
malfunction
-
enzyme-deficient animals show enhanced insulin signaling-dependent phenotypes and are resistant to the metabolic consequences of a high-sugar diet
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
malfunction
-
long-Term loss of isoform PI5P4Kalpha by gene disruption results in compromised Akt phosphorylation
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
-
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
-
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
-
greater type II alpha PIP kinase activity in the light-adapted rod outer segment membrane results from light-driven translocation of PIPKIIalpha from the rod inner segment to rod outer segment, and subsequent binding to the rod outer segment membrane, thus improving access of the kinase to its lipid substrates. Light-induced tyrosine phosphorylation of rod outer segment membrane proteins regulate the translocation, membrane binding and activation of type II alpha phosphatidylinositol-5-phosphate 4-kinase
physiological function
-
greater type II alpha PIP kinase activity in the light-adapted rod outer segment membrane results from light-driven translocation of PIPKIIalpha from the rod inner segment to rod outer segment, and subsequent binding to the rod outer segment membrane, thus improving access of the kinase to its lipid substrates. Light-induced tyrosine phosphorylation of rod outer segment membrane proteins regulate the translocation, membrane binding and activation of type II alpha phosphatidylinositol-5-phosphate 4-kinase
physiological function
-
the enzyme is part of piperine-mediated anti-inflammatory signaling mechanisms
physiological function
-
isoform PI4Kgamma5 interacts with transcription factor ANAC078 to negatively regulate auxin synthesis and hence influences cell proliferation and leaf development
physiological function
-
the enzyme regulates TOR signaling and cell growth during Drosophila development
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
-
the enzyme regulates clathrin-mediated endocytosis of rhodopsin 1 and supports rhodopsin 1 trafficking during pupal metamorphosis
physiological function
-
the enzyme plays a critical role in autophagy in times of energy stress
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
physiological function
-
the enzyme isoforms play potential roles in synaptic transmission
physiological function
-
the enzyme is necessary for maintenance of normal plasma membrane phosphatidylinositol (3,4,5)-trisphosphate levels in DT-40 cells. The enzyme is an acute negative regulator of mammalian target of rapamycin complex 2
physiological function
-
greater type II alpha PIP kinase activity in the light-adapted rod outer segment membrane results from light-driven translocation of PIPKIIalpha from the rod inner segment to rod outer segment, and subsequent binding to the rod outer segment membrane, thus improving access of the kinase to its lipid substrates. Light-induced tyrosine phosphorylation of rod outer segment membrane proteins regulate the translocation, membrane binding and activation of type II alpha phosphatidylinositol-5-phosphate 4-kinase
-
Show AA Sequence and Transmembrane Helices (4215 entries)
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PDB
SCOP
CATH
UNIPROT
ORGANISM
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MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
47000
49000
-
2 * 49000, recombinant isozyme PIP4Kbeta, SDS-PAGE, and crystal structure of isozyme PIP4Kbeta
53000
47000
predicted and confirmed by western blotting, represents the phosphorylated form of mature PIP4Kgamma
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SUBUNIT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
homodimer
homodimer
-
2 * 70000, enhanced monomeric green fluorescent protein-tagged isoform PI5P4Kalpha, SDS-PAGE
homodimer
-
2 * 49000, recombinant isozyme PIP4Kbeta, SDS-PAGE, and crystal structure of isozyme PIP4Kbeta
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POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
phosphoprotein
phosphoprotein
-
enzyme PIPKIIgamma is phosphorylated in vivo. Phosphorylation is induced by treatment of mitogens such as serum and epidermal growth factor
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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)
-
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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.
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
additional information
-
knockdown of both isozymes, enzyme activity associated with kinase-inactive Myc-PIP4Kbeta is reduced to 24% compared with that associated with the active Myc-PIP4Kbeta
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PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
affinity purification of FLAG-His6 tagged proteins using TALON beads
recombinant GST-tagged isozymes by glutathione affinity chromatography, recombinant HA-tagged isozymes by affinity chromatography from HEK-293 cells
-
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CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
expressed in a enzyme-deficient mutant of Drosophila melanogaster
expressed in Escherichia coli BL21(DE3) cells
expression of EGFP-tagged isozymes PIPKIIbeta and PIPKIIalpha in SW480-ADH cells cytosol and nucleus or cytosol, respectively
-
PI5P4Kalpha is predominantly in the cytoplasm, principally cytosolic, when recombinantly expressed
-
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.
quantitative real-time PCR expression analysis, expression of isozyme PIPKIIalpha in Xenopus laevis oocytes
-
recombinant expression of GST-tagged isozymes and of HA-tagged isozymes in HEK-293 cells
-
recombinant expression of Myc-tagged isozymes, co-expression of the wild-type PIP4Kalpha isozyme suppresses ubiquitination of isozyme PIP4Kbeta
-
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.
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.
-
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.
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EXPRESSION
ORGANISM
UNIPROT
LITERATURE
at later embryonic stages, high PIP4Kalpha expression is detected in the head and the pectoral fins
-
the expression of isoform PI5P4Kgamma increases when the cells grow to confluence and polarize
-
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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
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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
brenda
Itoh, T.; Ijuin, T.; Takenawa, T.
A novel phosphatidylinositol-5-phosphate 4-kinase (phosphatidylinositol-phosphate kinase IIgamma) is phosphorylated in the endoplasmic reticulum in response to mitogenic signals
J. Biol. Chem.
273
20292-20299
1998
Rattus norvegicus
brenda
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
brenda
Hinchliffe, K.A.; Irvine, R.F.
Regulation of type II PIP kinase by PKD phosphorylation
Cell. Signal.
18
1906-1913
2006
Sus scrofa
brenda
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
Mus musculus (Q91XU3), Homo sapiens (Q8TBX8)
brenda
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
Homo sapiens (P78356), Gallus gallus
brenda
Clarke, J.; Irvine, R.
