Reaction Details
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RAC-beta serine/threonine-protein kinase
Ligand
BDBM16954
Substrate
biotinylated Akt peptide substrate
Meas. Tech.
Akt Kinase Assay
pH
7.5000±n/a
Temperature
295.1500±n/a K
IC50
5±n/a nM
Citation
Zhu, GD; Gong, J; Claiborne, A; Woods, KW; Gandhi, VB; Thomas, S; Luo, Y; Liu, X; Shi, Y; Guan, R; Magnone, SR; Klinghofer, V; Johnson, EF; Bouska, J; Shoemaker, A; Oleksijew, A; Stoll, VS; De Jong, R; Oltersdorf, T; Li, Q; Rosenberg, SH; Giranda, VL Isoquinoline-pyridine-based protein kinase B/Akt antagonists: SAR and in vivo antitumor activity. Bioorg Med Chem Lett 16:3150-5 (2006) [PubMed] Article More Info.:
Target
Name:
RAC-beta serine/threonine-protein kinase
Synonyms:
Serine/threonine-protein kinase AKT | RAC-PK-beta | Protein kinase Akt-2 | Protein kinase B beta (AKT2) | RAC-alpha serine/threonine-protein kinase (AKT2) | RAC-beta serine/threonine-protein kinase | Protein kinase B, beta | PKB beta | Protein kinase B (Akt 2) | RAC-beta serine/threonine-protein kinase (AKT2) | Serine/threonine-protein kinase Rac alpha/beta | Serine/threonine-protein kinase AKT2 | AKT2_HUMAN | AKT2
Type:
Enzyme
Mol. Mass.:
55766.64
Organism:
Human
Description:
n/a
Residue:
481
Sequence:
MNEVSVIKEGWLHKRGEYIKTWRPRYFLLKSDGSFIGYKERPEAPDQTLPPLNNFSVAECQLMKTERPRPNTFVIRCLQWTTVIERTFHVDSPDEREEWMRAIQMVANSLKQRAPGEDPMDYKCGSPSDSSTTEEMEVAVSKARAKVTMNDFDYLKLLGKGTFGKVILVREKATGRYYAMKILRKEVIIAKDEVAHTVTESRVLQNTRHPFLTALKYAFQTHDRLCFVMEYANGGELFFHLSRERVFTEERARFYGAEIVSALEYLHSRDVVYRDIKLENLMLDKDGHIKITDFGLCKEGISDGATMKTFCGTPEYLAPEVLEDNDYGRAVDWWGLGVVMYEMMCGRLPFYNQDHERLFELILMEEIRFPRTLSPEAKSLLAGLLKKDPKQRLGGGPSDAKEVMEHRFFLSINWQDVVQKKLLPPFKPQVTSEVDTRYFDDEFTAQSITITPPDRYDSLGLLELDQRTHFPQFSYSASIRE
Inhibitor
Name:
BDBM16954
Synonyms:
6-{5-[(2S)-2-amino-3-(1H-indol-3-yl)propoxy]-2-chloropyridin-3-yl}isoquinoline | Isoquinoline-pyridine, 10a
Type:
Small organic molecule
Emp. Form.:
TBD
Mol. Mass.:
TBD
SMILES:
TBD
Substrate
Name:
biotinylated Akt peptide substrate
Synonyms:
n/a
Type:
Biotinylated Peptide
Mol. Mass.:
3178.04
Organism:
n/a
Description:
Km=15 uM
Residue:
28
Sequence:
ITINAHEELSPFRGRSRSAPPNLWAAQR
