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2.7.1.137: phosphatidylinositol 3-kinase

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

Word Map on EC 2.7.1.137

Reaction

ATP
+
1-phosphatidyl-1D-myo-inositol
=
ADP
 +
1-phosphatidyl-1D-myo-inositol 3-phosphate

Synonyms

class 3 phosphatidylinositol 3-kinase vacuolar protein sorting 34, class I phosphoinositide 3-kinase, class III phosphatidylinositol 3-kinase, class III phosphoinositide 3-kinase, class III PI3K, HsC2-PI3K, hVps34, hVps34 PI 3-kinase, kinase (phosphorylating), phosphatidylinositol 3-, kinase, phosphatidylinositol 3- (phosphorylating), lipid kinase Vps34, mammalian vacuolar protein sorting 34 homologue, More, p110a, p110delta I PI3K., p110g-related PI 3-kinase, p85/p110 phosphoinositide 3-kinase, p85/p110 type phosphatidylinositol kinase, p85a phosphoinositide 3-kinase, phosphatidyl-inositol-3-kinase, phosphatidylinositide 3-kinase, phosphatidylinositide 3-kinase C2alpha, phosphatidylinositol 3 kinase, phosphatidylinositol 3'-kinase, phosphatidylinositol 3-kinase, phosphoinositide 3'-kinase, phosphoinositide 3-kinase, phosphoinositide 3-kinase Dp110, phosphoinositide 3-kinase gamma, phosphoinositide-3-kinase, PI 3-K, PI 3-kinase, PI-3-K, PI-3K, PI3 K, PI3 kinase, PI3-K, PI3-K-related protein MEC1, PI3-kinase, PI3K, PI3K type III, PI3Kalpha, PI3Kbeta, PI3Kgamma, PI3K_59F, PI3K_68D, PIK3, PIK3C3, protein sorting mutant 34 protein, PtdIns 3'-kinase, PtdIns 3-kinase, PtdIns 3-kinase vacuolar protein sorting 34, receptor-linked phosphatidylinositol 3-kinase, Rickettsia intracellular secreted kinase-1, Risk1, RT0135, TcVps34, type III phosphatidylinositol 3-kinase, vacuolar protein sorting 34, VPS34, Vps34p

ECTree

     2 Transferases
         2.7 Transferring phosphorus-containing groups
             2.7.1 Phosphotransferases with an alcohol group as acceptor
                2.7.1.137 phosphatidylinositol 3-kinase

