SCFSkp2-IN-2 functions as a Skp2 inhibitor, possessing a KD of 28.77 μM. Meanwhile, AAA-237 induces apoptosis in non-small cell lung cancer (NSCLC) cells and exhibits antitumor activities[1].
体内研究
SCFSkp2-IN-2, administered intraperitoneally at dosages of 15 or 45 mg/kg daily for 14 days, demonstrates antitumor activity in a lung cancer A549 xenograft mice model[1].
体外研究
SCFSkp2-IN-2, in concentrations ranging from 0.3 to 3 μM over a duration of 24 to 72 hours, directly binds to Skp2, leading to its degradation via the proteasome. AAA-237 does not significantly impact the mRNA expression of Skp2 but does inhibit its protein expression in NSCLC cells, showing a time-dependent effect[1].
SCFSkp2-IN-2, within the same concentration and time frame, impedes the proliferation of A549 and H1299 cells in a manner reliant on dosage and duration[1].
SCFSkp2-IN-2, within the same concentration and time frame, halts the cell cycle at the G0/G1 checkpoint by modulating the Skp2-Cip/Kip and PI3K/Akt-FOXO1 signaling pathways[1].
SCFSkp2-IN-2, under the same conditions, induces apoptosis in A549 and H1299 cells, with its effect contingent upon both dosage and duration[1].
SCFSkp2-IN-2, at a concentration of 0.3 μM over a span of 1 to 7 days, triggers cellular senescence in NSCLC cells[1].
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