444930-42-1

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. 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.

PCNA-I1 is a potent PCNA (proliferating cell nuclear antigen) inhibitor. PCNA-I1 directly binds PCNA trimers with a Kd of 0.41 μM and exhibits antitumor activity both in vitro and in vivo[1].

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[1] Tan Z, et al. Small-molecule targeting of proliferating cell nuclear antigen chromatin association inhibits tumor cell growth. Mol Pharmacol. 2012 Jun;81(6):811-9. DOI:10.1124/mol.112.077735