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Target
Phosphorylase b kinase regulatory subunit alpha, skeletal muscle isoform
Ligand
BDBM2693
Substrate
Phosphorylase b
Meas. Tech.
Phosphorylase Kinasse Assay
IC50
2000±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:
BDBM2693
Synonyms:
3-(1H-indol-3-yl)-4-{1-[3-(morpholin-4-yl)propyl]-1H-indol-3-yl}-2,5-dihydro-1H-pyrrole-2,5-dione | Bisindolyl deriv. 21
Type:
Small organic molecule
Emp. Form.:
C27H26N4O3
Mol. Mass.:
454.5203
SMILES:
O=C1NC(=O)C(=C1c1c[nH]c2ccccc12)c1cn(CCCN2CCOCC2)c2ccccc12 |c:5|
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