Target
Glycogen synthase kinase-3 beta
Ligand
BDBM7420
Substrate
GSK-3 Peptide Substrate
Meas. Tech.
Kinase Inhibition Assay
Temperature
303.15±n/a K
IC50
25±n/a nM
Comments
extracted
Citation
 Polychronopoulos, PMagiatis, PSkaltsounis, ALMyrianthopoulos, VMikros, ETarricone, AMusacchio, ARoe, SMPearl, LLeost, MGreengard, PMeijer, 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:
BDBM7420
Synonyms:
(2 Z)-6-Bromo-5-methylindirubin | 6-bromo-5-methyl-3-[(2Z)-3-oxo-2,3-dihydro-1H-indol-2-ylidene]-2,3-dihydro-1H-indol-2-one | 6-bromo-5-methylindirubin | indirubin deriv. 5f
Type:
Small organic molecule
Emp. Form.:
C17H11BrN2O2
Mol. Mass.:
355.185
SMILES:
Cc1cc2\C(C(=O)Nc2cc1Br)=C1\Nc2ccccc2C1=O
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