Skp2 inhibitor 1 is a Skp2-Cks1 interaction inhibitor (IC50: 2.8μM) with antitumor activity and can be used to study cancer.

MGC-803 cells:7.0 μM, PC-3 cells:4.8 μM

Skp2 inhibitor 1 (2.8 μM, 72 h) was able to interfere with the interaction between Skp2 and Cks1, with IC50 values of 4.8 μM and 7.0 μM for PC-3 and MGC-803 cells, respectively. [1]
At a concentration of 10 μM, after 48 h treatment, Skp2 inhibitor 1 was able to inhibit the proliferation and migration of PC-3 and MGC-803 cells, induced cell arrest in S phase, and promoted apoptosis. [1]

Skp2 inhibitor 1, administered at doses of 10 mg/kg, 25 mg/kg, and 50 mg/kg via intragastric administration every two days over a 21-day period, significantly suppressed tumor growth in xenograft models of PC-3 and MGC-803 cells within NOD-SCID mice, showing no notable toxicity. A dose of 50 mg/kg (every 2 days) completely inhibited tumor growth [1]. The compound functions by inhibiting the Skp2 signaling pathway, thereby reducing tumor malignancy and increasing apoptotic cell proportions in tumor tissues [1]. The tumor growth inhibition ratios were 55.68%, 71.86%, and 90.42% for 10, 25, and 50 mg/kg respectively.