OSU-03012

Описание

Cyclooxygenase-2 (COX-2) appears to play a significant role in the development and progression of cancer and COX-2 inhibitors such as celecoxib exhibit anti-cancer activity. OSU03012 is an analog of celecoxib that exhibits anti-cancer activity in a COX-2-independent manner via inhibition of the phosphatidyl inositol-3-kinase/Akt pathway. It has an IC₅₀ value of 5 μM for inhibition of 3-phosphoinositide-dependent kinase-1, and therefore Akt activation, with no measurable COX-2 inhibition up to 50 μM. OSU03012 is a potent inhibitor of tumor cell growth with an average inhibitory concentration of 1.1 μM across a panel of 60 cancer cell lines. It does not inhibit signal transduction through the mitogen-activated protein kinase (MAPK) pathway. OSU03012 induces apoptosis of chronic lymphocytic leukemia cells independent of bcl-2 overexpression using both caspase-dependent and independent pathways.

Использование

OSU 03012 is a PDK1 inhibitor and inducer of caspase and p53-independent apoptosis, also used in the development of anticancer agents by modification of novel immunosuppressant FTY720 and PDK1 inhibitor OSU-03012, compound for treating Alzheimers diseases.

Определение

ChEBI: A member of the class of pyrazoles that is N-[4-(pyrazol-1-yl)phenyl]glycinamide in which the pyrazole ring is substituted at positions 3 and 5 by trifluoromethyl and phenanthrene-2-yl groups respectively.