PCAF-IN-2 (compound 17) is a potent PCAF inhibitor with an IC50 value of 5.31 µM. PCAF-IN-2 shows anti-tumour activity. CAF-IN-2 induces apoptosis and arrest the cell cycle at the G2/M phase[1].
PCAF-IN-2 shows anti-tumour activity with IC50s of 3.06, 5.69, 7.56, 2.83 µM for HePG2, MCF-7, PC3, HCT-116 cells, respectively[1].
PCAF-IN-2 (10 µM; 24 h) induces apoptosis and arrest the cell cycle at the G2/M phase in HePG2 cells[1].
[1]. Turky A, et al. Design, synthesis, and antitumor activity of novel compounds based on 1,2,4-triazolophthalazine scaffold: Apoptosis-inductive and PCAF-inhibitory effects. Bioorg Chem. 2020 Aug;101:104019.