Target
cAMP-dependent protein kinase catalytic subunit alpha
Ligand
BDBM2689
Substrate
histone (type H IIas)
Meas. Tech.
PKA assay
IC50
>10000±n/a nM
Citation
 Toullec, DPianetti, PCoste, HBellevergue, PGrand-Perret, TAjakane, MBaudet, VBoissin, PBoursier, ELoriolle, 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_RAT | PKA, catalytic subunit | Prkaca | cAMP-Dependent Protein Kinase (PKA) | cAMP-dependent protein kinase alpha-catalytic subunit
Type:
Enzyme catalytic subunit
Mol. Mass.:
40627.70
Organism:
Rattus norvegicus (rat)
Description:
The catalytic subunit of cAMP-dependent protein kinase (PKA) was used in the assay. It did not require cAMP for activity.
Residue:
351
Sequence:
MGNAAAAKKGSEQESVKEFLAKAKEDFLKKWEDPSQNTAQLDHFDRIKTLGTGSFGRVMLVKHKESGNHYAMKILDKQKVVKLKQIEHTLNEKRILQAVNFPFLVKLEFSFKDNSNLYMVMEYVPGGEMFSHLRRIGRFSEPHARFYAAQIVLTFEYLHSLDLIYRDLKPENLLIDQQGYIQVTDFGFAKRVKGRTWTLCGTPEYLAPEIILSKGYNKAVDWWALGVLIYEMAAGYPPFFADQPIQIYEKIVSGKVRFPSHFSSDLKDLLRNLLQVDLTKRFGNLKNGVNDIKNHKWFATTDWIAIYQRKVEAPFIPKFKGPGDTSNFDDYEEEEIRVSINEKCGKEFTEF
  
Inhibitor
Name:
BDBM2689
Synonyms:
3-[1-(3-dymethylaminopropyl)-indol-3-yl]-4-(indol-3-yl)-3-pyrrolin-2-one | 3-{1-[3-(dimethylamino)propyl]-1H-indol-3-yl}-4-(1H-indol-3-yl)-2,5-dihydro-1H-pyrrol-2-one | Bisindolyl deriv. 17
Type:
Small organic molecule
Emp. Form.:
C25H26N4O
Mol. Mass.:
398.5001
SMILES:
CN(C)CCCn1cc(C2=C(CNC2=O)c2c[nH]c3ccccc23)c2ccccc12 |t:9|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
histone (type H IIas)
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
13378.65
Organism:
n/a
Description:
20 uM [gamma-32P]ATP as co-substrate.
Residue:
124
Sequence:
MSGRGKGGKVKGKAKSRSNRAGLQFPVGRIHRLLRKGNYAERVGAGAPVYLAAVMEYLAAEVLELAGNAARDNKKTRIIPRHLQLAIRNDEELNKLLSGVTIAQGGVLPNIQAVLLPKKTEKKA