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Target
cAMP-dependent protein kinase catalytic subunit alpha
Ligand
BDBM2579
Substrate
Kemptide
Meas. Tech.
Kinase Activity Assay
pH
6.8±n/a
Temperature
298.15±n/a K
IC50
<45±n/a nM
Km
12000±n/a nM
Citation
 Bonn, S; Herrero, S; Breitenlechner, CB; Erlbruch, A; Lehmann, W; Engh, RA; Gassel, M; Bossemeyer, D Structural analysis of protein kinase A mutants with Rho-kinase inhibitor specificity. J Biol Chem 281:24818-30 (2006) [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:
BDBM2579
Synonyms:
(2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.1^{2,6}.0^{7,28}.0^{8,13}.0^{15,19}.0^{20,27}.0^{21,26}]nonacosa-8(13),9,11,14(28),15(19),20(27),21(26),22,24-nonaen-16-one | CHEMBL388978 | Staurosporin, 4 | Staurosporine | Staurosporine, 8 | US20240002365, Compound staurosporine | US9206188, Staurosporine | US9226923, Staurosporine
Type:
Small organic molecule
Emp. Form.:
C28H26N4O3
Mol. Mass.:
466.531
SMILES:
CN[C@@H]1C[C@H]2O[C@@](C)([C@@H]1OC)n1c3ccccc3c3c4CNC(=O)c4c4c5ccccc5n2c4c13 |r|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Kemptide
Synonyms:
Aurora Peptide Substrate
Type:
Peptide
Mol. Mass.:
773.92
Organism:
n/a
Description:
50 uM ATP as co-substrate.
Residue:
7
Sequence:
LRRASLG