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2.7.1.153: phosphatidylinositol-4,5-bisphosphate 3-kinase

This is an abbreviated version!
For detailed information about phosphatidylinositol-4,5-bisphosphate 3-kinase, go to the full flat file.

Word Map on EC 2.7.1.153

Reaction

ATP
+
1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
=
ADP
+
1-phosphatidyl-1D-myo-inositol 3,4,5-trisphosphate

Synonyms

class I phosphoinositide 3-kinase, class I PI3K, class IA phosphatidylinositol 3-kinase, class IA phosphatidylinositol-4,5-bisphosphate 3-kinase, CXCR2/phosphatidylinositol 3-kinase gamma, kinase (phosphorylating), phosphatidylinositol 4,5-diphosphate 3-, More, p101-PI3K, p110alpha, p110beta, p110delta, p110delta PI 3-kinase, p110gamma/p101, P120-PI3K, phosphatidyl-inositol-3-kinase, phosphatidylinositol (4,5)-bisphosphate 3-hydroxykinase, phosphatidylinositol 3'-kinase, phosphatidylinositol 3-hydroxyl kinase, phosphatidylinositol 3-kinase alpha, phosphatidylinositol 3-kinase gamma, phosphatidylinositol-4,5-bisphosphate 3-kinase, phosphoinositide 3-kinase, phosphoinositide 3-kinase p110delta, phosphoinositol 3-kinase, PI 3-K, PI 3-kinase, PI-3K, PI3-K, PI3-kinase, PI3K, PI3K p110delta, PI3Kalpha, PI3Kbeta, PI3Kdelta, PI3Kgamma, PI3Kp110delta, PIK3, PIK3CA, Pik3r1, PtdIns(4,5)P2 3-OH kinase, PtdIns-3-kinase p101, PtdIns-3-kinase p110, PtdInsP 3-OH-kinase, type I phosphoinositide 3-kinase

ECTree

     2 Transferases
         2.7 Transferring phosphorus-containing groups
             2.7.1 Phosphotransferases with an alcohol group as acceptor
                2.7.1.153 phosphatidylinositol-4,5-bisphosphate 3-kinase

