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Synonyms: AG-L-66494 | GNF-Pf-3800
Compound class: Synthetic organic
Comment: This compound is a mixture of tautomers (KP372-1A and KP372-1B), present in almost equal amounts. Our image shows the structure of KP372-1B.
This compound has been shown to directly inhibit both PDK1 and Akt activities in in vitro kinase assays in a dose-dependent manner and block cellular phosphorylation of Akt at both Ser473 and Thr308 residues .
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011)
Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity.
Nat. Biotechnol., 29 (11): 1039-45. [PMID:22037377]
2. Gao Y, Davies SP, Augustin M, Woodward A, Patel UA, Kovelman R, Harvey KJ. (2013)
A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
Biochem. J., 451 (2): 313-28. [PMID:23398362]
3. Koul D, Shen R, Bergh S, Sheng X, Shishodia S, Lafortune TA, Lu Y, de Groot JF, Mills GB, Yung WK. (2006)
Inhibition of Akt survival pathway by a small-molecule inhibitor in human glioblastoma.
Mol. Cancer Ther., 5 (3): 637-44. [PMID:16546978]
4. Mandal M, Kim S, Younes MN, Jasser SA, El-Naggar AK, Mills GB, Myers JN. (2005)
The Akt inhibitor KP372-1 suppresses Akt activity and cell proliferation and induces apoptosis in thyroid cancer cells.
Br. J. Cancer, 92 (10): 1899-905. [PMID:15870708]
5. Mandal M, Younes M, Swan EA, Jasser SA, Doan D, Yigitbasi O, McMurphey A, Ludwick J, El-Naggar AK, Bucana C et al.. (2006)
The Akt inhibitor KP372-1 inhibits proliferation and induces apoptosis and anoikis in squamous cell carcinoma of the head and neck.
Oral Oncol., 42 (4): 430-9. [PMID:16442835]
6. Zeng Z, Samudio IJ, Zhang W, Estrov Z, Pelicano H, Harris D, Frolova O, Hail Jr N, Chen W, Kornblau SM et al.. (2006)
Simultaneous inhibition of PDK1/AKT and Fms-like tyrosine kinase 3 signaling by a small-molecule KP372-1 induces mitochondrial dysfunction and apoptosis in acute myelogenous leukemia.
Cancer Res., 66 (7): 3737-46. [PMID:16585200]