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Target
RAC-alpha serine/threonine-protein kinase
Ligand
BDBM29521
Substrate
Biotinylated GSK3 alpha Substrate Peptide
Meas. Tech.
Homogeneous Time-Resolved Fluorescence Resonance Energy Transfer Lance Assay
pH
7.4±n/a
Temperature
295.15±n/a K
IC50
383±n/a nM
Citation
 Salaski, EJ; Krishnamurthy, G; Ding, WD; Yu, K; Insaf, SS; Eid, C; Shim, J; Levin, JI; Tabei, K; Toral-Barza, L; Zhang, WG; McDonald, LA; Honores, E; Hanna, C; Yamashita, A; Johnson, B; Li, Z; Laakso, L; Powell, D; Mansour, TS Pyranonaphthoquinone lactones: a new class of AKT selective kinase inhibitors alkylate a regulatory loop cysteine. J Med Chem 52:2181-4 (2009) [PubMed]  Article 
Target
Name:
RAC-alpha serine/threonine-protein kinase
Synonyms:
AKT phosphorylation (p-AKT) | AKT1 | AKT1/PPP1CA | AKT1_HUMAN | C-AKT | PKB | PKB alpha | Protein kinase Akt-1 | Protein kinase B | Protein kinase B (AKT1) | Protein kinase B (Akt 1) | Protein kinase B (Akt) | Protein kinase B alpha | Protein kinase B alpha (AKT1) | Proto-oncogene Akt (Akt1) | Proto-oncogene c-Akt (AKT) | Proto-oncogene c-Akt (AKT1) | RAC | RAC-PK-alpha | RAC-alpha serine/threonine-protein kinase (AKT) | RAC-alpha serine/threonine-protein kinase (AKT1) | RAC-alpha serine/threonine-protein kinase (pAKT)
Type:
Enzyme
Mol. Mass.:
55681.25
Organism:
Homo sapiens (Human)
Description:
P31749
Residue:
480
Sequence:
MSDVAIVKEGWLHKRGEYIKTWRPRYFLLKNDGTFIGYKERPQDVDQREAPLNNFSVAQCQLMKTERPRPNTFIIRCLQWTTVIERTFHVETPEEREEWTTAIQTVADGLKKQEEEEMDFRSGSPSDNSGAEEMEVSLAKPKHRVTMNEFEYLKLLGKGTFGKVILVKEKATGRYYAMKILKKEVIVAKDEVAHTLTENRVLQNSRHPFLTALKYSFQTHDRLCFVMEYANGGELFFHLSRERVFSEDRARFYGAEIVSALDYLHSEKNVVYRDLKLENLMLDKDGHIKITDFGLCKEGIKDGATMKTFCGTPEYLAPEVLEDNDYGRAVDWWGLGVVMYEMMCGRLPFYNQDHEKLFELILMEEIRFPRTLGPEAKSLLSGLLKKDPKQRLGGGSEDAKEIMQHRFFAGIVWQHVYEKKLSPPFKPQVTSETDTRYFDEEFTAQMITITPPDQDDSMECVDSERRPHFPQFSYSASGTA
  
Inhibitor
Name:
BDBM29521
Synonyms:
Pyranonaphthoquinone (PNQ) lactone, 11k
Type:
n/a
Emp. Form.:
C18H16O5
Mol. Mass.:
312.3166
SMILES:
CCC[C@@H]1O[C@@H]2CC(=O)O[C@@H]2C2=C1C(=O)c1ccccc1C2=O |r,c:12|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Biotinylated GSK3 alpha Substrate Peptide
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
1041.12
Organism:
n/a
Description:
n/a
Residue:
10
Sequence:
SGRARTSSFA