Information on EC 2.7.11.12 - cGMP-dependent protein kinase

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The enzyme appears in viruses and cellular organisms

EC NUMBER
COMMENTARY hide
2.7.11.12
-
RECOMMENDED NAME
GeneOntology No.
cGMP-dependent protein kinase
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
ATP + a protein = ADP + a phosphoprotein
show the reaction diagram
-
-
-
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phospho group transfer
SYSTEMATIC NAME
IUBMB Comments
ATP:protein phosphotransferase (cGMP-dependent)
CGMP is required to activate this enzyme. The enzyme occurs as a dimer in higher eukaryotes. The C-terminal region of each polypeptide chain contains the catalytic domain that includes the ATP and protein substrate binding sites. This domain catalyses the phosphorylation by ATP to specific serine or threonine residues in protein substrates [3]. The enzyme also has two allosteric cGMP-binding sites (sites A and B). Binding of cGMP causes a conformational change that is associated with activation of the kinase [4].
CAS REGISTRY NUMBER
COMMENTARY hide
141588-27-4
-
141588-27-4
cGMP-dependent protein kinase
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
gene amfor
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
C57BL/6
-
-
Manually annotated by BRENDA team
PKG-Ialpha and PKG-Ibeta
-
-
Manually annotated by BRENDA team
-
-
-
Manually annotated by BRENDA team
-
-
-
Manually annotated by BRENDA team
Liberian isolate
UniProt
Manually annotated by BRENDA team
-
-
-
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
evolution
malfunction
metabolism
physiological function
additional information
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
ATP + a peptide
ADP + a phosphorylated peptide
show the reaction diagram
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
ATP + a protein
ADP + phosphorylated protein
show the reaction diagram
ATP + Akt
ADP + phosphorylated Akt
show the reaction diagram
ATP + Arg-Lys-Arg-Ser-Arg-Ala-Glu
ADP + Arg-Lys-Arg-O-phospho-Ser-Arg-Ala-Glu
show the reaction diagram
-
i.e. Glasstide, a commercial peptide substrate
-
-
?
ATP + BAD protein
ADP + BAD phosphoprotein
show the reaction diagram
-
phosphorylation on Ser155 by PKG I
-
-
?
ATP + big potassium channel BKCa
ADP + phosphorylated big potassium channel BKCa
show the reaction diagram
ATP + BKCa channel protein
ADP + BKCa channel phosphoprotein
show the reaction diagram
ATP + BPDEtide
ADP + phosphorylated BPDEtide
show the reaction diagram
-
-
-
-
?
ATP + CFTR
ADP + phosphorylated CFTR
show the reaction diagram
ATP + CREb protein
ADP + phosphorylated CREb protein
show the reaction diagram
-
-
-
-
?
ATP + cysteine-riche protein 2
ADP + phosphorylated vasodilator-stimulated phosphoprotein
show the reaction diagram
ATP + DAPK2 protein
ADP + DAPK2 phosphoprotein
show the reaction diagram
ATP + EKRKRTYETF
ADP + phosphorylated EKRKRTYETF
show the reaction diagram
-
p65-derived synthetic peptide substrate
-
-
?
ATP + FoxO1a
ADP + phosphorylated FoxO1a
show the reaction diagram
ATP + GKKRKRSRKES
ADP + GKKRKRS(P)RKES
show the reaction diagram
-
i.e. MCPD-4, a commercial peptide substrate
-
-
?
ATP + GluA1 protein
ADP + GluA1 phosphoprotein
show the reaction diagram
ATP + glycogen synthase kinase-3
ADP + phosphorylated glycogen synthase kinase 3
show the reaction diagram
-
phosphorylation at Ser9 by PKGI and PKGII inhibiting the glycogen synthase kinase-3 inducing dephosphorylation of C/EBPbeta, i.e. the CCAAT enhancer-binding protein beta, important in regulation of gene expression during cell proliferation, differentiation, and apoptosis
-
-
?
ATP + glycogen synthase kinase-3beta
ADP + phosphorylated glycogen synthase kinase-3beta
show the reaction diagram
-
-
-
-
?
ATP + glycogen synthase kinase3
ADP + phosphorylated glycogen synthase kinase 3
show the reaction diagram
-
phosphorylation at Ser9 by PKGI and PKGII inhibiting the glycogen synthase kinase-3, substrate phosphorylation site mapping
-
-
?
ATP + GRTGRRNSI
ADP + phosphorylated GRTGRRNSI
show the reaction diagram
-
i.e. PKI, a commercial peptide substrate
-
-
?
