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Target
Protein kinase C alpha type
Ligand
BDBM3189
Substrate
Lysine-rich histone
Meas. Tech.
PKC assay
IC50
3200±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 
Target
Name:
Protein kinase C alpha type
Synonyms:
KPCA_HUMAN | PKC alpha | PKC alpha and beta-2 | PKC-A | PKC-alpha | PKCA | PRKACA | PRKCA | Protein Kinase C- alpha | Protein kinase C alpha | Protein kinase C alpha (PKCa) | Protein kinase C alpha type (PKC-A) | Protein kinase C alpha type (PRKCA) | Proto-oncogene c-RAF | RAF proto-oncogene serine/threonine-protein kinase
Type:
Enzyme
Mol. Mass.:
76755.65
Organism:
Homo sapiens (Human)
Description:
The recombinant human PKC enzymes were produced using a baculovirus expression system in SF9 cells
Residue:
672
Sequence:
MADVFPGNDSTASQDVANRFARKGALRQKNVHEVKDHKFIARFFKQPTFCSHCTDFIWGFGKQGFQCQVCCFVVHKRCHEFVTFSCPGADKGPDTDDPRSKHKFKIHTYGSPTFCDHCGSLLYGLIHQGMKCDTCDMNVHKQCVINVPSLCGMDHTEKRGRIYLKAEVADEKLHVTVRDAKNLIPMDPNGLSDPYVKLKLIPDPKNESKQKTKTIRSTLNPQWNESFTFKLKPSDKDRRLSVEIWDWDRTTRNDFMGSLSFGVSELMKMPASGWYKLLNQEEGEYYNVPIPEGDEEGNMELRQKFEKAKLGPAGNKVISPSEDRKQPSNNLDRVKLTDFNFLMVLGKGSFGKVMLADRKGTEELYAIKILKKDVVIQDDDVECTMVEKRVLALLDKPPFLTQLHSCFQTVDRLYFVMEYVNGGDLMYHIQQVGKFKEPQAVFYAAEISIGLFFLHKRGIIYRDLKLDNVMLDSEGHIKIADFGMCKEHMMDGVTTRTFCGTPDYIAPEIIAYQPYGKSVDWWAYGVLLYEMLAGQPPFDGEDEDELFQSIMEHNVSYPKSLSKEAVSVCKGLMTKHPAKRLGCGPEGERDVREHAFFRRIDWEKLENREIQPPFKPKVCGKGAENFDKFFTRGQPVLTPPDQLVIANIDQSDFEGFSYVNPQFVHPILQSAV
  
Inhibitor
Name:
BDBM3189
Synonyms:
(+-)-2-[[2,6-Dihydroxy-4-[[[3-(4-hydroxyphenyl)-2-[(naphthylsulfonyl)amino]propyl]oxy]carbonyl]phenyl]carbonyl]-3-hydroxybenzoic Acid | 2-[(2,6-dihydroxy-4-{[3-(4-hydroxyphenyl)-2-(naphthalene-2-sulfonamido)propoxy]carbonyl}phenyl)carbonyl]-3-hydroxybenzoic acid | Acyclic Balanol Analog 16b
Type:
Small organic molecule
Emp. Form.:
C34H27NO11S
Mol. Mass.:
657.643
SMILES:
OC(=O)c1cccc(O)c1C(=O)c1c(O)cc(cc1O)C(=O)OCC(Cc1ccc(O)cc1)NS(=O)(=O)c1ccc2ccccc2c1
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