Reaction Details
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cAMP-dependent protein kinase catalytic subunit alpha
Ligand
BDBM3185
Substrate
Histone type HL
Meas. Tech.
PKA assay
IC50
>50000±n/a nM
Citation
Defauw, JM; Murphy, MM; Jagdmann, GE; Hu, H; Lampe, JW; Hollinshead, SP; Mitchell, TJ; Crane, HM; Heerding, JM; Mendoza, JS; Davis, JE; Darges, JW; Hubbard, FR; Hall, SE Synthesis and protein kinase C inhibitory activities of acyclic balanol analogs that are highly selective for protein kinase C over protein kinase A. J Med Chem 39:5215-27 (1996) [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:
BDBM3185
Synonyms:
(+-)-2-[[2,6-Dihydroxy-4-[[[3-(4-hydroxyphenyl)-2-[(phenylsulfonyl)amino]propyl]oxy]carbonyl]phenyl]carbonyl]-3-hydroxybenzoic Acid | 2-[(4-{[2-benzenesulfonamido-3-(4-hydroxyphenyl)propoxy]carbonyl}-2,6-dihydroxyphenyl)carbonyl]-3-hydroxybenzoic acid | Acyclic Balanol Analog 6b
Type:
Small organic molecule
Emp. Form.:
C30H25NO11S
Mol. Mass.:
607.585
SMILES:
OC(=O)c1cccc(O)c1C(=O)c1c(O)cc(cc1O)C(=O)OCC(Cc1ccc(O)cc1)NS(=O)(=O)c1ccccc1
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