ATP + GRTGRRNSI-amide
ADP + phosporylated GRTGRRNSI-amide
show the reaction diagram
-
assay substrate
-
-
?
ATP + HER2 protein
ADP + phosphorylated HER2 protein
show the reaction diagram
-
phosphorylation at threonine 686
-
-
?
ATP + histone
ADP + phosphorylated histone
show the reaction diagram
-
DG1
-
-
?
ATP + histone H2B
ADP + phosphorylated histone H2B
show the reaction diagram
-
-
-
-
?
ATP + human serotonin transporter
ADP + phosphorylated human serotonin transporter
show the reaction diagram
ATP + inositol 1,4,5-trisphosphate receptor-I
ADP + phosphorylated inositol 1,4,5-trisphosphate receptor-I
show the reaction diagram
ATP + IRAG
ADP + phosphorylated IRAG
show the reaction diagram
ATP + Kemptide
ADP + Kemptide phosphate
show the reaction diagram
ATP + Kemptide
ADP + phosphorylated Kemptide
show the reaction diagram
ATP + Maxi-K channel
ADP + phosphorylated Maxi-K channel
show the reaction diagram
-
-
-
-
?
ATP + maxiK channel
ADP + phosphorylated maxiK channel
show the reaction diagram
ATP + MQLRRPSDRE
ADP + phosphorylated MQLRRPSDRE
show the reaction diagram
-
p65-derived synthetic peptide substrate
-
-
?
ATP + myosin phosphatase
ADP + phosphorylated RhoA
show the reaction diagram
ATP + Na+/K+ ATPase
ADP + phosphorylated Na+/K+ ATPase
show the reaction diagram
ATP + NF-kappaB
ADP + phosphorylated NF-kappaB
show the reaction diagram
ATP + p21-activated kinase
ADP + phosphorylated p21-activated kinase
show the reaction diagram
ATP + p65
ADP + phosphorylated p65
show the reaction diagram
-
activity with recombinant wild-type p65 and mutants T305A and S276A
-
-
?
ATP + peptide W15
ADP + phosphorylated peptide W15
show the reaction diagram
-
peptide substrate sequence TQAKRKKSLAMA
-
-
?
ATP + phosphodiesterase 5
ADP + phosphorylated phosphodiesterase 5
show the reaction diagram
ATP + phospholamban
ADP + phosphorylated phospholamban
show the reaction diagram
ATP + phospholipase Cbeta3
ADP + phosphorylated phospholipase Cbeta3
show the reaction diagram
ATP + protein
ADP + phosphoprotein
show the reaction diagram
ATP + Rab11 protein
ADP + phosphorylated Rab11 protein
show the reaction diagram
-
-
-
-
?
ATP + Rac1
ADP + phosphorylated Rac-1
show the reaction diagram
ATP + Rho
ADP + phosphorylated rho
show the reaction diagram
ATP + RhoA
ADP + phosphorylated RhoA
show the reaction diagram
ATP + RKISASEFDRPL
ADP + phosphorylated RKISASEFDRPL
show the reaction diagram
-
BPDEtide, substrate in activity assay
-
-
?
ATP + RKISASEFDRPLR
ADP + phosphorylated RKISASEFDRPLR
show the reaction diagram
-
-
-
-
?
ATP + RKRSRAE
ADP + RKRS(P)RAE
show the reaction diagram
ATP + septin 3
ADP + phosphorylated septin 3
show the reaction diagram
ATP + septin 3 peptide 86-98
ADP + phosphorylated septin 3 peptide 86-98
show the reaction diagram
-
-
-
-
?
ATP + steroidogenic acute regulatory protein
ADP + phosphorylated steroidogenic acute regulatory protein
show the reaction diagram
-
i.e. StAR, recombinant GST-tagged substrate expressed in HEK-293 cells, phosphorylation in vitro at Ser55, Ser56, and Ser99
-
-
?
ATP + target membrane SNARe complex
ADP + phosphorylated target membrane SNARe complex
show the reaction diagram
-
the enzyme is involved in regulation of degranulation of leukocytes by phosphorylation of target membrane SNARe complex together with the phosphoinositide 3-kinase
-
-
?
ATP + TPIalpha
ADP + phosphorylated TPIalpha
show the reaction diagram
ATP + TQAKRKKSLAMA
ADP + phosphorylated TQAKRKKSLAMA
show the reaction diagram
-
substrate in activity assay
-
-
?
