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Target
cAMP-dependent protein kinase catalytic subunit alpha
Ligand
BDBM6847
Substrate
Lysine-rich histone
Meas. Tech.
CDK Kinase Inhibition Assay
Temperature
298.15±n/a K
IC50
16600±n/a nM
Comments
extracted
Citation
 Engler, TA; Furness, K; Malhotra, S; Sanchez-Martinez, C; Shih, C; Xie, W; Zhu, G; Zhou, X; Conner, S; Faul, MM; Sullivan, KA; Kolis, SP; Brooks, HB; Patel, B; Schultz, RM; DeHahn, TB; Kirmani, K; Spencer, CD; Watkins, SA; Considine, EL; Dempsey, JA; Ogg, CA; Stamm, NB; Anderson, BD; Campbell, RM; Vasudevan, V; Lytle, ML Novel, potent and selective cyclin D1/CDK4 inhibitors: indolo[6,7-a]pyrrolo[3,4-c]carbazoles. Bioorg Med Chem Lett 13:2261-7 (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:
BDBM6847
Synonyms:
18-methyl-5-[3-(4-methylpiperazin-1-yl)propyl]-3,13,18-triazahexacyclo[14.7.0.0^{2,10}.0^{4,9}.0^{11,15}.0^{17,21}]tricosa-1(16),2(10),4(9),5,7,11(15),17(21),19,22-nonaene-12,14-dione | indolocarbazole deriv. 14g
Type:
Small organic molecule
Emp. Form.:
C29H29N5O2
Mol. Mass.:
479.5729
SMILES:
CN1CCN(CCCc2cccc3c2[nH]c2c3c3C(=O)NC(=O)c3c3c4n(C)ccc4ccc23)CC1
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