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Version: 17.06d (Release date: 2017-06-26)
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PDK1 Inhibitor AR-12 (Code C88271)

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Terms & Properties

Preferred Name: PDK1 Inhibitor AR-12

Definition: An orally bioavailable, small-molecule, celecoxib-derived inhibitor of phosphoinositide-dependent kinase-1 (PDK1) with potential antineoplastic activity. Devoid of any COX inhibiting activity, PDK1 inhibitor AR-12 binds to and inhibits the phosphorylation of 3-phosphoinositide-dependent kinase-1 (PDK-1).; subsequently, the phosphorylation and activation of the serine/threonine protein kinase Akt (protein kinase B or PKB) is inhibited, which may result in inhibition of the PI3K/Akt signaling pathway, inhibition of tumor cell proliferation, and the induction of tumor cell apoptosis. In addition, this agent appears to induce the activity of protein kinase R-like endoplasmic reticulum kinase (PERK), which plays a key role in the endoplasmic reticulum stress pathway. Activation and dysregulation of the PI3K/Akt signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K/Akt signaling may contribute to tumor resistance to a variety of antineoplastic agents.

Label: PDK1 Inhibitor AR-12

NCI Thesaurus Code: C88271 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: C1569671  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)
PDK1 Inhibitor AR-12

External Source Codes: 
CAS Registry Number 742112-33-0 (see NLM ChemIDplus info)
PDQ Closed Trial Search ID 655950
PDQ Open Trial Search ID 655950 (check for NCI PDQ open clinical trial info)
UMLS CUI C1569671

Other Properties:
     Name Value (qualifiers indented underneath)
code C88271
Contributing_Source FDA
Semantic_Type Pharmacologic Substance

Additional Concept Data: 
Defined Fully by Roles: No  


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