ATP + transient receptor potential channel 6
ADP + phosphorylated transient receptor potential channel 6
show the reaction diagram
ATP + TRAP protein
ADP + phosphorylated TRAP protein
show the reaction diagram
-
-
-
-
?
ATP + TRIM39
ADP + phosphorylated TRIM39
show the reaction diagram
ATP + TRIM39R
ADP + phosphorylated TRIM39R
show the reaction diagram
ATP + troponin T
ADP + phosphorylated troponin T
show the reaction diagram
ATP + TRPC3
ADP + phosphorylated TRPC3
show the reaction diagram
ATP + vasodilator stimulated phosphoprotein
ADP + phosphorylated vasodilator stimulated phosphoprotein
show the reaction diagram
ATP + vasodilator-stimulated phosphoprotein
ADP + phosphorylated vasodilator-stimulated phosphoprotein
show the reaction diagram
ATP + VASP
ADP + VAS(P)P
show the reaction diagram
-
-
-
-
?
ATP + VASP protein
ADP + phosphorylated VASP protein
show the reaction diagram
additional information
?
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
ATP + a protein
ADP + phosphorylated protein
show the reaction diagram
ATP + Akt
ADP + phosphorylated Akt
show the reaction diagram
-
-
-
-
?
ATP + BAD protein
ADP + BAD phosphoprotein
show the reaction diagram
-
phosphorylation on Ser155 by PKG I
-
-
?
ATP + big potassium channel BKCa
ADP + phosphorylated big potassium channel BKCa
show the reaction diagram
ATP + CFTR
ADP + phosphorylated CFTR
show the reaction diagram
-
phosphorylation leads to stimulation of chloride channels
-
-
?
ATP + CREb protein
ADP + phosphorylated CREb protein
show the reaction diagram
-
-
-
-
?
ATP + cysteine-riche protein 2
ADP + phosphorylated vasodilator-stimulated phosphoprotein
show the reaction diagram
ATP + DAPK2 protein
ADP + DAPK2 phosphoprotein
show the reaction diagram
-
i.e death-associated protein kinase 2, phosphorylation at Ser299, Ser367 and Ser368 type I cGMP-dependent protein kinase
-
-
?
ATP + FoxO1a
ADP + phosphorylated FoxO1a
show the reaction diagram
-
interaction of enzyme with FocO1a is involved in regulation of myoblast cell fusion during myogenesis
-
-
?
ATP + GluA1 protein
ADP + GluA1 phosphoprotein
show the reaction diagram
ATP + glycogen synthase kinase-3
ADP + phosphorylated glycogen synthase kinase 3
show the reaction diagram
-
phosphorylation at Ser9 by PKGI and PKGII inhibiting the glycogen synthase kinase-3 inducing dephosphorylation of C/EBPbeta, i.e. the CCAAT enhancer-binding protein beta, important in regulation of gene expression during cell proliferation, differentiation, and apoptosis
-
-
?
ATP + HER2 protein
ADP + phosphorylated HER2 protein
show the reaction diagram
-
phosphorylation at threonine 686
-
-
?
ATP + human serotonin transporter
ADP + phosphorylated human serotonin transporter
show the reaction diagram
-
i.e. hSERT, the naturally occuring hSERT mutant I425V is associated with obsessive-compulsive disorder and other neuropsychiatric disorders
-
-
?
ATP + inositol 1,4,5-trisphosphate receptor-I
ADP + phosphorylated inositol 1,4,5-trisphosphate receptor-I
show the reaction diagram
-
the phosphorylation of the receptor inhibits inositol 1,4,5-trisphosphate-induced Ca2+ release
-
-
?
ATP + IRAG
ADP + phosphorylated IRAG
show the reaction diagram
ATP + Kemptide
ADP + Kemptide phosphate
show the reaction diagram
-
-
-
-
?
ATP + maxiK channel
ADP + phosphorylated maxiK channel
show the reaction diagram
-
phosphorylation by isoyzme cGKI enhances the channel activity
-
-
?
ATP + myosin phosphatase
ADP + phosphorylated RhoA
show the reaction diagram
-
phosphorylation by isoyzme cGKIalpha leads to decreased level of phosphorylated MLC
-
-
?
ATP + Na+/K+ ATPase
ADP + phosphorylated Na+/K+ ATPase
show the reaction diagram
-
the enzyme has a positive regulatory function on the ion pump activity induced by No and glutamate via increased cGMP, overview
-
-
?
