Preferred Label : PDK1 Inhibitor AR-12;
NCIt related terms : AR-12;
NCIt 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.;
UNII : EX3O2Q61UV;
InChIKey : YULUCECVQOCQFQ-UHFFFAOYSA-N;
CAS number : 742112-33-0;
Molecule name : AR-12;
Origin ID : C88271;
UMLS CUI : C2981794;
Semantic type(s)
- concept_is_in_subset
- has_target