Inhibitors

Inhibitors on EC 2.7.1.137 - phosphatidylinositol 3-kinase

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(+/-)-2-[hydroxy[tetrahydro-2-(octadecyloxy)methylfuran-2-yl]methoxyl]phosphinyloxy-N,N,N-trimethylethaniminium hydroxide
(1E,4S,4aR,5R,6aS,7S)-5-(acetyloxy)-1-[[[3-(dimethylamino)-propyl](methyl)amino]methylene]-11-hydroxy-4-(methoxymethyl)-4a,6a-dimethyl-2,10-dioxo-1,2,4,4a,5,6,6a,7,8,9,9a,10-dodecahydroindeno[4,5-h]isochromen-7-yl-(1R,2R,4S)-4-[(2R)-2-[(3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34aS)-9,27-dihydroxy-10,21-dimethoxy-6,8,12,14,20,26-hexamethyl-1,5,11,28,29-pentaoxo-1,4,5,6,9,10,11,12,13,14,21,22,23,24,25,26,27,28,29,31,32,33,34,34a-tetracosahydro-3H-23,27-epoxypyrido[2,1-c][1,4]oxazacyclohentriacontin-3-yl]propyl]-2-methoxycyclohexyl octanedioate
-
-
(1E,4S,4aR,5R,6aS,7S)-5-(acetyloxy)-1-{[[3-(dimethylamino)propyl](methyl)amino]methylene}-11-hydroxy-4-(methoxymethyl)-4a,6a-dimethyl-2,10-dioxo-1,2,4,4a,5,6,6a,7,8,9,9a,10-dodecahydroindeno[4,5-h]isochromen-7-yl-(1R,2R,4S)-4-{(2R)-2-[(3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34aS)-9,27-dihydroxy-10,21-dimethoxy-6,8,12,14,20,26-hexamethyl-1,5,11,28,29-pentaoxo-1,4,5,6,9,10,11,12,13,14,21,22,23,24,25,26,27,28,29,31,32,33,34,34a-tetracosahydro-3H-23,27-epoxypyrido[2,1-c][1,4]oxazacyclohentriacontin-3-yl]propyl}-2-methoxycyclohexyl octanedioate
-
-
(1E,4S,4aR,5R,6aS,7S,9aR)-1-({[3-(dimethylamino)propyl](methyl)amino}methylidene)-7,11-dihydroxy-4-(methoxymethyl)-4a,6a,9a-trimethyl-2,10-dioxo-1,2,4,4a,5,6,6a,7,8,9,9a,10-dodecahydroindeno[4,5-h]isochromen-5-yl acetate
-
-
(1Z,4S,4aR,6aS,9aR)-1-([[3-(dimethylamino)propyl](methyl)amino]methylidene)-5-ethoxy-7,11-dihydroxy-4-(methoxymethyl)-4a,6a-dimethyl-4a,5,6,6a,7,8,9,9a-octahydroindeno[4,5-h]isochromene-2,10(1H,4H)-dione
-
-
(3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34aS)-9,27-dihydroxy-3-[(2R)-1-[(1S,3R)-4-hydroxy-3-methoxycyclohexyl]propan-2-yl]-10,21-dimethoxy-6,8,12,14,20,26-hexamethyl-9,10,12,13,14,21,22,23,24,25,26,27,32,33,34,34a-hexadecahydro-3H-23,27-epoxypyrido[2,1-c][1,4]oxazacyclohentriacontine-1,5,11,28,29(4H,6H,31H)-pentone
-
-
(3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34aS)-9,27-dihydroxy-3-{(2R)-1-[(1S,3R)-3-hydroxycyclohexyl]propan-2-yl}-10,21-dimethoxy-6,8,12,14,20,26-hexamethyl-9,10,12,13,14,21,22,23,24,25,26,27,32,33,34,34a-hexadecahydro-3H-23,27-epoxypyrido[2,1-c][1,4]oxazacyclohentriacontine-1,5,11,28,29(4H,6H,31H)-pentone
-
-
(8S)-2-[(3R)-3-methylmorpholin-4-yl]-9-(3-methyl-2-oxobutyl)-8-(trifluoromethyl)-6,7,8,9-tetrahydro-4H-pyrimido[1,2-a]pyrimidin-4-one
-
1-((3-(4-octylphenyl)-1,2,4-oxadiazol-5-yl)methyl)guanidine
i.e. idelalisib
1-([2-[(2-chloropyridin-4-yl)amino]-4'-(cyclopropylmethyl)[4,5'-bipyrimidin]-2'-yl]amino)-2-methylpropan-2-ol
Vpsn34-IN1
1-O-octadecyl-2-O-methyl-rac-3-glycerophospho-myo-inositol
1-O-octadecyl-2-O-methyl-rac-glycero-3-phosphocholine
17-hydroxywortmannin
2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one
2-morpholin-4-yl-3-phenylchromen-4-one
-
weak inhibition, IC50 is above 0.2 mM for the recombinant wild-type enzyme and for the recombinant mutant C838V/I848A
2-morpholin-4-yl-3-propylchromen-4-one
-
IC50 is 0.0031 mM for the recombinant wild-type enzyme and 0.068 mM for the recombinant mutant C838V/I848A
3-benzyl-2-morpholin-4-yl-chromen-4-one
-
weak inhibition, IC50 is above 0.2 mM for the recombinant wild-type enzyme and for the recombinant mutant C838V/I848A
3-butyl-2-morpholin-4-yl-chromen-4-one
-
IC50 is 0.025 mM for the recombinant wild-type enzyme and 0.048 mM for the recombinant mutant C838V/I848A
3-ethyl-2-morpholin-4-yl-chromen-4-one
-
