Target
Glycogen synthase kinase-3 beta
Ligand
BDBM7438
Substrate
GSK-3 Peptide Substrate
Meas. Tech.
Kinase Inhibition Assay
pH
7.5±n/a
Temperature
303.15±n/a K
IC50
7000±n/a nM
Citation
 Laronze, MBoisbrun, MLeonce, SPfeiffer, BRenard, PLozach, OMeijer, LLansiaux, ABailly, CSapi, JLaronze, 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:
BDBM7438
Synonyms:
10-[2-(dimethylamino)ethyl]-8-methyl-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 | 6-(2-Dimethylaminoethyl)-5-methyl-1,2-di-hydro-6H-2,4,6-triaza-cyclopenta[c]fluoren-3-one | pyrrolo-beta-carboline deriv. 36
Type:
Small organic molecule
Emp. Form.:
C18H20N4O
Mol. Mass.:
308.3776
SMILES:
CN(C)CCn1c2ccccc2c2c3CNC(=O)c3nc(C)c12
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