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Target
Protein kinase C beta type
Ligand
BDBM2712
Substrate
Lysine-rich histone
Meas. Tech.
PKC assay
IC50
9.8±n/a nM
Citation
 Bit, RA; Davis, PD; Elliott, LH; Harris, W; Hill, CH; Keech, E; Kumar, H; Lawton, G; Maw, A; Nixon, 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:
BDBM2712
Synonyms:
3-(1-methyl-1H-indol-3-yl)-4-{2-[(methylamino)methyl]-1H,2H,3H,4H-pyrido[1,2-a]indol-10-yl}-2,5-dihydro-1H-pyrrole-2,5-dione | 3-[6,7,8,9-Tetrahydro-8-[(methylamino)methyl]pyrido[1,2-a]indol-10-yl]-4-(1-methyl-3-indolyl)-1H-pyrrole-2,5-dione Hydrochloride | Bisindolylmaleimide deriv. 18a
Type:
Small organic molecule
Emp. Form.:
C27H26N4O2
Mol. Mass.:
438.5209
SMILES:
CNCC1CCn2c(C1)c(C1=C(C(=O)NC1=O)c1cn(C)c3ccccc13)c1ccccc21 |t:11|
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