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Target
cAMP-dependent protein kinase catalytic subunit alpha
Ligand
BDBM2687
Substrate
Lysine-rich histone
Meas. Tech.
PKC assay
IC50
200±n/a nM
Citation
 Toullec, D; Pianetti, P; Coste, H; Bellevergue, P; Grand-Perret, T; Ajakane, M; Baudet, V; Boissin, P; Boursier, E; Loriolle, F The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C. J Biol Chem 266:15771-81 (1991) [PubMed] 
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:
BDBM2687
Synonyms:
Bisindolyl deriv. 13 | methyl 3-{3-[4-(1H-indol-3-yl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]-1H-indol-1-yl}propanoate
Type:
Small organic molecule
Emp. Form.:
C24H19N3O4
Mol. Mass.:
413.4254
SMILES:
COC(=O)CCn1cc(C2=C(C(=O)NC2=O)c2c[nH]c3ccccc23)c2ccccc12 |t:9|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Lysine-rich histone
Synonyms:
ING Peptide | Lys-rich histone | histone type IIIS
Type:
Peptide
Mol. Mass.:
10508.21
Organism:
Bos taurus (bovine)
Description:
Purified as a lysine rich fraction of histone H1 from calf thymus.
Residue:
105
Sequence:
SETAPAAPAAAPPAEKTPVKKKAAKKPAGARRKASGPPVSELITKAVAASKERSGVSLAALKKALAAAGYDVEKNNSRIKLGLKSLVSKGTLVQTKGTGASGSFK