Inhibitors

Inhibitors on EC 2.7.1.153 - phosphatidylinositol-4,5-bisphosphate 3-kinase

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
1-[2-methyl-3-(trifluoromethyl)benzyl]-2-methyl-7-(morpholin-4-yl)-6,7-dihydroimidazo[1,2-a]pyrimidin-5(1H)-one
-
1-[2-methyl-3-(trifluoromethyl)benzyl]-7-(morpholin-4-yl)-6,7-dihydroimidazo[1,2-a]pyrimidin-5(1H)-one
-
1-[2-methyl-3-(trifluoromethyl)benzyl]-7-[(2R)-2-methylmorpholin-2-yl]-6,7-dihydroimidazo[1,2-a]pyrimidin-5(1H)-one
-
1-[4-[(4-methylpiperazin-1-yl)carbonyl]phenyl]-3-[4-[4-morpholin-4-yl-7-(2,2,2-trifluoroethyl)-7H-pyrrolo[2,3-d ]pyrimidin-2-yl]phenyl]urea
dual catalytic subunit alpha isoform/mTOR kinase inhibitor, demonstrates inhibition of tumor cell growth in vitro and in vivo and causes suppression of the pathway specific biomarkers in the human MDA-361 cell line
17-hydroxywortmannin
-
-
2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one
-
i.e. LY294002, treatment prevents interleukin-13-induced hyper-responsiveness
2-(6-aminopurin-9-ylmethyl)-5-methyl-3-O-tolyl-3H-quinazolin-4-one
-
i.e.IC87114, selective for isoform p110delta. Treatment prevents interleukin-13-induced hyper-responsiveness
2-(difluoromethyl)-1-[4,6-di-(4-morpholinyl)-1,3,5-triazin-2-yl]-1H-benzimidazole
lead compound for structure-activity study
2-(methylsulfanyl)-3-[2-methyl-3-(trifluoromethyl)benzyl]-5-(morpholin-4-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7(3H)-one
-
2-methyl-3-[2-methyl-3-(trifluoromethyl)benzyl]-5-(2methylmorpholin-4-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7(3H)-one
-
2-methyl-3-[2-methyl-3-(trifluoromethyl)benzyl]-5-(morpholin-4-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7(3H)-one
-
2-[(6-amino-9H-purin-9-yl)methyl]-5-methyl-3-(2-methylphenyl)-4(3H)-quinazolinone
-
i.e. IC87114, selectively inhibits isoform p110delta
3-(2-morpholino-6-(2-(pyridin-4-yl)ethylamino)pyrimidin-4-yl)phenol
-
3-(2-morpholino-6-(pyridin-2-ylmethoxy)pyrimidin-4-yl)phenol
-
3-(4-morpholino-6-(pyridin-2-yl)pyrimidin-2-yl)phenol
-
3-Methyladenine
3-phenyl-2-[(S)-1-(9H-purin-6-ylamino)-propyl]-3H-quinazolin-4-one
i.e. CAL-101, highly selective and small molecule inhibitor of isoform PI3Kdelta. Inhibitor blocks constitutive phosphatidylinositol-3-kinase signaling, resulting in decreased phosphorylation of Akt and other downstream effectors, an increase in poly(ADP-ribose) polymerase and caspase cleavage and an induction of apoptosis
3-[4-(4-morpholinyl)thieno(3,2-d)pyrimidin-2-yl]-phenol
-
a p110 PI3K isoform selective inhibitor
3-[4-(morpholin-4-yl)pyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl]phenol
among the compounds tested, treatment with 3-[4-(morpholin-4-yl)thieno[3,2-d]pyrimidin-2-yl]phenol or 3-[4-(morpholin-4-yl)pyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl]phenol leads to the most efficient inhibition
3-[4-(morpholin-4-yl)thieno[3,2-d]pyrimidin-2-yl]phenol
among the compounds tested, treatment with 3-[4-(morpholin-4-yl)thieno[3,2-d]pyrimidin-2-yl]phenol or 3-[4-(morpholin-4-yl)pyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl]phenol leads to the most efficient inhibition
4-(2-((6-methoxypyridin-3-yl)amino)-5-((4-(methylsulfonyl)piperazin-1-yl)methyl)pyridin-3-yl)-6-methyl-1,3,5-triazin-2-amine
not inhibitory to serine/threonine kinase mTOR; not inhibitory to serine/threonine kinase mTOR
4-[2-[(6-methoxypyridin-3-yl)amino]-5-phenylpyridin-3-yl]-6-methyl-1,3,5-triazin-2-amine
not inhibitory to serine/threonine kinase mTOR; not inhibitory to serine/threonine kinase mTOR
4-[4-(morpholin-4-yl)-5a,6-dihydro[1]benzofuro[3,2-d]pyrimidin-2-yl]phenol
4-[5-(3,6-dihydro-2H-pyran-4-yl)-2-[(6-methoxypyridin-3-yl)amino]pyridin-3-yl]-6-methyl-1,3,5-triazin-2-amine
not inhibitory to serine/threonine kinase mTOR; not inhibitory to serine/threonine kinase mTOR
5-[2,2-difluoro-benzo(1,3)-dioxol-5-ylmethylene]-thiazolidine-2,4-dione
-
a p110 PI3K isoform selective inhibitor
6-amino-2-(difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-4-methoxy-1H-benzimidazole
