Catalog No.: PC-21767Not For Human Use, Lab Use Only.
AAA-237 (AAA237) is a small molecule Skp2 E3 ligase inhibitor, binds to Skp2 protein (KD=28.77 uM) and inhibits the degradation of Skp2 substrates, inhibits the proliferation of the NSCLC cells.
AAA-237 (AAA237) is a small molecule Skp2 E3 ligase inhibitor, binds to Skp2 protein (KD=28.77 uM) and inhibits the degradation of Skp2 substrates, inhibits the proliferation of the NSCLC cells. AAA-237 has no significant effect on the mRNA expression of Skp2 but inhibits the protein expression of Skp2 in NSCLC cells in a time-dependent manner. AAA-237 increases the expression levels of p21Cip1 and p27Kip1 in A549 and H1299 cells. AAA-237 inhibits the proliferation of A549 and H1299 cells in a dose- and time-dependent manner, inhibits colony formation of A549 and H1299 cells. AAA-237 arrests the cell cycle at the G0/G1 checkpoint by regulating the Skp2-Cip/Kip and PI3K/Akt-FOXO1 signaling pathways. AAA-237 (15 or 45 mg/kg) suppresses growth of xenograft tumors by inducing apoptosis and senescence in lung cancer A549 xenograft mice model.