ATP + p21-activated kinase
ADP + phosphorylated p21-activated kinase
show the reaction diagram
-
PKG phosphorylation of p21-activated kinase, i.e. Pak, regulates HeLa cell and human umbilical vein endothelial cell morphology and cellular remodeling, time course of Pak1 activation in vivo, overview, PKG stimulates association of vasodilator-stimulated phosphoprotein VASP with Pak
-
-
?
ATP + phosphodiesterase 5
ADP + phosphorylated phosphodiesterase 5
show the reaction diagram
-
phosphorylation at Ser92 by isoyzme cGKI leads to enhanced hydrolysis of cGMP, regulatory function
-
-
?
ATP + phospholamban
ADP + phosphorylated phospholamban
show the reaction diagram
ATP + phospholipase Cbeta3
ADP + phosphorylated phospholipase Cbeta3
show the reaction diagram
-
potentially involved in inhibition of phospholipase C activity
-
-
?
ATP + Rab11 protein
ADP + phosphorylated Rab11 protein
show the reaction diagram
-
-
-
-
?
ATP + Rac1
ADP + phosphorylated Rac-1
show the reaction diagram
-
the enzyme activates the recombinant Myc-tagged small GTPase Rac1 in HEK-293 cells leading to activation of PAK1, the enzyme induces phosphorylation of p38 which activates MAPK, regulation, overview
-
-
?
ATP + Rho
ADP + phosphorylated rho
show the reaction diagram
ATP + RhoA
ADP + phosphorylated RhoA
show the reaction diagram
-
phosphorylation at Ser188 by isoyzme cGKI leading to translocation of RhoA from the membrane to the cytosol and inactivates RhoA
-
-
?
ATP + septin 3
ADP + phosphorylated septin 3
show the reaction diagram
-
potentially involved in vesicle trafficking
-
-
?
ATP + target membrane SNARe complex
ADP + phosphorylated target membrane SNARe complex
show the reaction diagram
-
the enzyme is involved in regulation of degranulation of leukocytes by phosphorylation of target membrane SNARe complex together with the phosphoinositide 3-kinase
-
-
?
ATP + TPIalpha
ADP + phosphorylated TPIalpha
show the reaction diagram
-
involved in desensitization of TPIalpha signalling
-
-
?
ATP + TRAP protein
ADP + phosphorylated TRAP protein
show the reaction diagram
-
-
-
-
?
ATP + TRIM39
ADP + phosphorylated TRIM39
show the reaction diagram
-
-
-
-
?
ATP + TRIM39R
ADP + phosphorylated TRIM39R
show the reaction diagram
-
PKGI interacts with TRIM39R, a Rpp21 domain-containing TRIM protein, in the kinase phosphorylation domain
-
-
?
ATP + troponin T
ADP + phosphorylated troponin T
show the reaction diagram
-
phosphorylation by isoyzme cGKI in cardiomyocytes
-
-
?
ATP + TRPC3
ADP + phosphorylated TRPC3
show the reaction diagram
-
involved in inhibition of store operated Ca2+ influx
-
-
?
ATP + vasodilator stimulated phosphoprotein
ADP + phosphorylated vasodilator stimulated phosphoprotein
show the reaction diagram
ATP + vasodilator-stimulated phosphoprotein
ADP + phosphorylated vasodilator-stimulated phosphoprotein
show the reaction diagram
ATP + VASP protein
ADP + phosphorylated VASP protein
show the reaction diagram
-
-
-
-
?
additional information
?