The activity, evolution and association of phosphatidylinositol 5-phosphate 4-kinases
Adv. Biol. Regul.
52
40-45
2012
Mammalia
brenda
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
brenda
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
brenda
Huang, Z.; Anderson, R.E.; Cao, W.; Wiechmann, A.F.; Rajala, R.V.
Light-induced tyrosine phosphorylation of rod outer segment membrane proteins regulate the translocation, membrane binding and activation of type II alpha phosphatidylinositol-5-phosphate 4-kinase
Neurochem. Res.
36
627-635
2011
Mus musculus, Rattus norvegicus, Rattus norvegicus Sprague-Dawley
brenda
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
brenda
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
brenda
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)
brenda
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 (Q8TBX8), Homo sapiens (P78356), Homo sapiens (P48426), Homo sapiens
brenda
Clarke, J.H.; Giudici, M.L.; Burke, J.E.; Williams, R.L.; Maloney, D.J.; Marugan, J.; Irvine, R.F.
The function of phosphatidylinositol 5-phosphate 4-kinase gamma (PI5P4Kgamma) explored using a specific inhibitor that targets the PI5P-binding site
Biochem. J.
466
359-367
2015
Mus musculus
brenda
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
brenda
Boura, E.; Nencka, R.
Phosphatidylinositol 4-kinases: Function, structure, and inhibition
Exp. Cell Res.
337
136-145
2015
Homo sapiens
brenda
Elouarrat, D.; van der Velden, Y.U.; Jones, D.R.; Moolenaar, W.H.; Divecha, N.; Haramis, A.P.
Role of phosphatidylinositol 5-phosphate 4-kinase ? in zebrafish development
Int. J. Biochem. Cell Biol.
45
1293-1301
2013
Danio rerio
brenda
Xu, J.X.; Si, M.; Zhang, H.R.; Chen, X.J.; Zhang, X.D.; Wang, C.; Du, X.N.; Zhang, H.L.
Phosphoinositide kinases play key roles in norepinephrine- and angiotensin II-induced increase in phosphatidylinositol 4,5-bisphosphate and modulation of cardiac function
J. Biol. Chem.
289
6941-6948
2014
Rattus norvegicus
brenda
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
brenda
Tang, Y.; Zhao, C.Y.; Tan, S.T.; Xue, H.W.
Arabidopsis type II phosphatidylinositol 4-kinase PI4Kgamma5 regulates auxin biosynthesis and leaf margin development through interacting with membrane-bound transcription factor ANAC078
PLoS Genet.
12
e1006252
2016
Arabidopsis thaliana
brenda
Gupta, A.; Toscano, S.; Trivedi, D.; Jones, D.R.; Mathre, S.; Clarke, J.H.; Divecha, N.; Raghu, P.
Phosphatidylinositol 5-phosphate 4-kinase (PIP4K) regulates TOR signaling and cell growth during Drosophila development
Proc. Natl. Acad. Sci. USA
110
5963-5968
2013
Drosophila melanogaster
brenda
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
brenda
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
brenda
Droubi, A.; Bulley, S.; Clarke, J.; Irvine, R.
Nuclear localizations of phosphatidylinositol 5-phosphate 4-kinases alpha and beta are dynamic and independently regulated during starvation-induced stress
Biochem. J.
473
2155-2163
2016
Gallus gallus
brenda
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
brenda
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
brenda
Sharma, S.; Mathre, S.; Ramya, V.; Shinde, D.; Raghu, P.
Phosphatidylinositol 5 phosphate 4-kinase regulates plasma-membrane PIP3 turnover and insulin signaling
Cell Rep.
27
1979-1990
2019
Drosophila melanogaster
brenda
Kamalesh, K.; Trivedi, D.; Toscano, S.; Sharma, S.; Kolay, S.; Raghu, P.
Phosphatidylinositol 5-phosphate 4-kinase regulates early endosomal dynamics during clathrin-mediated endocytosis
J. Cell Sci.
130
2119-2133
2017
Drosophila melanogaster
brenda
Noch, E.K.; Yim, I.; Milner, T.A.; Cantley, L.C.
Distribution and localization of phosphatidylinositol 5-phosphate, 4-kinase alpha and beta in the brain
J. Comp. Neurol.
529
434-449
2020
Mus musculus
brenda
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
brenda
Davis, M.; Sasaki, A.; Simeonov, A.
Method for assaying the lipid kinase phosphatidylinositol-5-phosphate 4-kinase alpha in quantitative high-throughput screening (qHTS) bioluminescent format
Methods Mol. Biol.
1376
1-9
2016
Homo sapiens (P48426)
brenda
Lundquist, M.; Goncalves, M.; Loughran, R.; Possik, E.; Vijayaraghavan, T.; Yang, A.; Pauli, C.; Ravi, A.; Verma, A.; Yang, Z.; Johnson, J.; Wong, J.; Ma, Y.; Hwang, K.; Weinkove, D.; Divecha, N.; Asara, J.; Elemento, O.; Rubin, M.; Kimmelman, A.; Pause, A.
Phosphatidylinositol-5-phosphate 4-kinases regulate cellular lipid metabolism by facilitating autophagy
Mol. Cell.
70
531-544
2018
Mus musculus
brenda
Bulley, S.J.; Droubi, A.; Clarke, J.H.; Anderson, K.E.; Stephens, L.R.; Hawkins, P.T.; Irvine, R.F.
In B cells, phosphatidylinositol 5-phosphate 4-kinase-alpha synthesizes PI(4,5)P2 to impact mTORC2 and Akt signaling
Proc. Natl. Acad. Sci. USA
113
10571-10576
2016
Gallus gallus
brenda
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