PCNA-I1

PCNA-I1 is an inhibitor of proliferating cell nuclear antigen (PCNA) that binds to PCNA trimers (K_d = 0.41 µM) and dose-dependently reduces the level of PCNA associated with chromatin in PC3 cells.¹ It preferentially inhibits growth of a variety of human and mouse cancer cell lines (IC₅₀s = 0.05-0.3 µM) over non-transformed cells (IC₅₀s = 0.99-2 µM). PCNA-I1 leads to an accumulation of cells in the G₁ phase during the first 24 hours of incubation and halts the cell cycle in the S and G₂/M phases by 72 hours following treatment. It also reduces tumor growth in an LNCaP prostate cancer mouse xenograft model when administered at a dose of 10 mg/kg, five days per week, for two weeks.²

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1. Tan, Z., Wortman, M., Dillehay, K.L., et al. Small-molecule targeting of proliferating cell nuclear antigen chromatin association inhibits tumor cell growth. Mol. Pharmacol. 81(6), (2012).

2. Dillehay, K.L., Lu, S., and Dong, Z. Antitumor effects of a novel small molecule targeting PCNA chromatin association in prostate cance. Mol. Cancer Ther. 13(12), 2817-2826 (2014).