-
COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
8-bromo-cAMP
-
50% activation at 0.00062 mM
8-Bromo-cGMP
-
50% activation at 0.00004 mM
cIMP
-
50% activation at 0.0053 mM
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(9S,10R,12R)-2,3,9,10,11,12-hexahydro-10-methoxy-2,9-dimethyl-1-oxo-9,12-epoxy-1H-diindolo [1,2,3-fg:',2',1'-kl]pyrrolo [3,4-i][1,6]benzodiazocine-10-carboxylic acid methyl ester
-
KT-5823, specific PKG inhibitor
(Z)-1-(N-(2-aminoethyl)-N-(2-ammonioethyl)amino)diazen-1-ium-1,2-diolate
-
24 h exposure to 1 mM (Z)-1-(N-(2-aminoethyl)-N-(2-ammonioethyl)amino)diazen-1-ium-1,2-diolate leads to both reduction in cGKI expression and specific activity
1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
-
-
2,2'-(hydroxynitrosohydrazono)-bis-ethanamine
-
24 h incubation with 2,2'-(hydroxynitrosohydrazono)-bis-ethanamine after incubation with cGMP is associated with decreased PKG activity
4-methoxy-3,6-diphenylcyclohexa-3,5-diene-1,2-dione
4-[2-(4-fluorophenyl)-5-(1-methylpiperidin-4-yl)-1H-pyrrol-3-yl]pyridine
4-[2-(4-fluorophenyl)-5-(1-methylpiperidine-4-yl)-1H-pyrrol-3-yl]pyridine
4-[2-(fluorophenyl)-5-(1-methylpiperidine-4-yl)-1H pyrrol-3-yl] pyridine
-
highly specific ATP-competitive inhibitor of PKG
4-[2-(fluorophenyl)-5-(1-methylpiperidine-4-yl)-1H-pyrrol-3-yl]pyridine
-
4-[7-[(dimethylamino)methyl]-2-(4-fluorophenyl)imidazo[1,2-a]pyridine-3-yl]pyrimidin-2-amine
-
-
6'-methoxy-1,1':4',1''-terphenyl-2,2',5'-triol
6'-methoxy-1,1':4',1''-terphenyl-2,2',5,5'-tetrol
6-anilino-5,8-quinolinedione
-
-
7-nitroindazole
-
-
8-(4-chlorophenylthio)guanosine 3',5'-cyclic monophosphate
-
-
8-(4-chlorophenylthio)guanosine 3',5'-cyclic monophosphorothioate Rp-isomer
-
-
8-Bromo-cGMP
-
-
all-D-YGRKKRRQRRRPPLRKKKKKH
angiotensin
-
causes a decrease in expression of isozyme cGKIalpha, and an increase in expression of isozyme cGKIbeta
beta-phenyl-1,N2-etheno-8-bromoguanosine-3',5'-cyclic monophosphorothioate
-
-
D-glucose
-
high levels reduce enzyme activity in vivo leading to increased thrombospondin 1-dependent activation of transforming growth factor-beta, and increased TGF-beta-dependent expression of fibronectin and collagene type IV
DT-2 peptide
KT-5823
KT5823
KT5926
LRKKKKKH
-
-
N-[2-(methylamino)ethyl]-5-isoquinolinesulfonamide
-
-
nitroglycerine
-
24 h incubation with nitroglycerine after incubation with cGMP is associated with decreased PKG activity, PKG mRNA and protein are downregulated by a 24 h incubation with nitroglycerine at 0.01 mM but not at 0.0001 mM
pyrrole 4-[2-(4-fluorophenyl)-5-(1-methylpiperidine-4-yl)-1H pyrrol-3-yl] pyridine
-
inhibits native and recombinant enzyme, shows antiparasitic activity being active against Plasmodium falciparum blood cell stages cultured in vitro, IC50 for the native enzyme is 8.35 nM, and for the recombinant FLAG-tagged enzyme 3.48 nM
regulatory subunit of photoreceptor cGMP phosphodiesterase
-
inhibits PKGIalpha, the N-terminal 61 amino acids are important containing a cationic region
-
retro-inverso-all-D-YGRKKRRQRRRPPLRKKKKKH
Rp-8-Br-cGMP
-
in vivo inhibition in leukemia cells causes reduced agonist-stimulated beta-hexosaminidase release and abolishes vesicular fusion with the plasma membrane
Rp-8-Br-pCPT-cGMPS
Rp-8-Br-PET-cGMPS
Rp-8-bromo-PET-cGMPS
-
-
Rp-8-p-CPT-cGMP
-
i.e. Rp-8-(4-chlorophenylthio)guanosine 3',5'-cyclic monophosphate
Rp-8-pCPT-cGMP
Rp-8-pCPT-cGMPS
Rp-8-pCTP-cGMPS
-
selective for PKG
