Reaction Details
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cAMP-dependent protein kinase catalytic subunit alpha
Ligand
BDBM11820
Substrate
Peptide Substrate
Meas. Tech.
Fluorescence Polarization-based Assay
pH
7.2±n/a
Temperature
295.15±n/a K
IC50
1900±1000 nM
Citation
Breitenlechner, CB; Friebe, WG; Brunet, E; Werner, G; Graul, K; Thomas, U; Kunkele, KP; Schafer, W; Gassel, M; Bossemeyer, D; Huber, R; Engh, RA; Masjost, B Design and crystal structures of protein kinase B-selective inhibitors in complex with protein kinase A and mutants. J Med Chem 48:163-70 (2005) [PubMed] Article Target
Name:
cAMP-dependent protein kinase catalytic subunit alpha
Synonyms:
KAPCA_BOVIN | PKA C-alpha | PKC | PRKACA | Protein Kinase C | Protein Kinase C, bovine brain | cAMP-Dependent Protein Kinase (PKA) | cAMP-dependent Protein Kinase, bovine heart | cAMP-dependent protein kinase A | cAMP-dependent protein kinase alpha-catalytic subunit | cAMP-dependent protein kinase, alpha-catalytic subunit
Type:
Enzyme Complex
Mol. Mass.:
40627.77
Organism:
Bos taurus (bovine)
Description:
The PKA holoenzyme purified from bovine heart, exists as an inactive tetrameric complex, which consists of a regulatory dimer associated with two catalytic subunits. It requires cAMP to activate the enzymatic reaction.
Residue:
351
Sequence:
MGNAAAAKKGSEQESVKEFLAKAKEDFLKKWENPAQNTAHLDQFERIKTLGTGSFGRVMLVKHMETGNHYAMKILDKQKVVKLKQIEHTLNEKRILQAVNFPFLVKLEFSFKDNSNLYMVMEYVPGGEMFSHLRRIGRFSEPHARFYAAQIVLTFEYLHSLDLIYRDLKPENLLIDQQGYIQVTDFGFAKRVKGRTWTLCGTPEYLAPEIILSKGYNKAVDWWALGVLIYEMAAGYPPFFADQPIQIYEKIVSGKVRFPSHFSSDLKDLLRNLLQVDLTKRFGNLKNGVNDIKNHKWFATTDWIAIYQRKVEAPFIPKFKGPGDTSNFDDYEEEEIRVSINEKCGKEFSEF
Inhibitor
Name:
BDBM11820
Synonyms:
(3R,4R)-N-(4-{4-[5-(3,3-dimethylpiperidin-1-yl)-2-hydroxybenzoyl]benzoylamino}azepan-3-yl)isonicotinamide hydrochloride | N-[(3R,4R)-4-[(4-{[5-(3,3-dimethylpiperidin-1-yl)-2-hydroxyphenyl]carbonyl}benzene)amido]azepan-3-yl]pyridine-4-carboxamide hydrochloride | Protein Kinase B-Selective Inhibitor 4
Type:
Small organic molecule
Emp. Form.:
C33H39N5O4
Mol. Mass.:
569.6939
SMILES:
CC1(C)CCCN(C1)c1ccc(O)c(c1)C(=O)c1ccc(cc1)C(=O)N[C@@H]1CCCNC[C@H]1NC(=O)c1ccncc1 |r|
Structure:
Substrate
Name:
Peptide Substrate
Synonyms:
biotinylated tridecapeptide substrate
Type:
Peptide
Mol. Mass.:
1564.86
Organism:
n/a
Description:
n/a
Residue:
13
Sequence:
RFARKGSLRQKNV