Target
Protein kinase C beta type
Ligand
BDBM2699
Substrate
Lysine-rich histone
Meas. Tech.
PKC assay
pH
7.5±n/a
Temperature
303.15±n/a K
IC50
14±8 nM
Citation
 Bit, RADavis, PDElliott, LHHarris, WHill, CHKeech, EKumar, HLawton, GMaw, ANixon, JS Inhibitors of protein kinase C. 3. Potent and highly selective bisindolylmaleimides by conformational restriction. J Med Chem 36:21-9 (1993) [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:
BDBM2699
Synonyms:
3-[2-(aminomethyl)-1H,2H,3H-benzo[b]pyrrolizin-9-yl]-4-(1-methyl-1H-indol-3-yl)-2,5-dihydro-1H-pyrrole-2,5-dione | Bisindolylmaleimide deriv. 9a | ROCHE screening, 61
Type:
Small organic molecule
Emp. Form.:
C25H22N4O2
Mol. Mass.:
410.4678
SMILES:
Cn1cc(C2=C(C(=O)NC2=O)c2c3CC(CN)Cn3c3ccccc23)c2ccccc12 |t:4|
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