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Literature summary extracted from

  • Valtcheva, N.; Nestorov, P.; Beck, A.; Russwurm, M.; Hillenbrand, M.; Weinmeister, P.; Feil, R.
    The commonly used cGMP-dependent protein kinase type I (cGKI) inhibitor Rp-8-Br-PET-cGMPS can activate cGKI in vitro and in intact cells (2009), J. Biol. Chem., 284, 556-562.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
2.7.11.12 cGMP
-
 Mus musculus
2.7.11.12 cGMP
-
 Bos taurus

Application

EC Number Application Comment Organism
2.7.11.12 additional information data obtained with Rp-8-Br-PET-cGMPS as cGKI inhibitor should be interpreted with caution and not be used as sole evidence to dissect the role of cGKI in signaling processes Mus musculus
2.7.11.12 additional information data obtained with Rp-8-Br-PET-cGMPS as cGKI inhibitor should be interpreted with caution and not be used as sole evidence to dissect the role of cGKI in signaling processes Bos taurus

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.7.11.12 cGKIalpha and cGKIbeta are cloned for expression in Sf9 insect cells Bos taurus

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.11.12 KT5823
-
 Bos taurus
2.7.11.12 KT5823
-
 Mus musculus
2.7.11.12 Rp-8-Br-PET-cGMPS beta-phenyl-1,N2-etheno-8-bromoguanosine-3',5'-cyclic monophosphorothioate Bos taurus
2.7.11.12 Rp-8-Br-PET-cGMPS beta-phenyl-1,N2-etheno-8-bromoguanosine-3',5'-cyclic monophosphorothioate Mus musculus

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.11.12 ATP + a protein Mus musculus
-
 ADP + a phosphoprotein
-
 ?
2.7.11.12 ATP + a protein Bos taurus
-
 ADP + a phosphoprotein
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.11.12 Bos taurus
-
-
-
2.7.11.12 Mus musculus
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.7.11.12 by affinity chromatography Bos taurus

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.7.11.12 aorta
-
 Mus musculus
-
2.7.11.12 vascular smooth muscle cell VSMC Mus musculus
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.11.12 ATP + a protein
-
 Mus musculus ADP + a phosphoprotein
-
 ?
2.7.11.12 ATP + a protein
-
 Bos taurus ADP + a phosphoprotein
-
 ?
2.7.11.12 ATP + GRTGRRNSI-amide assay substrate Bos taurus ADP + phosphorylated GRTGRRNSI-amide
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.7.11.12 cGKI isoforms alpha and beta Mus musculus
2.7.11.12 cGKI isoforms alpha and beta Bos taurus
2.7.11.12 cGMP-dependent protein kinase type I
-
 Mus musculus
2.7.11.12 cGMP-dependent protein kinase type I
-
 Bos taurus

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.7.11.12 30
-
 activity assay Bos taurus

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.7.11.12 0.00003
-
 Rp-8-Br-PET-cGMPS cGKI alpha Bos taurus
2.7.11.12 0.00005
-
 Rp-8-Br-PET-cGMPS cGKI beta Bos taurus