Reaction Details
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cAMP-dependent protein kinase catalytic subunit alpha
Ligand
BDBM2583
Substrate
histone (type H IIas)
Meas. Tech.
PKA assay
pH
7±n/a
Temperature
303.15±n/a K
IC50
2000±600 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_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:
BDBM2583
Synonyms:
3,4-Bis(3-indolyl)-1H-pyrrole-2,5-dione | 3,4-bis(1H-indol-3-yl)-2,5-dihydro-1H-pyrrole-2,5-dione | BIM-4 | Bisindolyl deriv. 3 | Bisindolylmaleimide deriv. 5 | CHEMBL266487 | bis-indolylmaleimide deriv. 8a
Type:
Small organic molecule
Emp. Form.:
C20H13N3O2
Mol. Mass.:
327.3361
SMILES:
O=C1NC(=O)C(=C1c1c[nH]c2ccccc12)c1c[nH]c2ccccc12 |c:5|
Structure:
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