Wnt-p53 inhibitor compound 2

Modify Date: 2024-04-02 17:11:26

Wnt-p53 inhibitor compound 2 Structure
Wnt-p53 inhibitor compound 2 structure
Common Name Wnt-p53 inhibitor compound 2
CAS Number 1448427-02-8 Molecular Weight 371.455
Density N/A Boiling Point N/A
Molecular Formula C19H21N3O3S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of 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.

 Names

Name Wnt-p53 inhibitor compound 2

 Wnt-p53 inhibitor compound 2 Biological Activity

Description 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 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

 Chemical & Physical Properties

Molecular Formula C19H21N3O3S
Molecular Weight 371.455