zinc-95605533

T2AA (4-[4-[(2S)-2-amino-3-hydroxypropyl]-2,6-diiodophenoxy]phenol) 是一种增殖细胞核抗原 (PCNA) 抑制剂，对 PCNA PIP-box 肽相互作用的 IC50 为 1 μM。 T2AA 通过停止 DNA 复制叉和抑制 PCNA 与 DNA 聚合酶 δ 的相互作用来引起 DNA 复制压力并抑制癌细胞生长。

T2AA, a proliferating cell nuclear antigen (PCNA) inhibitor, disrupts protein-protein interactions between PCNA and both a PIP-box-containing peptide (IC50= 1 μM) and full-length p21, reducing cellular colocalization of PCNA with DNA polymerase δ. This compound effectively inhibits DNA replication and cell proliferation in U2OS and HeLa cells in a concentration-dependent manner, additionally inducing S phase cell cycle arrest at a 20 μM concentration. Furthermore, T2AA enhances DNA double strand break formation alongside cisplatin in a neutral comet assay and augments cisplatin-induced reductions in clonogenic survival in HeLa and U2OS cells.