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Target
RAC-alpha serine/threonine-protein kinase [139-480,S378A,S381A,T450D,S473D]
Ligand
BDBM16939
Substrate
biotinylated Akt peptide substrate
Meas. Tech.
Akt Kinase Assay
IC50
3.3±n/a nM
Citation
Zhu, GD; Gandhi, VB; Gong, J; Luo, Y; Liu, X; Shi, Y; Guan, R; Magnone, SR; Klinghofer, V; Johnson, EF; Bouska, J; Shoemaker, A; Oleksijew, A; Jarvis, K; Park, C; Jong, RD; Oltersdorf, T; Li, Q; Rosenberg, SH; Giranda, VL Discovery and SAR of oxindole-pyridine-based protein kinase B/Akt inhibitors for treating cancers. Bioorg Med Chem Lett 16:3424-9 (2006) [PubMed] Article
More Info.:
Target
Name:
RAC-alpha serine/threonine-protein kinase [139-480,S378A,S381A,T450D,S473D]
Synonyms:
AKT1 | AKT1_HUMAN | C-AKT | PKB | Protein kinase B (Akt 1) | Protein kinase B alpha | RAC | RAC-PK-alpha
Type:
Enzyme
Mol. Mass.:
39513.28
Organism:
Human
Description:
Recombinant His-tagged Akt1 (S378A, S381A, T450D,
S473D; 139-480)
Residue:
342
Sequence:
AKPKHRVTMNEFEYLKLLGKGTFGKVILVKEKATGRYYAMKILKKEVIVAKDEVAHTLTENRVLQNSRHPFLTALKYSFQTHDRLCFVMEYANGGELFFHLSRERVFSEDRARFYGAEIVSALDYLHSEKNVVYRDLKLENLMLDKDGHIKITDFGLCKEGIKDGATMKTFCGTPEYLAPEVLEDNDYGRAVDWWGLGVVMYEMMCGRLPFYNQDHEKLFELILMEEIRFPRTLGPEAKALLAGLLKKDPKQRLGGGSEDAKEIMQHRFFAGIVWQHVYEKKLSPPFKPQVTSETDTRYFDEEFTAQMITIDPPDQDDSMECVDSERRPHFPQFDYSASGTA
Inhibitor
Name:
BDBM16939
Synonyms:
(3Z)-5-{5-[(2S)-2-amino-3-(1H-indol-3-yl)propoxy]pyridin-3-yl}-3-(cyclopropylmethylidene)-2,3-dihydro-1H-indol-2-one | Z/E=1:1 | oxindole pyridine, 11a
Type:
Small organic molecule
Emp. Form.:
C28H26N4O2
Mol. Mass.:
450.5316
SMILES:
N[C@H](COc1cncc(c1)-c1ccc2NC(=O)\C(=C/C3CC3)c2c1)Cc1c[nH]c2ccccc12 |r|
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