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2.7.4.21: inositol-hexakisphosphate 5-kinase

This is an abbreviated version!
For detailed information about inositol-hexakisphosphate 5-kinase, go to the full flat file.

Word Map on EC 2.7.4.21

Reaction

ATP
+
1D-myo-inositol 1-diphosphate 2,3,4,5,6-pentakisphosphate
=
ADP
 +
1D-myo-inositol 1,5-bis(diphosphate) 2,3,4,6-tetrakisphosphate

Synonyms

AtIPK2alpha, AtIpk2beta, ATP:1D-myo-inositol-hexakisphosphate phosphotransferase, AtVip1, AtVip2, diphosphoinositol pentakisphosphate kinase 2, diphosphoinositol pentakisphosphate synthetase, EC 2.7.1.152, EhIP6KA, IHPK2, inositol hexakisphosphate 5-kinase, inositol hexakisphosphate kinase, inositol hexakisphosphate kinase 1, inositol hexakisphosphate kinase 2, inositol hexakisphosphate kinase 3, inositol hexakisphosphate kinase type 2, inositol hexakisphosphate kinase-1, inositol hexakisphosphate kinase-2, inositol hexakisphosphate kinase-3, inositol polyphosphate kinase, inositol-hexakisphosphate kinase, InsP6 kinase, InsP6-kinase, InsP6K1, InsP6K2, InsP6K3, IP6 kinase, IP6 kinase 1, IP6K, IP6K1, IP6K2, IP6K3, Ipk2, IPMK, Kcs1, kinase (phosphorylating), inositol hexakisphosphate, More, Pi uptake stimulator, PiUS, PPIP5K1, PPIP5K2, RID-2

ECTree

     2 Transferases
         2.7 Transferring phosphorus-containing groups
             2.7.4 Phosphotransferases with a phosphate group as acceptor
                2.7.4.21 inositol-hexakisphosphate 5-kinase

Inhibitors

Inhibitors on EC 2.7.4.21 - inositol-hexakisphosphate 5-kinase

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
1,3,4,5,6-inositol pentakisphosphate
-
IC50 for inositol hexakisphosphate kinase activity is 0.022 mM, IC50 for ATP synthase activity is 0.0128 mM
2,5-O-benzyl-myo-inositol 1,3,4,6-tetrakisphosphate
activates the ATP hydrolysis activity and inhibits the PPIP5K2 activity and InsP6 kinase activity, and the 1,5-[PP]2-InsP4 dephosphorylation activity of the enzyme. The compound can inhibit inositol phosphate kinase activity without occupying the catalytic site
2-O-benzyl-5-O-alpha-phosphonoacetyl-myo-inositol 1,3,4,6-tetrakisphosphate
stimulates ATP hydrolysis 9fold, but inhibits 1,5-[PP]2-InsP4 dephosphorylation activity of the enzyme. The compound can inhibit inositol phosphate kinase activity without occupying the catalytic site
2-O-benzyl-5-O-diphosphate-myo-inositol 1,3,4,6-tetrakisphosphate
activates ATP hydrolysis activity but inhibits 1,5-[PP]2-InsP4 dephosphorylation activity of the enzyme
2-O-benzyl-myo-inositol 1,2,3,4,6-pentakisphosphate
activates ATP hydrolysis activity but inhibits 1,5-[PP]2-InsP4 dephosphorylation activity of the enzyme
5-O-alpha-diphosphate-myo-inositol 1,3,4,6-tetrakisphosphate
activates ATP hydrolysis activity but inhibits 1,5-[PP]2-InsP4 dephosphorylation activity of the enzyme
5-O-alpha-phosphonoacetyl-myo-inositol 1,2,3,4,6-pentakisphosphate
stimulates ATP hydrolysis 5fold, but inhibits 1,5-[PP]2-InsP4 dephosphorylation activity of the enzyme
6-hydroxy-DL-DOPA
-
C8-PtdIns(4,5)P2
0.05 mM, inhibits 1D-myo-inositol 1,5-bis(diphosphate) 2,3,4,6-tetrakisphosphate dephosphorylation by approximately 60%
-
diphosphoinositol pentakisphosphate
-
IC50 for inositol hexakisphosphate kinase activity is 0.0066 mM, IC50 for ATP synthase activity is 0.0018 mM
EDTA
-
-
H2O2
-
H2O2 as low as 0.1 mM dramatically reduces enzymatic activity
heat shock protein Hsp90
-
binding of HSP90 inhibits IP6K2 catalytic activity, IP6K2 binds to HSP90's C terminus. Depletion of HSP90 by RNAi in HEK-293 cells increases IP6K catalytic activity about 2.5fold, specificity of IP6K2-HSP90 interaction, overview. Drugs and selective mutations that abolish HSP90–IP6K2 binding elicit activation of IP6K2, leading to cell death. Overexpression of HSP90 markedly and specifically reduces IP6K catalytic activity in HEK-293 cells, overexpression of HSP90 does not influence catalytic activity of IP6K1
-
inositol 1,2,4,5,6-pentakisphosphate
-
IC50 for inositol hexakisphosphate kinase activity is 0.022 mM
Inositol 1,3,4,5-tetrakisphosphate
-
IC50 for inositol hexakisphosphate kinase activity is 0.061 mM, IC50 for ATP synthase activity is 0.0325 mM
Inositol 1,4,5-trisphosphate
-
IC50 for ATP synthase activity is 0.253 mM
Inositol hexakisphosphate
-
IC50 for inositol hexakisphosphate kinase activity is 0.0008 mM, IC50 for ATP synthase activity is 0.0018 mM
myricetin
-
N(2)-(m-(trifluoromethyl)benzyl) N(6)-(p-nitrobenzyl)purine
N2-(3-(trifluoromethyl)benzyl)-N6-(4-nitrobenzyl)purine
-
-
N2-(3-trifluorobenzyl)-N6-(4-nitrobenzyl)purine
N2-(m-(trifluoromethy)lbenzyl)N6-(p-nitrobenzyl)purine
potent and selective inhibitor
N2-(m-(trifluoromethyl) benzyl) N6-(p-nitrobenzyl) purine
TNP, a selective inhibitor, abolishes the basal and Cx43-potentiated Runx2 activity in response to FGF2 treatment relative to DMSO treated controls
N2-(m-trifluorobenzyl),N6-(p-nitrobenzyl)purine
-
phosphate
1D-myo-inositol 5-diphosphate 1,2,3,4,6-pentakisphosphate phosphatase activities of PPIP5Ks are 40-90% inhibited by phosphate within the 0-1 mM range; 1D-myo-inositol 5-diphosphate 1,2,3,4,6-pentakisphosphate phosphatase activities of PPIP5Ks are 40-90% inhibited by phosphate within the 0-1 mM range
additional information
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