Skp2 Inhibitor 1

Skp2 inhibitor 1 is an inhibitor of the protein-protein interaction between S-phase kinase-associated protein 2 (SKP2) and cyclin-dependent kinases regulatory subunit 1 (CKS1; IC₅₀ = 2.8 µM in an HTRF assay).¹ It selectively reduces the viability of H1299 lung, MGC803 gastric, and ES-2 ovarian cancer cells with high SKP2 expression (IC₅₀s = 3.6, 7, and 3.6 µM, respectively) over A549 lung, NCI N87 gastric, and A2780 ovarian cancer cells with low SKP2 expression (IC₅₀s = 18.2, 15.5, and 14.3 µM, respectively). It also reduces colony formation and migration and induces cell cycle arrest at the S phase and apoptosis in MGC803 and PC3 cells. Skp2 inhibitor 1 (10 and 25 mg/kg every two days) induces intratumoral apoptosis and reduces tumor growth and weight in a PC3 mouse xenograft model with complete tumor growth suppression at a dose of 50 mg/kg every two days.

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1. Zhang, K., Hu, K., Li, Q., et al. Discovery of novel 1,3-diphenylpyrazine derivatives as potent S-phase kinase-associated protein 2 (Skp2) inhibitors for the treatment of cancer. J. Med. Chem. 66(11), 7221-7242 (2023).