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Synonyms: AR-12 | OSU03012
Compound class: Synthetic organic
Comment: OSU-03012 is a potent inhibitor of recombinant 3-phosphoinositide dependent protein kinase 1 (PDK1). Its discovery is described in , where it is compound 34. The PDK1/Akt signaling pathway plays a key role in cancer cell growth, survival, and tumour angiogenesis and represents a promising target for oncology therapeutics [1-2].
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. Hanada M, Feng J, Hemmings BA. (2004)
Structure, regulation and function of PKB/AKT--a major therapeutic target.
Biochim Biophys Acta, 1697 (1-2): 3-16. [PMID:15023346]
2. Shiojima I, Walsh K. (2002)
Role of Akt signaling in vascular homeostasis and angiogenesis.
Circ Res, 90 (12): 1243-50. [PMID:12089061]
3. Zhu J, Huang JW, Tseng PH, Yang YT, Fowble J, Shiau CW, Shaw YJ, Kulp SK, Chen CS. (2004)
From the cyclooxygenase-2 inhibitor celecoxib to a novel class of 3-phosphoinositide-dependent protein kinase-1 inhibitors.
Cancer Res, 64 (12): 4309-18. [PMID:15205346]