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Target
Protein kinase C beta type
Ligand
BDBM3236
Substrate
Lysine-rich histone
Meas. Tech.
PKC assay
IC50
110±n/a nM
Citation
 Lampe, JW; Biggers, CK; Defauw, JM; Foglesong, RJ; Hall, SE; Heerding, JM; Hollinshead, SP; Hu, H; Hughes, PF; Jagdmann, GE; Johnson, MG; Lai, YS; Lowden, CT; Lynch, MP; Mendoza, JS; Murphy, MM; Wilson, JW; Ballas, LM; Carter, K; Darges, JW; Davis, JE; Hubbard, FR; Stamper, ML Synthesis and protein kinase inhibitory activity of balanol analogues with modified benzophenone subunits. J Med Chem 45:2624-43 (2002) [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:
BDBM3236
Synonyms:
(1R,2R)-2-[(4-hydroxybenzene)amido]cyclopentyl 3,5-dihydroxy-4-[(2-hydroxy-6-methanesulfonamidophenyl)carbonyl]benzoate | Modified Benzophenone Carboxylic Acid, Balanol Analog 36 | trans-2-[3,5-Dihydroxy-4-[2-hydroxy-6-(methanesulfonylamino)benzoyl]benzoyloxy]-1-(4-hydroxybenzamido)cyclopentane
Type:
Small organic molecule
Emp. Form.:
C27H26N2O10S
Mol. Mass.:
570.568
SMILES:
CS(=O)(=O)Nc1cccc(O)c1C(=O)c1c(O)cc(cc1O)C(=O)O[C@@H]1CCC[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