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2.7.1.127: inositol-trisphosphate 3-kinase

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

Word Map on EC 2.7.1.127

Reaction

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

Synonyms

1D-myo-inositol-trisphosphate 3-kinase, Arg82, ArgRIII, D-myo-inositol 1,4,5-trisphosphate 3-kinase, GsIP3K-A, HsIP3K-A, inositol (1,4,5) trisphosphate 3 kinase B, inositol (1,4,5) trisphosphate 3-kinase, inositol 1,4,5-trisphosphate 3-kinase, inositol 1,4,5-trisphosphate 3-kinase A, inositol 1,4,5-trisphosphate 3-kinase B, inositol 1,4,5-trisphosphate 3-kinase C, inositol 1,4,5-trisphosphate 3-kinases, inositol 1,4,5-trisphosphate kinase, inositol 1,4,5-trisphosphate kinase 2, inositol 1,4,5-trisphosphate-3-kinase-A, inositol polyphosphate multikinase, inositol trisphosphate 3-kinase B, inositol(1,4,5)P3 3-kinase, inositol(1,4,5)trisphosphate 3-kinase, inositol(1,4,5)trisphosphate 3-kinases, inositol-1,4,5-trisphosphate 3-kinase, inositol-1,4,5-trisphosphate 3-kinase A, inositol-1,4,5-trisphosphate 3-kinase-A, inositol-1,4,5-trisphosphate-3-kinase, inositol-1,4,5-trisphosphate-3-kinase A, inositol-1,4,5-trisphosphate-3-kinase-A, inositol-trisphosphate 3-kinase B, Ins(1,4,5)P(3) 3-kinase B, Ins(1,4,5)P3 3-kinase, Ins(1,4,5)P3 3-kinase isoform B, Ins(1,4,5)P3 kinase, InsP3 3-kinase, InsP3 3-kinase A, InsP3 3-kinase B, InsP3 3-kinase C, InsP3K, InsP3KB, InsP3Kinase, IP3 3-kinase, IP3 3-kinase 2, IP3-3K, IP3K, IP3K-A, IP3K-B, IP3K-C, IP3K1, IP3K2, IP3KA, IP3KB, IP3KC, IP3kin, Ipk2, IPMK, ITPKA, Itpkb, Itpkc, kinase (phosphorylating), inositol 1,4,5-trisphosphate 3-, More, RnIP3K-C, wavy

ECTree

     2 Transferases
         2.7 Transferring phosphorus-containing groups
             2.7.1 Phosphotransferases with an alcohol group as acceptor
                2.7.1.127 inositol-trisphosphate 3-kinase