inhibitory against all three class Ia PI 3-kinase enzymes, i.e. p110alpha, p110beta, and p110delta, and also displays significant potency against two mutant forms of the p110alpha isoform, H1047R and E545K. In an in vivo U87MG human glioblastoma tumor xenograftmodel in Rag1-/- mice, and at a dose of 50mg/kg given by intraperitoneal injection it dramatically reduces cancer growth by 81% compared to untreated controls
7-methyl-2-(4-morpholinyl)-9-[1-(phenylamino)ethyl]-4H-pyrido[1,2-a]pyrimidin-4-one
-
i.e. TGX221, selectively inhibits isoform p110beta. Compound decreases secretion of vascular endothelial growth factor and interleukin-6 in nonasthmatic airway smooth muscle cells and lung fibroblasts
AS604850
PI3Kgamma inhibitor 2
AS605240
Baicalin
-
10 microM, 35.5% inhibition of isoform PI3Kalpha
BYL719
a p110alpha-specific inhibitor, BYL719 fails to display selective growth inhibition in p110alphahigh cells
-
CAL-101
-
a specific inhibitor of the PI3Kdelta isoform
CapG
-
nuclear actin-regulatory protein
-
GSK2636771
a p110beta-specific inhibitor
-
HS173
a p110alpha-specific inhibitor
-
IC-87114
IC87114
idelalisib
luteolin
-
1 microM, 75.8% inhibition of isoform PI3Kalpha
Ly-294002
-
LY294002
MLN1117
a p110alpha-specific inhibitor
-
myricetin
-
1 microM, almost complete inhibition of isoform PI3Kalpha
N-[(E)-(6-bromoimidazo[1,2-a]pyridin-3-yl)methylidene]-N,2-dimethyl-5-nitrobenzenesulfonohydrazide
-
i.e.PIK75, selectively inhibits isoform p110alpha. In cells stimulated with transforming growth factor-beta and/or 10% fetal bovine serum, compound attenuates transforming growth factor-induced fibronectin deposition in all cell types tested and decreases secretion of vascular endothelial growth factor and interleukin-6 in nonasthmatic airway smooth muscle cells and lung fibroblasts. Compound decreases cell survival in transforming growth factor-stimulated asthmatic, but not nonasthmatic, airway smooth muscle cells
N-[2-(dimethylamino)ethyl]-N-methyl-4-[([4-[4-morpholin-4-yl-7-(2,2,2-trifluoroethyl)-7H-pyrrolo[2,3-d ]pyrimidin-2-yl]phenyl]carbamoyl)amino]benzamide
dual catalytic subunit alpha isoform/mTOR kinase inhibitor, demonstrates inhibition of tumor cell growth in vitro and in vivo and causes suppression of the pathway specific biomarkers in the human MDA-361 cell line. Good in vivo efficacy in the MDA361 human breast tumor xenograft model
PI-103
PI103
-
suppressing phosphatidylinositol 3-kinase activity by inhibitors LY294002 and PI103 selectively reduces both the mRNA and protein levels of peroxisome proliferator-activated receptor gamma coactivator PGC-1beta but not PGC-1alpha. Reducing PGC-1b expression also leads to reduced mRNA expression levels of uncoupling protein 1, 2 and superoxide dismutase 2. Correspondingly, mitochondrial membrane potential and reactive oxygen species levels are increased
PIK-75
PIK75
p110alpha inhibitor PIK75 shows a strong cytotoxicity to all glioblastoma cell lines tested
PX-866
quercetagetin
-
1 microM, almost complete inhibition of isoform PI3Kalpha
quercetin
TGX-221
TGX-221-R
R-enantiomer of inhibitor TGX-221, 100fold more potent as a PI3K-beta inhibitor than the S-enantiomer
WAY-266175
-
-
-
WAY-266176
-
-
Wortmannin
XL147
YM024
a p110alpha-selective PI3K inhibitor
-
ZSTK474
-
a phosphatidylinositol 3-kinase inhibitor, inhibited phosphorylation of Ser65, Thr70 and Thr37/46 in 4E-BP1 by PI3K. Identification of the ZSTK474-sensitive phosphoproteins in A-549 cells, overview
[(4-[2-[(3-hydroxyphenyl)amino]-1H-benzimidazol-1-yl]-1,3,5-triazin-2-yl)amino]acetonitrile
lead compound for structure-based design of inhibitors, dual inhibitor of phosphatidylinositol 3-kinase and serine/threonine kinase mTOR; lead compound for structure-based design of inhibitors, dual inhibitor of phosphatidylinositol 3-kinase and serine/threonine kinase mTOR
[3-[4-morpholin-4-yl-7-(pyrrolidin-1-ylmethyl)-5H-pyrrolo-[3,2-d ]pyrimidin-2-yl]phenyl]methanol
selective for catalytic subunit alpha isoform
additional information
-