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Target
Protein kinase C beta type
Ligand
BDBM2681
Substrate
Lysine-rich histone
Meas. Tech.
PKC assay
IC50
45±n/a nM
Citation
 Davis, PD; Elliott, LH; Harris, W; Hill, CH; Hurst, SA; Keech, E; Kumar, MK; Lawton, G; Nixon, JS; Wilkinson, SE Inhibitors of protein kinase C. 2. Substituted bisindolylmaleimides with improved potency and selectivity. J Med Chem 35:994-1001 (1992) [PubMed]  Article 
Target
Name:
Protein kinase C beta type
Synonyms:
KPCB_RAT | PKC, rat brain | Pkcb | Prkcb | Prkcb1 | Protein Kinase C | Protein kinase C (PKC) | Protein kinase C beta
Type:
Enzyme Mixture
Mol. Mass.:
76755.54
Organism:
Rattus norvegicus (rat)
Description:
PKC from rat brain is known to contain predominately the conventional PKC isoforms, alpha, beta I, beta II, gamma.
Residue:
671
Sequence:
MADPAAGPPPSEGEESTVRFARKGALRQKNVHEVKNHKFTARFFKQPTFCSHCTDFIWGFGKQGFQCQVCCFVVHKRCHEFVTFSCPGADKGPASDDPRSKHKFKIHTYSSPTFCDHCGSLLYGLIHQGMKCDTCMMNVHKRCVMNVPSLCGTDHTERRGRIYIQAHIDREVLIVVVRDAKNLVPMDPNGLSDPYVKLKLIPDPKSESKQKTKTIKCSLNPEWNETFRFQLKESDKDRRLSVEIWDWDLTSRNDFMGSLSFGISELQKAGVDGWFKLLSQEEGEYFNVPVPPEGSEGNEELRQKFERAKIGQGTKAPEEKTANTISKFDNNGNRDRMKLTDFNFLMVLGKGSFGKVMLSERKGTDELYAVKILKKDVVIQDDDVECTMVEKRVLALPGKPPFLTQLHSCFQTMDRLYFVMEYVNGGDLMYHIQQVGRFKEPHAVFYAAEIAIGLFFLQSKGIIYRDLKLDNVMLDSEGHIKIADFGMCKENIWDGVTTKTFCGTPDYIAPEIIAYQPYGKSVDWWAFGVLLYEMLAGQAPFEGEDEDELFQSIMEHNVAYPKSMSKEAVAICKGLMTKHPGKRLGCGPEGERDIKEHAFFRYIDWEKLERKEIQPPYKPKARDKRDTSNFDKEFTRQPVELTPTDKLFIMNLDQNEFAGFSYTNPEFVINV
  
Inhibitor
Name:
BDBM2681
Synonyms:
3-{1-[3-(dimethylamino)propyl]-1H-indol-3-yl}-4-(1-methyl-1H-indol-3-yl)-2,5-dihydro-1H-pyrrole-2,5-dione | Bisindolyl deriv. 11 | CHEMBL268769
Type:
Small organic molecule
Emp. Form.:
C26H26N4O2
Mol. Mass.:
426.5102
SMILES:
CN(C)CCCn1cc(C2=C(C(=O)NC2=O)c2cn(C)c3ccccc23)c2ccccc12 |t:9|
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