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Target
Glycogen synthase kinase-3 beta
Ligand
BDBM7447
Substrate
GSK-3 Peptide Substrate
Meas. Tech.
Kinase Inhibition Assay
pH
7.5±n/a
Temperature
303.15±n/a K
IC50
>10000±n/a nM
Citation
 Laronze, M; Boisbrun, M; Leonce, S; Pfeiffer, B; Renard, P; Lozach, O; Meijer, L; Lansiaux, A; Bailly, C; Sapi, J; Laronze, JY Synthesis and anticancer activity of new pyrrolocarbazoles and pyrrolo-beta-carbolines. Bioorg Med Chem 13:2263-83 (2005) [PubMed]  Article
Target
Name:
Glycogen synthase kinase-3 beta
Synonyms:
GSK-3 alpha/beta | Glycogen Synthase Kinase-3, beta
Type:
Enzyme Mixture
Mol. Mass.:
48062.20
Organism:
Porcine
Description:
Purification of GSK-3 alpha and GSK-3 beta from Porcine Brain on Axin-Sepharose. Porcine brains were obtained from a local slaughter and directly homogenized and processed for affinity chromatography.
Residue:
433
Sequence:
MSGRPRTTSFAESCKPVQQPSAFGSMKVSRDKDGSKVTTVVATPGQGPDRPQEVSYTDTKVIGNGSFGVVYQAKLCDSGELVAIKKVLQDKRFKNRELQIMRKLDHCNIVRLRYFFYSSGEKKDEVYLNLVLDYVPETVYRVARHYSRAKQTLPVIYVKLYMYQLFRSLAYIHSFGICHRDIKPQNLLLDPDTAVLKLCDFGSAKQLVRGEPNVSYICSRYYRAPELIFGATDYTSSIDVWSAGCVLAELLLGQPIFPGDSGVDQLVEIIKVLGTPTREQIREMNPNYTEFKFPQIKAHPWTKDSSGTGHFTSGVRVFRPRTPPEAIALCSRLLEYTPTARLTPLEACAHSFFDELRDPNVKLPNGRDTPALFNFTTQELSSNPPLATILIPPHARIQAAASTPSNATAASDTNAGDRGQTNNTASASASNST
  
Inhibitor
Name:
BDBM7447
Synonyms:
N-[(2,4-dimethyl-1,3-dioxo-5-{[2-(trimethylsilyl)ethoxy]methyl}-1H,2H,3H,5H-pyrrolo[3,4-b]carbazol-10-yl)methyl]-3-(dimethylamino)propanamide | pyrrolocarbazole deriv. 26a
Type:
Small organic molecule
Emp. Form.:
C28H38N4O4Si
Mol. Mass.:
522.7112
SMILES:
CN(C)CCC(=O)NCc1c2C(=O)N(C)C(=O)c2c(C)c2n(COCC[Si](C)(C)C)c3ccccc3c12
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
GSK-3 Peptide Substrate
Synonyms:
GS-1 Peptide | Phospho-GS2 Substrate Peptide
Type:
Peptide
Mol. Mass.:
3045.17
Organism:
n/a
Description:
n/a
Residue:
27
Sequence:
YRRAAVPPSPSLSRHSSPHQSPEDEEE