tcsc0035401 PK11007

PK11007 is a p53 targeting compound, has anti-tumor activities through activation of unstable p53.

IC50 & Target: p53^[1]

In Vitro: PK11007 (15-30 µM) reduces the viability of mutant p53 cell lines MKN1 (V143A), HUH-7 (Y220C), NUGC-3 (Y220C), and SW480 (R273H/P309S). PK11007 also shows inhibitory activities against the p53 wt cancer cell lines HUH-6 and NUGC-4, as well as the fibroblast cell line WI-38 only at high concentrations (60 and 120 µM). PK11007 increases levels of p53 target genes and activates the unfolded protein response pathway. PK11007 also increases p53 activity in HUH-6 and NUGC-4 cells. PK11007 induces cell death via caspase-independent pathways. PK11007 (30, 60 µM) induces reactive oxygen species (ROS) especially in mutant p53 cells^[1]. PK11007 inhibits the proliferation of a panel of 17 breast cell lines, with IC₅₀s ranging from 2.3 to 42.2 μM^[2].