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SCFSkp2-IN-2 (Compound AAA-237) is a Skp2 inhibitor with a K D of 28.77 μM. AAA-237 induces apoptosis of NSCLC cells and shows antitumor activities
In Vitro
SCFSkp2-IN-2 (Compound AAA-237) (0.3-3 μM; 24-72 h) can directly bind to Skp2, causing the degradation of Skp2 by proteasome. 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. SCFSkp2-IN-2 (0.3-3 μM; 24-72 h) inhibits the proliferation of A549 and H1299 cells in a dose- and time-dependent manner. SCFSkp2-IN-2 (0.3-3 μM; 24-72 h) arrests the cell cycle at the G0/G1 checkpoint by regulating the Skp2-Cip/Kip and PI3K/Akt-FOXO1 signaling pathways. SCFSkp2-IN-2 (0.3-3 μM; 24-72 h) induces apoptosis of A549 and H1299 cells in a dose- and time-dependent manner. SCFSkp2-IN-2 (0.3 μM; 1-7 days) induces cellular senescence of the NSCLC cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: A549 and H1299 cells Concentration: 0.3, 1 and 3 μM Incubation Time: 24, 48 and 72 h Result: Increased the expression levels of p21Cip1 and p27Kip1. Decreased the level of Skp2. Reduced the expression levels of CDK2, p-CDK2, cyclin E1, CDK4, p-CDK4 and cyclin D. Increased the levels of cleaved PARP, cleaved caspase 3, cleaved caspase 9 and Bax. Decreased the expression of PARP and Bcl-2. Cell Proliferation AssayCell Line: A549 and H1299 cells Concentration: 0.3, 1 and 3 μM Incubation Time: 24, 48 and 72 h Result: Inhibited the proliferation of A549 and H1299 cells in a dose- and time-dependent manner. The IC 50 for A549 was 3 μM at 24 h, 2.5 μM at 48 h and 0.7 μM at 72 h. The IC 50 for H1299 was 3.9 μM at 24 h, 1.8 μM at 48 h and 1.1 μM at 72 h. Cell Cycle AnalysisCell Line: A549 and H1299 cells Concentration: 0.3, 1 and 3 μM Incubation Time: 24, 48 and 72 h Result: Arrested the cell cycle at G0/G1 in a dose- and time-dependent manner. Apoptosis AnalysisCell Line: A549 and H1299 cells Concentration: 0.3, 1 and 3 μM Incubation Time: 24, 48 and 72 h Result: The ratio of JC-1 monomer/JC-1 polymer was increased in A549 and H1299 cells as the concentration was increased.
In Vivo
SCFSkp2-IN-2 (Compound AAA-237) (15 or 45 mg/kg; i.p.; daily for 14 days) shows antitumor activity in lung cancer A549 xenograft mice model . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: A549 xenograft model Dosage: 15 or 45 mg/kg Administration: Intraperitoneal administration, daily for 14 days Result: Significantly reduced tumor volume and weight. The tumor growth inhibition of the low dose and high dose was 55% and 64%, respectively. No obvious weight loss or abnormal behavior was observed. Reduced the expression of Ki67 in tumor tissue. Reduced the expression of Skp2 and Bcl-2 and increased the expression of p27, the cleaving of caspase 3, caspase 9, PARP and Bax.
IC50& Target:KD: 28.77 μM (Skp2)
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