Reaction Details
Report a problem with these data
Report a problem with these dataTarget
cAMP-dependent protein kinase catalytic subunit alpha
Ligand
BDBM2583
Substrate
histone (type Vs)
Meas. Tech.
PKA assay
pH
8.5±n/a
Temperature
310.15±n/a K
IC50
11800±3600 nM
Citation
Davis, PD; Hill, CH; Lawton, G; Nixon, JS; Wilkinson, SE; Hurst, SA; Keech, E; Turner, SE Inhibitors of protein kinase C. 1. 2,3-Bisarylmaleimides. J Med Chem 35:177-84 (1992) [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:
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 Vs)
Synonyms:
n/a
Type:
Other Protein Type
Mol. Mass.:
358.43
Organism:
n/a
Description:
11 uM [gamma-32P]ATP as co-substrate.
Residue:
3
Sequence:
NA