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Target
Protein kinase C beta type
Ligand
BDBM3149
Substrate
Lysine-rich histone
Meas. Tech.
PKC assay
IC50
10±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 beta type
Synonyms:
KPCB_HUMAN | PKC alpha and beta-2 | PKC beta | PKC beta isoform 2 | PKCB | PRKCB | PRKCB1 | Protein Kinase C, beta II | Protein kinase C beta type | Protein kinase C beta type II (PRKCB2)
Type:
Enzyme
Mol. Mass.:
76873.67
Organism:
Homo sapiens (Human)
Description:
The recombinant human PKC enzymes were produced using a baculovirus expression system in SF9 cells
Residue:
671
Sequence:
MADPAAGPPPSEGEESTVRFARKGALRQKNVHEVKNHKFTARFFKQPTFCSHCTDFIWGFGKQGFQCQVCCFVVHKRCHEFVTFSCPGADKGPASDDPRSKHKFKIHTYSSPTFCDHCGSLLYGLIHQGMKCDTCMMNVHKRCVMNVPSLCGTDHTERRGRIYIQAHIDRDVLIVLVRDAKNLVPMDPNGLSDPYVKLKLIPDPKSESKQKTKTIKCSLNPEWNETFRFQLKESDKDRRLSVEIWDWDLTSRNDFMGSLSFGISELQKASVDGWFKLLSQEEGEYFNVPVPPEGSEANEELRQKFERAKISQGTKVPEEKTTNTVSKFDNNGNRDRMKLTDFNFLMVLGKGSFGKVMLSERKGTDELYAVKILKKDVVIQDDDVECTMVEKRVLALPGKPPFLTQLHSCFQTMDRLYFVMEYVNGGDLMYHIQQVGRFKEPHAVFYAAEIAIGLFFLQSKGIIYRDLKLDNVMLDSEGHIKIADFGMCKENIWDGVTTKTFCGTPDYIAPEIIAYQPYGKSVDWWAFGVLLYEMLAGQAPFEGEDEDELFQSIMEHNVAYPKSMSKEAVAICKGLMTKHPGKRLGCGPEGERDIKEHAFFRYIDWEKLERKEIQPPYKPKARDKRDTSNFDKEFTRQPVELTPTDKLFIMNLDQNEFAGFSYTNPEFVINV
  
Inhibitor
Name:
BDBM3149
Synonyms:
2-{[2,6-dihydroxy-4-({[(3R,4R)-3-[(4-hydroxybenzene)amido]azepan-4-yl]oxy}carbonyl)phenyl]carbonyl}-3-hydroxybenzoic acid | Acyclic Balanol Analog (-)-1 | Balanol analog 1 | Balanol, 1 | CHEMBL60254
Type:
Small organic molecule
Emp. Form.:
C28H26N2O10
Mol. Mass.:
550.5134
SMILES:
OC(=O)c1cccc(O)c1C(=O)c1c(O)cc(cc1O)C(=O)O[C@@H]1CCCNC[C@H]1NC(=O)c1ccc(O)cc1 |r|
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