IC50 is 0.028 mM for the recombinant wild-type enzyme and 0.0044 mM for the recombinant mutant C838V/I848A
3-isopropyl-2-morpholin-4-yl-chromen-4-one
-
IC50 is 0.051 mM for the recombinant wild-type enzyme and more than 0.2 mM for the recombinant mutant C838V/I848A
3-methyl-2-morpholin-4-yl-chromen-4-one
-
IC50 is 0.033 mM for the recombinant wild-type enzyme and 0.040 mM for the recombinant mutant C838V/I848A
3-Methyladenine
5'-p-fluorosulfonylbenzoyladenosine
-
-
adenosine
-
above 0.1 mM
ADP
-
above 0.1 mM
AMP
-
above 0.1 mM
apocynin
-
specific PI3K inhibitor, restores vasorelaxation and hyperpolarization in response to an ATP-sensitive K+ channel opener levcromakalim
Ca2+
-
0.1 mM, 60% inhibition, in presence of 10 mM MgCl2
cardiolipin
Dodecyl sucrose
-
-
Ead125
-
-
EDTA
-
-
ethanol
-
dose-dependent inhibition of insulin receptor substrate-1-associated PI3K activity in skeletal muscle, but not in adipose tissue, ethanol-induced diabetic rats
GDC-0941
Gö6976
inhibitor directly targets phosphatidylinositol 3-kinase and confers profound inhibition of autophagic flux by inhibiting the formation of autophagosomes. It does not inhibit the cell survival promoting class I phosphoinositide 3-kinase-Akt signaling at the concentrations required for effective autophagy inhibition
hexadecylphosphocholine
IC87114
-
-
isoquercetin
-
PI 3-kinase I and PI 3-kinase II; strong inhibition of PI 3-kinase I and II, noncompetitive, apparent Ki value: 4 mM for PI 3-kinase I and 2.5 mM for PI 3-kinase II
KU55933
inhibitor directly targets phosphatidylinositol 3-kinase and confers profound inhibition of autophagic flux by inhibiting the formation of autophagosomes. Inhibits wild-type activity in vitro almost as efficiently as LY294002. It does not inhibit the cell survival promoting class I phosphoinositide 3-kinase-Akt signaling at the concentrations required for effective autophagy inhibition
LY 294002
-
-
Ly-294002
-
-
LY292223
-
i.e. 2-morpholin-4-yl-chromen-4-one, IC50 is 0.0026 mM for the recombinant wild-type enzyme and 0.025 mM for the recombinant mutant C838V/I848A
LY294002
LY301497
LY303511
-
the inhibitor potently, reversibly blocks voltage-dependent K+ channel currents via a direct mechanism, IC50 is 0.065 mM
lysophosphatidic acid
-
-
Mg2+
-
inhibition above 2.5 mM, activation below
naloxone
-
-
noggin
-
-
-
Nonidet P40
NVP-BEZ235
octylglucoside
-
-
palmitate
-
-
peptide N24
-
a peptide inhibitor derived from p55PIK phosphatidylinositol 3-kinase, N24, regulatory subunit acts as inhibitor in cancer therapy, it blocks cell proliferation and induces cell cycle arrest in all cancer cell lines tested. Modeling of mechanisms of Rb-dependent and Rb-independent cell cycle arrest by N24 peptide, overview
-
phosphatidic acid
-
-
phosphatidylcholine
PI3Kalpha inhibitor IV
-
-
-
PI3Kbeta inhibitor VI
-
i.e. TGX-221
-
PI3Kgamma inhibitor
-
-
-
PIK-III
-
-
proteinase K
proteinase K treatment of partially purified Rickettsia typhi results in a dose-dependent degradation of Risk1 on the bacterial membrane
-
PWT-458
PX-866
quercetin
sodium cholate
-
-
sodium deoxycholate
-
-
staurosporine
-
-
TGFbeta
-
significantly inhibits phosphorylation of both p85 and ERK1/2 in vivo. TGFbeta does not activate the ERK pathway but turns off the GM-CSF-induced ERK signal via inhibition of the PI3-kinase-Akt pathway in human leukemia cells, overview
-
Tiron
-
specific PI3K inhibitor, restores vasorelaxation and hyperpolarization in response to an ATP-sensitive K+ channel opener levcromakalim
Triton X-100
-
-
Vps34-IN-1
-
-
Wortmannin
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
additional information
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