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Target
Protein kinase C delta type
Ligand
BDBM2683
Substrate
Peptide Substrate
Meas. Tech.
Protein Kinase Assays
pH
7.4±n/a
Temperature
296.15±n/a K
IC50
8.7±1.5 nM
Citation
Wagner, J; von Matt, P; Sedrani, R; Albert, R; Cooke, N; Ehrhardt, C; Geiser, M; Rummel, G; Stark, W; Strauss, A; Cowan-Jacob, SW; Beerli, C; Weckbecker, G; Evenou, JP; Zenke, G; Cottens, S Discovery of 3-(1H-indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrole-2,5-dione (AEB071), a potent and selective inhibitor of protein kinase C isotypes. J Med Chem 52:6193-6 (2009) [PubMed] Article
Target
Name:
Protein kinase C delta type
Synonyms:
KPCD_HUMAN | PKC delta | PKCD | PRKCD | Protein Kinase C- delta | Protein kinase C, PKC; classical/novel | nPKC-delta
Type:
Enzyme
Mol. Mass.:
77516.79
Organism:
Human
Description:
The recombinant human PKC enzymes were
produced using a baculovirus expression system in SF9 cells
Residue:
676
Sequence:
MAPFLRIAFNSYELGSLQAEDEANQPFCAVKMKEALSTERGKTLVQKKPTMYPEWKSTFDAHIYEGRVIQIVLMRAAEEPVSEVTVGVSVLAERCKKNNGKAEFWLDLQPQAKVLMSVQYFLEDVDCKQSMRSEDEAKFPTMNRRGAIKQAKIHYIKNHEFIATFFGQPTFCSVCKDFVWGLNKQGYKCRQCNAAIHKKCIDKIIGRCTGTAANSRDTIFQKERFNIDMPHRFKVHNYMSPTFCDHCGSLLWGLVKQGLKCEDCGMNVHHKCREKVANLCGINQKLLAEALNQVTQRASRRSDSASSEPVGIYQGFEKKTGVAGEDMQDNSGTYGKIWEGSSKCNINNFIFHKVLGKGSFGKVLLGELKGRGEYFAIKALKKDVVLIDDDVECTMVEKRVLTLAAENPFLTHLICTFQTKDHLFFVMEFLNGGDLMYHIQDKGRFELYRATFYAAEIMCGLQFLHSKGIIYRDLKLDNVLLDRDGHIKIADFGMCKENIFGESRASTFCGTPDYIAPEILQGLKYTFSVDWWSFGVLLYEMLIGQSPFHGDDEDELFESIRVDTPHYPRWITKESKDILEKLFEREPTKRLGVTGNIKIHPFFKTINWTLLEKRRLEPPFRPKVKSPRDYSNFDQEFLNEKARLSYSDKNLIDSMDQSAFAGFSFVNPKFEHLLED
Inhibitor
Name:
BDBM2683
Synonyms:
2-[1-(3-dimethylaminopropyl)-indol-3-yl]-3-(indol-3-yl)maleimide | 3-{1-[3-(dimethylamino)propyl]-1H-indol-3-yl}-4-(1H-indol-3-yl)-2,5-dihydro-1H-pyrrole-2,5-dione | BIM-1 | CHEMBL7463 | GF 109203X | JMC526193 Compound 2
Type:
Small organic molecule
Emp. Form.:
C25H24N4O2
Mol. Mass.:
412.4837
SMILES:
CN(C)CCCn1cc(C2=C(C(=O)NC2=O)c2c[nH]c3ccccc23)c2ccccc12 |t:9|
Substrate
Name:
Peptide Substrate
Synonyms:
biotinylated tridecapeptide substrate
Type:
Peptide
Mol. Mass.:
1564.86
Organism:
n/a
Description:
n/a
Residue:
13
Sequence:
RFARKGSLRQKNV