Wnt-p53 inhibitor compound 2

Wnt-p53 inhibitor compound 2 is a novel inhibitor targets both Wnt signaling and ATM/p53, potently inhibits Wnt transcription (IC50=11 nM) and p53 transcription (EC50=1.9 nM); decreases HCT-116 CRC cell viability (IC50=10 nM) and proliferation (IC50=8 nM), decreases DLD-1, SW480 and 10.1 cancer cell viability (IC50=12, 27 and 41 nM) and proliferation (IC50=18,15 and 13 nM); compound 2 potently activates apoptosis of HCT-116, DLD-1 and SW480 cells (EC50=13, 15 and 18 nM) in a p53-dependent manner; inhibits cell migration and invasion in HCT-116 at 20-200 nM, also modulates mitotic stress signaling, leading to both inhibition of Wnt responsiveness and stabilization and activation of p53 to cause cell cycle arrest; induces cell death and inhibits tumor growth in mouse xenografts (20 mg/kg/day, i.p.), without acute cytotoxicity nor toxicity.

References 1. Cheng J, et al. Cancer Res. 2018 Jul 21. pii: canres.2642.2017. doi: 10.1158/0008-5472.CAN-17-2642. View Related Products by Target Wnt