The search textbox has an autosuggest feature. When you enter three or more characters,
a list of up to 10 suggestions will popup under the textbox. Use the arrow keys
to move through the suggestions. To select a suggestion, hit the enter key. Using
the escape key closes the listbox and puts you back at the textbox. The radio buttons
allow you to toggle between having all search items start with or contain the text
you entered in the search box.
PDK1 inhibitor AR-12
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. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)
Code name: | AR-12 | ||
Chemical structure: | 2-amino-N-[4-[5-(2 phenanthrenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl] phenyl]-acetamide | ||