NSC 694621 is a PCAF and histone acetyltransferase (HAT) inhibitor that forms a covalent bond with Cys574, the active site of PCAF, thereby irreversibly inhibiting its acetyltransferase activity, and is able to inhibit the proliferation of SK-N-SH and HCT116 cells, which has anticancer potential.

PCAF (HAT) H4 (2–24):1.59 μM, SK-N-SH neuroblastoma cells:19.2 ± 1.22 μM (GI₅₀), PCAF (HAT) H3 (1–21): 5.19 μM

NSC 694621 可抑制 PCAF HAT 活性，对 H3 的 IC₅₀ 为 5.19 μM，对 H4 为 1.59 μM，对 H4 的抑制更强 [1]。NSC 694621 在 SK-N-SH 神经母细胞瘤细胞中表现出中等抗增殖活性，GI₅₀ 为 19.2 ± 1.22 μM。在 HCT116 结直肠癌细胞中，25 μM 浓度下抑制率为 29% [1]。