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Target
Glycogen synthase kinase-3 beta
Ligand
BDBM7411
Substrate
GSK-3 Peptide Substrate
Meas. Tech.
Kinase Inhibition Assay
Temperature
303.15±n/a K
IC50
13±n/a nM
Comments
extracted
Citation
 Polychronopoulos, P; Magiatis, P; Skaltsounis, AL; Myrianthopoulos, V; Mikros, E; Tarricone, A; Musacchio, A; Roe, SM; Pearl, L; Leost, M; Greengard, P; Meijer, L Structural basis for the synthesis of indirubins as potent and selective inhibitors of glycogen synthase kinase-3 and cyclin-dependent kinases. J Med Chem 47:935-46 (2004) [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:
BDBM7411
Synonyms:
(2 Z,3 E)-6-Iodoindirubin-3 -acetoxime | 6-iodoindirubin-3 -acetoxime | [(3E)-2-[(3Z)-6-iodo-2-oxo-2,3-dihydro-1H-indol-3-ylidene]-2,3-dihydro-1H-indol-3-ylidene]amino acetate | indirubin deriv. 8c
Type:
Small organic molecule
Emp. Form.:
C18H12IN3O3
Mol. Mass.:
445.2107
SMILES:
CC(=O)ON=C1C(Nc2ccccc12)=C1C(=O)Nc2cc(I)ccc12 |w:6.5,4.3|
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