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Target
cAMP-dependent protein kinase catalytic subunit alpha
Ligand
BDBM6860
Substrate
Lysine-rich histone
Meas. Tech.
Kinase Inhibition Assay
Temperature
298.15±n/a K
IC50
>20000±n/a nM
Comments
extracted
Citation
 Zhu, G; Conner, SE; Zhou, X; Shih, C; Li, T; Anderson, BD; Brooks, HB; Campbell, RM; Considine, E; Dempsey, JA; Faul, MM; Ogg, C; Patel, B; Schultz, RM; Spencer, CD; Teicher, B; Watkins, SA Synthesis, structure-activity relationship, and biological studies of indolocarbazoles as potent cyclin D1-CDK4 inhibitors. J Med Chem 46:2027-30 (2003) [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:
BDBM6860
Synonyms:
6-bromo-3,13,23-triazahexacyclo[14.7.0.0^{2,10}.0^{4,9}.0^{11,15}.0^{17,22}]tricosa-1(16),2(10),4(9),5,7,11(15),17(22),18,20-nonaene-12,14-dione | Indolocarbazole deriv. 4(d)
Type:
Small Organic Molecule
Emp. Form.:
C20H10BrN3O2
Mol. Mass.:
404.216
SMILES:
Brc1ccc2c(c1)[nH]c1c3[nH]c4ccccc4c3c3C(=O)NC(=O)c3c21
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Lysine-rich histone
Synonyms:
ING Peptide | Lys-rich histone | histone type IIIS
Type:
Peptide
Mol. Mass.:
10508.21
Organism:
Bos taurus (bovine)
Description:
Purified as a lysine rich fraction of histone H1 from calf thymus.
Residue:
105
Sequence:
SETAPAAPAAAPPAEKTPVKKKAAKKPAGARRKASGPPVSELITKAVAASKERSGVSLAALKKALAAAGYDVEKNNSRIKLGLKSLVSKGTLVQTKGTGASGSFK