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Target
Glycogen synthase kinase-3 beta
Ligand
BDBM25017
Substrate
GSK-3 Peptide Substrate
Meas. Tech.
Kinase Inhibition Assay
pH
7.5±n/a
Temperature
295.15±n/a K
IC50
1590±21 nM
Citation
Sapkota, GP; Cummings, L; Newell, FS; Armstrong, C; Bain, J; Frodin, M; Grauert, M; Hoffmann, M; Schnapp, G; Steegmaier, M; Cohen, P; Alessi, DR BI-D1870 is a specific inhibitor of the p90 RSK (ribosomal S6 kinase) isoforms in vitro and in vivo. Biochem J 401:29-38 (2007) [PubMed] Article
More Info.:
Target
Name:
Glycogen synthase kinase-3 beta
Synonyms:
GSK-3 beta | GSK-3, beta | GSK3B | GSK3B_HUMAN | Glycogen synthase kinase 3 beta (GSK3B) | Glycogen synthase kinase 3-beta (GSK3B) | Glycogen synthase kinase-3 beta (GSK-3B) | Glycogen synthase kinase-3 beta (GSK3 Beta) | Glycogen synthase kinase-3 beta (GSK3B) | Glycogen synthase kinase-3B (GSK-3B) | Glycogen synthase kinase-3beta (GSK3B) | Serine/threonine-protein kinase GSK3B
Type:
Enzyme
Mol. Mass.:
46756.38
Organism:
Homo sapiens (Human)
Description:
P49841
Residue:
420
Sequence:
MSGRPRTTSFAESCKPVQQPSAFGSMKVSRDKDGSKVTTVVATPGQGPDRPQEVSYTDTKVIGNGSFGVVYQAKLCDSGELVAIKKVLQDKRFKNRELQIMRKLDHCNIVRLRYFFYSSGEKKDEVYLNLVLDYVPETVYRVARHYSRAKQTLPVIYVKLYMYQLFRSLAYIHSFGICHRDIKPQNLLLDPDTAVLKLCDFGSAKQLVRGEPNVSYICSRYYRAPELIFGATDYTSSIDVWSAGCVLAELLLGQPIFPGDSGVDQLVEIIKVLGTPTREQIREMNPNYTEFKFPQIKAHPWTKVFRPRTPPEAIALCSRLLEYTPTARLTPLEACAHSFFDELRDPNVKLPNGRDTPALFNFTTQELSSNPPLATILIPPHARIQAAASTPTNATAASDANTGDRGQTNNAASASASNST
Inhibitor
Name:
BDBM25017
Synonyms:
2-[(3,5-difluoro-4-hydroxyphenyl)amino]-5,7-dimethyl-8-(3-methylbutyl)-5,6,7,8-tetrahydropteridin-6-one | BI-D1870 | US11851436, Compound BI-D1870
Type:
Small organic molecule
Emp. Form.:
C19H23F2N5O2
Mol. Mass.:
391.415
SMILES:
CC(C)CCN1C(C)C(=O)N(C)c2cnc(Nc3cc(F)c(O)c(F)c3)nc12
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