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Target
Glycogen synthase kinase-3 beta
Ligand
BDBM7434
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:
BDBM7434
Synonyms:
2-Benzyl-5-phenyl-1,2-dihydro-6H-2,4,6-triazacyclopenta[c]fluoren-3-one | 4-benzyl-8-phenyl-4,7,10-triazatetracyclo[7.7.0.0^{2,6}.0^{11,16}]hexadeca-1(9),2(6),7,11(16),12,14-hexaen-5-one | pyrrolo-beta-carboline deriv. 30
Type:
Small organic molecule
Emp. Form.:
C26H19N3O
Mol. Mass.:
389.4486
SMILES:
O=C1N(Cc2ccccc2)Cc2c1nc(-c1ccccc1)c1[nH]c3ccccc3c21
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