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Target
Ribosomal protein S6 kinase alpha-6
Ligand
BDBM25017
Substrate
RSK Substrate Peptide
Meas. Tech.
Kinase Inhibition Assay
pH
7.5±n/a
Temperature
295.15±n/a K
IC50
15±7 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 
Target
Name:
Ribosomal protein S6 kinase alpha-6
Synonyms:
90 kDa ribosomal protein S6 kinase 6 | KS6A6_HUMAN | RPS6KA6 | RPS6KA6(Kin.Dom.1 - N-terminal) | RPS6KA6(Kin.Dom.2 - C-terminal) | RSK-4 | RSK4 | Ribosomal S6 Kinase 4 (RSK-4) | Ribosomal S6 kinase 4 | Ribosomal protein S6 kinase alpha 6 | Ribosomal protein S6 kinase alpha 6 (RSK4) | Ribosomal protein S6 kinase alpha-6 | S6K-alpha 6 | p90-RSK 6 | p90RSK | pp90RSK4
Type:
Serine/threonine-protein kinase
Mol. Mass.:
83868.06
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
745
Sequence:
MLPFAPQDEPWDREMEVFSGGGASSGEVNGLKMVDEPMEEGEADSCHDEGVVKEIPITHHVKEGYEKADPAQFELLKVLGQGSFGKVFLVRKKTGPDAGQLYAMKVLKKASLKVRDRVRTKMERDILVEVNHPFIVKLHYAFQTEGKLYLILDFLRGGDVFTRLSKEVLFTEEDVKFYLAELALALDHLHQLGIVYRDLKPENILLDEIGHIKLTDFGLSKESVDQEKKAYSFCGTVEYMAPEVVNRRGHSQSADWWSYGVLMFEMLTGTLPFQGKDRNETMNMILKAKLGMPQFLSAEAQSLLRMLFKRNPANRLGSEGVEEIKRHLFFANIDWDKLYKREVQPPFKPASGKPDDTFCFDPEFTAKTPKDSPGLPASANAHQLFKGFSFVATSIAEEYKITPITSANVLPIVQINGNAAQFGEVYELKEDIGVGSYSVCKRCIHATTNMEFAVKIIDKSKRDPSEEIEILMRYGQHPNIITLKDVFDDGRYVYLVTDLMKGGELLDRILKQKCFSEREASDILYVISKTVDYLHCQGVVHRDLKPSNILYMDESASADSIRICDFGFAKQLRGENGLLLTPCYTANFVAPEVLMQQGYDAACDIWSLGVLFYTMLAGYTPFANGPNDTPEEILLRIGNGKFSLSGGNWDNISDGAKDLLSHMLHMDPHQRYTAEQILKHSWITHRDQLPNDQPKRNDVSHVVKGAMVATYSALTHKTFQPVLEPVAASSLAQRRSMKKRTSTGL
  
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
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
RSK Substrate Peptide
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
1132.38
Organism:
n/a
Description:
n/a
Residue:
10
Sequence:
KKLNRTLSVA