Reaction Details Report a problem with these data
Target
cAMP-dependent protein kinase catalytic subunit alpha
Ligand
BDBM2711
Substrate
histone (type Vs)
Meas. Tech.
PKA assay
IC50
3200±n/a nM
Citation
 Bit, RA; Davis, PD; Elliott, LH; Harris, W; Hill, CH; Keech, E; Kumar, H; Lawton, G; Maw, A; Nixon, JS Inhibitors of protein kinase C. 3. Potent and highly selective bisindolylmaleimides by conformational restriction. J Med Chem 36:21-9 (1993) [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:
BDBM2711
Synonyms:
3-(1,2,3,4-Tetrahydropyrazino[1,2-a]indol-10-yl)-4-(1-methyl-3-indolyl)-1H-pyrrole-2,5-dione | 3-(1-methyl-1H-indol-3-yl)-4-{1H,2H,3H,4H-pyrazino[1,2-a]indol-10-yl}-2,5-dihydro-1H-pyrrole-2,5-dione | Bisindolylmaleimide deriv. 17 | ROCHE screening, 63
Type:
Small organic molecule
Emp. Form.:
C24H20N4O2
Mol. Mass.:
396.4412
SMILES:
Cn1cc(C2=C(C(=O)NC2=O)c2c3CNCCn3c3ccccc23)c2ccccc12 |t:4|
Structure:
Search PDB for entries with ligand similarity:
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