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Target
Protein kinase C alpha type
Ligand
BDBM3212
Substrate
Lysine-rich histone
Meas. Tech.
PKC assay
pH
7.5±n/a
Temperature
303.15±n/a K
IC50
860±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 alpha type
Synonyms:
KPCA_HUMAN | PKC alpha | PKC alpha and beta-2 | PKC-A | PKC-alpha | PKCA | PRKACA | PRKCA | Protein Kinase C- alpha | Protein kinase C alpha | Protein kinase C alpha (PKCa) | Protein kinase C alpha type (PKC-A) | Protein kinase C alpha type (PRKCA) | Proto-oncogene c-RAF | RAF proto-oncogene serine/threonine-protein kinase
Type:
Enzyme
Mol. Mass.:
76755.65
Organism:
Homo sapiens (Human)
Description:
The recombinant human PKC enzymes were
produced using a baculovirus expression system in SF9 cells
Residue:
672
Sequence:
MADVFPGNDSTASQDVANRFARKGALRQKNVHEVKDHKFIARFFKQPTFCSHCTDFIWGFGKQGFQCQVCCFVVHKRCHEFVTFSCPGADKGPDTDDPRSKHKFKIHTYGSPTFCDHCGSLLYGLIHQGMKCDTCDMNVHKQCVINVPSLCGMDHTEKRGRIYLKAEVADEKLHVTVRDAKNLIPMDPNGLSDPYVKLKLIPDPKNESKQKTKTIRSTLNPQWNESFTFKLKPSDKDRRLSVEIWDWDRTTRNDFMGSLSFGVSELMKMPASGWYKLLNQEEGEYYNVPIPEGDEEGNMELRQKFEKAKLGPAGNKVISPSEDRKQPSNNLDRVKLTDFNFLMVLGKGSFGKVMLADRKGTEELYAIKILKKDVVIQDDDVECTMVEKRVLALLDKPPFLTQLHSCFQTVDRLYFVMEYVNGGDLMYHIQQVGKFKEPQAVFYAAEISIGLFFLHKRGIIYRDLKLDNVMLDSEGHIKIADFGMCKEHMMDGVTTRTFCGTPDYIAPEIIAYQPYGKSVDWWAYGVLLYEMLAGQPPFDGEDEDELFQSIMEHNVSYPKSLSKEAVSVCKGLMTKHPAKRLGCGPEGERDVREHAFFRRIDWEKLENREIQPPFKPKVCGKGAENFDKFFTRGQPVLTPPDQLVIANIDQSDFEGFSYVNPQFVHPILQSAV
Inhibitor
Name:
BDBM3212
Synonyms:
(3R,4R)-3-[(4-hydroxybenzene)amido]azepan-4-yl 4-[(2,6-dihydroxyphenyl)carbonyl]-3,5-dihydroxybenzoate | Modified Benzophenone Ring, Balanol Analog 12 | trans-4-[3,5-Dihydroxy-4-(2,6-dihydroxybenzoyloxy)]-3-(4-hydroxybenzamido)azepane
Type:
Small organic molecule
Emp. Form.:
C27H26N2O9
Mol. Mass.:
522.5033
SMILES:
Oc1ccc(cc1)C(=O)N[C@@H]1CNCCC[C@H]1OC(=O)c1cc(O)c(C(=O)c2c(O)cccc2O)c(O)c1 |r|
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