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Target
Phosphorylase b kinase regulatory subunit alpha, skeletal muscle isoform
Ligand
BDBM2689
Substrate
Phosphorylase b
Meas. Tech.
Phosphorylase Kinasse Assay
IC50
2750±n/a nM
Citation
 Toullec, D; Pianetti, P; Coste, H; Bellevergue, P; Grand-Perret, T; Ajakane, M; Baudet, V; Boissin, P; Boursier, E; Loriolle, F The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C. J Biol Chem 266:15771-81 (1991) [PubMed] 
Target
Name:
Phosphorylase b kinase regulatory subunit alpha, skeletal muscle isoform
Synonyms:
KPB1_RABIT | PHKA1 | Phosphorylase Kinase
Type:
Enzyme Complex
Mol. Mass.:
138403.25
Organism:
Oryctolagus cuniculus (rabbit)
Description:
The enzyme is a hexadecamer of four types of subunits:alpha(4)beta(4)gamma(4)delta(4) isolated from skeletal muscle of rabbits.
Residue:
1237
Sequence:
MRSRSNSGVRLDSYARLVQQTILCHQNPVTGLLPASYDQKDAWVRDNVYSILAVWGLGLAYRKNADRDEDKAKAYELEQSVVKLMRGLLHCMIRQVDKVESFKYSQSTKDSLHAKYNTKTCATVVGDDQWGHLQLDATSVYLLFLAQMTASGLHIIHSLDEVNFIQNLVFYIEAAYKTADFGIWERGDKTNQGISELNASSVGMAKAALEALDELDLFGVKGGPQSVIHVLADEVQHCQSILNSLLPRASTSKEVDASLLSVISFPAFAVEDSKLVEITKQEIITKLQGRYGCCRFLRDGYKTPKEDPNRLYYEPAELKLFENIECEWPLFWTYFILDGVFSGNAEQVQEYREALEAVLIKGKNGVPLLPELYSVPPDKVDEEYQNPHTVDRVPMGKLPHMWGQSLYILGSLMAEGFLAPGEIDPLNRRFSTVPKPDVVVQVSILAETEEIKAILKDKGINVETIAEVYPIRVQPARILSHIYSSLGCNNRMKLSGRPYRHMGVLGTSKLYDIRKTIFTFTPQFIDQQQFYLALDNKMIVEMLRTDLSYLCSRWRMTGQPTITFPISQTMLDEDGTSLNSSILAALRKMQDGYFGGARIQTGKLSEFLTTSCCTHLSFMDPGPEGKLYSEDYDDNYDELESGDWMDGYNSTSTARCGDEVARYLDHLLAHTAPHPKLAPASQKGGLNRFRAAVQTTCDLMSLVTKAKELHVQNVHMYLPTKLFQASRPSLNLLDSSHPSQEDQVPTVRVEVHLPRDQSGEVDFQALVLQLKETSSLQEQADILYMLYTMKGPDWDTELYEEGSATVRELLTELYGKVGKIRHWGLIRYISGILRKKVEALDEACTDLLSHQKHLTVGLPPEPREKTISAPLPYEALTRLIEEACEGDMNISILTQEIMVYLAMYMRTQPGLFAEMFRLRIGLIIQVMATELAHSLRCSAEEATEGLMNLSPSAMKNLLHHILSGKEFGVERSVRPTDSNVSPAISIHEIGAVGATKTERTGIMQLKSEIKQVEFRRLSISTESQPNGGHSLGADLMSPSFLSPGTSVTPSSGSFPGHHTSKDSRQGQWQRRRRLDGALNRVPIGFYQKVWKVLQKCHGLSVEGFVLPSSTTREMTPGEIKFSVHVESVLNRVPQPEYRQLLVEAILVLTMLADIEIHSIGSIIAVEKIVHIANDLFLQEQKTLGADDIMLAKDPASGICTLLYDSAPSGRFGTMTYLSKAAATYVQEFLPHSICAMQ
  
Inhibitor
Name:
BDBM2689
Synonyms:
3-[1-(3-dymethylaminopropyl)-indol-3-yl]-4-(indol-3-yl)-3-pyrrolin-2-one | 3-{1-[3-(dimethylamino)propyl]-1H-indol-3-yl}-4-(1H-indol-3-yl)-2,5-dihydro-1H-pyrrol-2-one | Bisindolyl deriv. 17
Type:
Small organic molecule
Emp. Form.:
C25H26N4O
Mol. Mass.:
398.5001
SMILES:
CN(C)CCCn1cc(C2=C(CNC2=O)c2c[nH]c3ccccc23)c2ccccc12 |t:9|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Phosphorylase b
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
1157.29
Organism:
n/a
Description:
250 uM [gamma-32P]ATP as co-substrate.
Residue:
12
Sequence:
ISVGLAGVENVT