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Target
Glycogen synthase kinase-3 beta
Ligand
BDBM7424
Substrate
GSK-3 Peptide Substrate
Meas. Tech.
Kinase Inhibition Assay
Temperature
303.15±n/a K
IC50
4±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:
BDBM7424
Synonyms:
(2 Z,3 E)-5,6-Dichloroindirubin-3 -oxime | 5,6-dichloro-3-[(2Z,3E)-3-(hydroxyimino)-2,3-dihydro-1H-indol-2-ylidene]-2,3-dihydro-1H-indol-2-one | 6,5-dichloroindirubin-3 -oxime | indirubin deriv. 7e
Type:
Small organic molecule
Emp. Form.:
C16H9Cl2N3O2
Mol. Mass.:
346.168
SMILES:
Clc1cc2NC(=O)C(c2cc1Cl)c1[nH]c2ccccc2c1N=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