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Target
Glycogen synthase kinase-3 beta
Ligand
BDBM7336
Substrate
GSK-3 Peptide Substrate
Meas. Tech.
Kinase Inhibition Assay
pH
7.5±n/a
Temperature
303.15±n/a K
IC50
120±n/a nM
Citation
 Kunick, C; Lauenroth, K; Leost, M; Meijer, L; Lemcke, T 1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta. Bioorg Med Chem Lett 14:413-6 (2004) [PubMed]  Article 
Target
Name:
Glycogen synthase kinase-3 beta
Synonyms:
GSK-3, beta | GSK3B_RAT | Glycogen Synthase Kinase-3, beta | Gsk3b
Type:
Enzyme
Mol. Mass.:
46754.43
Organism:
Rattus norvegicus (rat)
Description:
The rat GSK-3 beta cDNA was inserted into the baculovirus vector. The protein was purified from virus-infected sf9 insect cells
Residue:
420
Sequence:
MSGRPRTTSFAESCKPVQQPSAFGSMKVSRDKDGSKVTTVVATPGQGPDRPQEVSYTDTKVIGNGSFGVVYQAKLCDSGELVAIKKVLQDKRFKNRELQIMRKLDHCNIVRLRYFFYSSGEKKDEVYLNLVLDYVPETVYRVARHYSRAKQTLPVIYVKLYMYQLFRSLAYIHSFGICHRDIKPQNLLLDPDTAVLKLCDFGSAKQLVRGEPNVSYICSRYYRAPELIFGATDYTSSIDMWSAGCVLAELLLGQPIFPGDSGVDQLVEIIKVLGTPTREQIREMNPNYTEFKFPQIKAHPWTKVFRPRTPPEAIALCSRLLEYTPTARLTPLEACAHSFFDELRDPNVKLPNGRDTPALFNFTTQELSSNPPLATILIPPHARIQAAASPPANATAASDTNAGDRGQTNNAASASASNST
  
Inhibitor
Name:
BDBM7336
Synonyms:
13-bromo-3-thia-7,17-diazatetracyclo[8.7.0.0^{2,6}.0^{11,16}]heptadeca-1(10),2(6),4,11(16),12,14-hexaen-8-one | 8-Bromo-6,11-dihydro-thieno[3 ,2 :2,3]azepino[4,5-b]indol-5(4H)-one | NSC 703058 | Paullone Analogue 71 | Thieno analogue of kenpaullone
Type:
Small organic molecule
Emp. Form.:
C14H9BrN2OS
Mol. Mass.:
333.203
SMILES:
Brc1ccc2[nH]c-3c(CC(=O)Nc4ccsc-34)c2c1
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