Inhibitors

Inhibitors on EC 2.7.1.127 - inositol-trisphosphate 3-kinase

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(2'S)-1D-1,2-O-[(2'-phosphoryloxy)propane-1',3'-diyl]-myo-inositol 4,5-bisphosphate
-
synthetic bicyclic inositol trisphosphate S epimer, IC50 is 0.156 mM
1D-myo-inositol 1,3,4,5-tetrakisphosphate
1D-myo-inositol 1,4,5-trisphosphate
2,3-diphosphoglycerate
-
-
2-[3,5-dimethyl-1-(4-nitrophenyl)-1H-pyrazol-4-yl]-5,8-dinitro-1H-benzo[de]isoquinoline-1,3(2H)-dione
BIP-4, BIP-4 is competitive to Ins(1,4,5)P3 and shows high selectivity for the Ins(1,4,5)P3 binding pocket, BIP-4 does not block the actin bundling activity of ITPKA
-
3',4',7,8-tetrahydroxyflavone
7-methylsulfanyl-3-phenyl-[1,3,4]thiadiazolo[2,3-c][1,2,4]triazin-4-one
55% inhibition at 0.04 mM
aurintricarboxylic acid
chlorogenic acid
chlorpromazine
D-2-deoxyinositol 1,3,4,5-tetrakisphosphate
-
strong inhibition of isozyme A, IC50 is 0.0054 mM
D-2-deoxyinositol 1,4,5-trisphosphate
-
strong inhibition of isozyme A, IC50 is 0.0017 mM
D-3-deoxyinositol 1,4,6-trisphosphate
-
strong inhibition of isozyme A, IC50 is 0.0014 mM
D-6-deoxyinositol 1,3,4,5-tetrakisphosphate
-
strong inhibition of isozyme A, IC50 is 0.0051 mM
D-myo-inositol 1,4,5-trisphosphate
-
strong inhibition, purified recombinant enzyme, IC50 value is 0.003 mM in absence of Ca2+
D-myo-inositol 2,4,5-trisphosphate
-
IC50 is 0.117 mM
D-scyllo-inositol 1,2,3,4-tetrakisphosphate
-
purified recombinant enzyme, IC50 value is above 0.1 mM in absence of Ca2+
D-scyllo-inositol 1,2,4-trisphosphate
-
purified recombinant enzyme, IC50 value is 0.044 mM in absence of Ca2+
ellagic acid
epicatechin-3-gallate
epigallocatechin-3-gallate
F-actin
-
-
gossypol
heparin
-
mixed-type inhibition
hypericin
inositol phosphate
-
inhibitory effects of all possible 38 regioisomers of synthetic inositol phosphates, only inositol trisphosphates and tetrakisphosphates inhibit, not or very weak: inositol monophosphates, bisphosphates and pentakisphosphates, the recognition of myo-inositol phosphate regioisomers is highly structure-selective
KN-62
KN-93
L-scyllo-inositol 1,2,3,4-tetrakisphosphate
-
purified recombinant enzyme, IC50 value is above 0.1 mM in absence of Ca2+
L-scyllo-inositol 1,2,4-trisphosphate
-
purified recombinant enzyme, IC50 value is 0.006 mM in absence of Ca2+
myricetin
N-(1,2-benzoxazol-3-yl)-4-methylbenzamide
68% inhibition at 0.04 mM, mixed type inhibitor, that is nearly completely taken up by H1299 cells and remains stable after cellular uptake, the compound exhibits a robust stability and a high membrane permeability. The inhibitor provides the possibility to partly inhibit the metastasis-promoting effect of ITPKA in lung tumor cells. Inhibition mechanism of BAMB-4, overview
N-(4-ethoxyphenyl)pyrazolo[1,5-a]pyridine-3-carboxamide
87% inhibition at 0.04 mM
N-(6-Aminohexyl)-5-chloro-1-naphthalenesulfonamide
protein kinase A
-
isoforms A and B are differentially regulated via phosphorylation by the cAMP-dependent protein kinase, isoform A: stimulation in the presence or absence of Ca2+/calmodulin, isoform B: no effect on activity in the absence of Ca2+/calmodulin, 45% inhibition in the presence of Ca2+/calmodulin
-
Protein kinase C
-
quercetin
Rose bengal
RS-20
-
calmodulin antagonist, prevents the Ca2+/calmodulin-mediated activation
-
scyllo-inositol 1,2,3,5-tetrakisphosphate
-
weak inhibition, purified recombinant enzyme, IC50 value is 0.028 mM in absence of Ca2+
scyllo-inositol 1,2,3-trisphosphate
-
purified recombinant enzyme, IC50 value is 0.027 mM in absence of Ca2+
scyllo-inositol 1,2,4,5-tetrakisphosphate
-
weak inhibition, purified recombinant enzyme, IC50 value is 0.039 mM in absence of Ca2+
scyllo-inositol 1,3,5-trisphosphate
-
purified recombinant enzyme, IC50 value is 0.090 mM in absence of Ca2+
TSH
-
thyroid-stimulating hormone, inhibits at a physiological concentration, inhibition is mimicked by dibuturyl cyclic AMP and forskolin, mechanism
additional information
-