Reaction Details
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cAMP-dependent protein kinase catalytic subunit alpha
Ligand
BDBM3225
Substrate
Histone type HL
Meas. Tech.
PKA assay
IC50
470±n/a nM
Citation
Lampe, JW; Biggers, CK; Defauw, JM; Foglesong, RJ; Hall, SE; Heerding, JM; Hollinshead, SP; Hu, H; Hughes, PF; Jagdmann, GE; Johnson, MG; Lai, YS; Lowden, CT; Lynch, MP; Mendoza, JS; Murphy, MM; Wilson, JW; Ballas, LM; Carter, K; Darges, JW; Davis, JE; Hubbard, FR; Stamper, ML Synthesis and protein kinase inhibitory activity of balanol analogues with modified benzophenone subunits. J Med Chem 45:2624-43 (2002) [PubMed] Article More Info.:
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:
BDBM3225
Synonyms:
2-{[2,6-dihydroxy-4-({[(3R,4R)-3-[(4-hydroxybenzene)amido]azepan-4-yl]oxy}carbonyl)phenyl]methyl}-3-hydroxybenzoic acid | Modified Benzophenone Carbonyl, Balanol Analog 25 | trans-4-[4-(2-Carboxy-6-hydroxybenzyl)-3,5-dihydroxybenzoyloxy]-3-(4-hydroxybenzamido)azepine
Type:
Small organic molecule
Emp. Form.:
C28H28N2O9
Mol. Mass.:
536.5299
SMILES:
OC(=O)c1cccc(O)c1Cc1c(O)cc(cc1O)C(=O)O[C@@H]1CCCNC[C@H]1NC(=O)c1ccc(O)cc1 |r|
Structure:
Substrate
Name:
Histone type HL
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
358.43
Organism:
n/a
Description:
unfractionated histone (Worthington)
30 uM [gamma-32P]ATP as co-substrate.
Residue:
3
Sequence:
NA