Rp-pCPT-cGMPS
staurosporine
terferol
TQAKRKKALAMA-NH2
-
-
TTYDFIASGRTGRRNAIHD-NH2
-
-
-
YGRKKRRQRRRPP
-
-
YGRKKRRQRRRPPLRKKKKKH
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
20 kDa heat shock protein
-
i.e. Hsp20, involved in cGKI-induced smooth muscle relaxation, probably via the actin binding sequence
-
8(4chlorophenylthio)guanosine3',5'cyclic monophosphate
-
-
-
8bromocGMP
-
-
-
8pCPTcGMP
-
-
-
8-(4-chlorophenylthio)guanosine 3',5'-cyclic monophosphate
-
-
8-APT-cGMP
-
cGKIalpha-selective activator
8-Br-cGMP
8-Br-PET-cGMP
8-Bromo-cGMP
8-bromo-cyclic GMP
-
-
8-NBD-cGMP
i.e. 8-[[2-[(7-nitro-4-benzofurazanyl)amino]ethyl]thio]guanosine-3',5'-cyclic monophosphate, poor, non-cooperative binding
8-pCPT-CGMP
8-pCPT-GMP
-
-
adenosine
-
adenosine-induced vasodilation in cerebral microvessesls involves cGMP and cGMP-dependent protein kinase
angiotensin
-
causes an increase in expression of isozyme cGKIbeta, and a decrease in expression of isozyme cGKIalpha
atrial natriuretic peptide
-
0.00001-0.01 mM
-
Bay412272
calcium/calmodulin-dependent kinase II
-
mediates NO-elicited PKG activation
-
cAMP
-
crossactivation at high levels in vivo
cgs-21680
-
-
dibutyryl-cGMP
-
0.001-0.1 mM
formyl-methionyl-leucyl-phenylalanine
-
-
forskolin
-
crossactivation at high levels above 0.001 mM in vivo
FoxO1a
-
directly activates enzyme expression binding to DNA in skeletal muscle
-
isoproterenol
-
crossactivation at high levels above 0.001 mM in vivo
lipopolysaccharides
-
induces enzyme expression and activates the enzyme
-
N2,2'-O-dibutyryl-cGMP
-
a membrane-permeable cGMP analogue, activates cGKI
nitric oxide
PET-cGMP
sodium nitroprusside
Sp-8-pCPT-cGMPS
-
cyclic guanosine monophosphate-dependent protein kinase activator, selective for PKG
Vasoactive intestinal peptide
-
i.e. VIP
additional information
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0104 - 0.0139
ATP
0.062
GRTGRRNSI
-
pH 7.4, 37°C, recombinant FLAG-tagged enzyme
0.00024
hSERT
-
-
-
0.00026
hSERT I425V
-
-
-
0.00019
hSERT T276A
-
-
-
0.00012
hSERT T276A/I425V
-
-
-
0.00011
hSERT T276D
-
-
-
0.00008
hSERT T276D/I425V
-
-
-
0.00013
hSERT T276E
-
-
-
0.0263 - 0.0313
RKRSRAE
0.0865
septin 3 peptide 86-98
-
pH 7.4, 30°C, PKG-I
-
additional information
additional information
-
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0000005 - 0.0000008
all-D-YGRKKRRQRRRPPLRKKKKKH
0.23
KT5823
-
cGKIalpha
0.00082
LRKKKKKH
-
-
0.0000028 - 0.0000055
retro-inverso-all-D-YGRKKRRQRRRPPLRKKKKKH
0.23 - 0.5
Rp-8-Br-pCPT-cGMPS
0.00003 - 0.9
Rp-8-Br-PET-cGMPS
0.0075
TQAKRKKALAMA-NH2
-
-
0.15
TTYDFIASGRTGRRNAIHD-NH2
-
-
-
0.0011
YGRKKRRQRRRPP
-
-
0.0000125 - 0.0000139
YGRKKRRQRRRPPLRKKKKKH
additional information
additional information
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0009
4-methoxy-3,6-diphenylcyclohexa-3,5-diene-1,2-dione
Eimeria tenella
-
-
0.000001 - 0.00021
4-[2-(4-fluorophenyl)-5-(1-methylpiperidin-4-yl)-1H-pyrrol-3-yl]pyridine
0.00000155 - 0.0178
4-[2-(fluorophenyl)-5-(1-methylpiperidine-4-yl)-1H pyrrol-3-yl] pyridine
0.000001
4-[2-(fluorophenyl)-5-(1-methylpiperidine-4-yl)-1H-pyrrol-3-yl]pyridine
Eimeria tenella
Q8MMZ8
inhibitor of apicomplexan parasite enzyme, IC50 is 1 nM for the enzyme of Eimeria tenella, mechanism
-
0.0052 - 0.0104
6'-methoxy-1,1':4',1''-terphenyl-2,2',5'-triol
0.0058 - 0.0095
6'-methoxy-1,1':4',1''-terphenyl-2,2',5,5'-tetrol
0.000012
all-D-YGRKKRRQRRRPPLRKKKKKH
Homo sapiens
-
-