Target
cAMP-dependent protein kinase catalytic subunit alpha
Ligand
BDBM2684
Substrate
histone (type H IIas)
Meas. Tech.
PKA assay
IC50
500±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:
BDBM2684
Synonyms:
3-[3-(dimethylamino)propyl]-3,13,23-triazahexacyclo[14.7.0.0^{2,10}.0^{4,9}.0^{11,15}.0^{17,22}]tricosa-1(16),2(10),4(9),5,7,11(15),17(22),18,20-nonaene-12,14-dione | Bisindolyl deriv. 16 | indolocarbazole deriv. 4f
Type:
Small organic molecule
Emp. Form.:
C25H22N4O2
Mol. Mass.:
410.4678
SMILES:
CN(C)CCCn1c2ccccc2c2c3C(=O)NC(=O)c3c3c4ccccc4[nH]c3c12
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